Pub Date : 2020-06-10DOI: 10.5772/intechopen.81146
Sundaram Singh, S. Kumari
A novel, convenient one-pot multicomponent synthesis of tetraheterocy-clicbenzimidazolo/benzothiazolo quinazolin-1-one derivatives has been reported in the presence of tetraethylammonium superoxide under non-aqueous condition. The superoxide induced three-component reaction of various aromatic aldehydes, 2-aminobenzimadazole/2-aminobenzothiazole and dimedone/1,3- cyclohexane-dione produced tetraheterocyclicbenzimidazolo/benzothiazolo quinazolin-1-one derivatives at room temperature under the mild reaction conditions. The tetraethylammonium superoxide has been generated by phase transfer reaction of potassium superoxide and tetraethylammonium bromide in dry DMF at room temperature. The present study extended the applicability of tetraethylammonium bromide as a phase transfer catalyst for the efficient use of superoxide ion in multi-component synthesis of structurally diverse drug-like complex heterocycles (quinazolines). role of O 2 • − in living cells. Since the investigation has been performed at an ambient temperature in the presence of in situ generated O 2• − , the results may be easily correlated with those occurring at physiological temperatures in more complex biological counterparts. A novel synthetic route has been developed for the synthesis of tetraheterocyclic benzimidazolo/benzothiazolo quinazolin-1-one ring systems using tetraethylammonium superoxide under non aqueous condition at room temperature (mild reaction condition) within 6 h. The yield of the products was obtained up to 88% without using any tedious purification process. The applicability of tetraethylammonium bromide as an inexpensive alternative to 18-crown-6 for superoxide ion generation has been extended in present report.
{"title":"One-Pot-Condensation Reaction of Heterocyclic Amine, 1,3-Diketone and Aldehydes Using In Situ Generated Superoxide Ion: A Rapid Synthesis of Structurally Diverse Drug-Like Complex Heterocycles","authors":"Sundaram Singh, S. Kumari","doi":"10.5772/intechopen.81146","DOIUrl":"https://doi.org/10.5772/intechopen.81146","url":null,"abstract":"A novel, convenient one-pot multicomponent synthesis of tetraheterocy-clicbenzimidazolo/benzothiazolo quinazolin-1-one derivatives has been reported in the presence of tetraethylammonium superoxide under non-aqueous condition. The superoxide induced three-component reaction of various aromatic aldehydes, 2-aminobenzimadazole/2-aminobenzothiazole and dimedone/1,3- cyclohexane-dione produced tetraheterocyclicbenzimidazolo/benzothiazolo quinazolin-1-one derivatives at room temperature under the mild reaction conditions. The tetraethylammonium superoxide has been generated by phase transfer reaction of potassium superoxide and tetraethylammonium bromide in dry DMF at room temperature. The present study extended the applicability of tetraethylammonium bromide as a phase transfer catalyst for the efficient use of superoxide ion in multi-component synthesis of structurally diverse drug-like complex heterocycles (quinazolines). role of O 2 • − in living cells. Since the investigation has been performed at an ambient temperature in the presence of in situ generated O 2• − , the results may be easily correlated with those occurring at physiological temperatures in more complex biological counterparts. A novel synthetic route has been developed for the synthesis of tetraheterocyclic benzimidazolo/benzothiazolo quinazolin-1-one ring systems using tetraethylammonium superoxide under non aqueous condition at room temperature (mild reaction condition) within 6 h. The yield of the products was obtained up to 88% without using any tedious purification process. The applicability of tetraethylammonium bromide as an inexpensive alternative to 18-crown-6 for superoxide ion generation has been extended in present report.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"126136482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-10DOI: 10.5772/intechopen.92030
B. Nandeshwarappa, G. Prakash, S. Sadashiv
{"title":"Introductory Chapter: Synthesis and Antimicrobial Activities of Dihydroazeto[2′,3′:4,5]seleno[2,3-b]quinolines","authors":"B. Nandeshwarappa, G. Prakash, S. Sadashiv","doi":"10.5772/intechopen.92030","DOIUrl":"https://doi.org/10.5772/intechopen.92030","url":null,"abstract":"","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128157502","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-06-10DOI: 10.5772/intechopen.81269
Roshan D. Nasare, M. Idrees, Satish S. Kola, Rajendra S. Dongre
Pharmaceutics and therapeutics industries enforced chemists to seek/discover antibacterial novel heterocycles owing specific bioactivity and innate characteristics significance. This chapter summarized potent antibacterial profile of 5-oxoimidazolines in the new millennium as an antibacterial against Gram-positive and Gram-negative bacteria viz. B. thuringiensis, S. aureus, E. coli, and E. aerogenes is presented in this chapter. 5-(H/Br benzofuran-2-yl)-1-phenyl 1H-pyrazole-3carbohydrazides are condensed with 4-(arylidene)-2 phenyloxazol-5(4H)-one in acetic acid at elevated temperature to yield product 5-(H/Br benzofuran-2-yl)-N(4-arylidene-5-oxo-2-phenyl-4,5-dihydroimidazol-1-yl)-1-phenyl-1H-pyrazole-3carboxamides. Different substrates like 4-(arylidene)-2-phenyloxazol-5(4H)-one allowed to react with benzaldehyde hippuric acid to yield 5-oxo-imidazolines/ 5-oxo-4,5-dihydroimidazole. All synthesized 5-oxo-imidazolines were characterized via elemental analysis and FT-IR, H-NMR and mass spectra techniques. All 5-oxo-imidazolines assayed in vitro for inherent antimicrobial activity at different concentration against stated bacterial strains and compared with standard chloramphenicol. 5-Oxo-imidazolines (3a and 3c) with 125 μg/mL concentration showed excellent antibacterial profile against Gram-positive bacteria, B. thuringiensis, while other derivatives at different concentrations showed moderate antibacterial activity against Gram-positive bacteria, S. aureus and B. thuringiensis. Gram-negative bacteria like E. coli and E. aerogenes are tested at higher concentration (1000, 500, and 125 μg/mL) and found good-to-moderate antibacterial activity. Tested products found non-active against E. aerogenes for 125, 61, and 31 μg/mL concentration also inactive at conc. 31 μg/mL against E. coli.
{"title":"Potent Antibacterial Profile of 5-Oxo-Imidazolines in the New Millennium","authors":"Roshan D. Nasare, M. Idrees, Satish S. Kola, Rajendra S. Dongre","doi":"10.5772/intechopen.81269","DOIUrl":"https://doi.org/10.5772/intechopen.81269","url":null,"abstract":"Pharmaceutics and therapeutics industries enforced chemists to seek/discover antibacterial novel heterocycles owing specific bioactivity and innate characteristics significance. This chapter summarized potent antibacterial profile of 5-oxoimidazolines in the new millennium as an antibacterial against Gram-positive and Gram-negative bacteria viz. B. thuringiensis, S. aureus, E. coli, and E. aerogenes is presented in this chapter. 5-(H/Br benzofuran-2-yl)-1-phenyl 1H-pyrazole-3carbohydrazides are condensed with 4-(arylidene)-2 phenyloxazol-5(4H)-one in acetic acid at elevated temperature to yield product 5-(H/Br benzofuran-2-yl)-N(4-arylidene-5-oxo-2-phenyl-4,5-dihydroimidazol-1-yl)-1-phenyl-1H-pyrazole-3carboxamides. Different substrates like 4-(arylidene)-2-phenyloxazol-5(4H)-one allowed to react with benzaldehyde hippuric acid to yield 5-oxo-imidazolines/ 5-oxo-4,5-dihydroimidazole. All synthesized 5-oxo-imidazolines were characterized via elemental analysis and FT-IR, H-NMR and mass spectra techniques. All 5-oxo-imidazolines assayed in vitro for inherent antimicrobial activity at different concentration against stated bacterial strains and compared with standard chloramphenicol. 5-Oxo-imidazolines (3a and 3c) with 125 μg/mL concentration showed excellent antibacterial profile against Gram-positive bacteria, B. thuringiensis, while other derivatives at different concentrations showed moderate antibacterial activity against Gram-positive bacteria, S. aureus and B. thuringiensis. Gram-negative bacteria like E. coli and E. aerogenes are tested at higher concentration (1000, 500, and 125 μg/mL) and found good-to-moderate antibacterial activity. Tested products found non-active against E. aerogenes for 125, 61, and 31 μg/mL concentration also inactive at conc. 31 μg/mL against E. coli.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128997549","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-01-02DOI: 10.5772/intechopen.90758
N. S. Goud, Pardeep Kumar, R. Bharath
Cancer is one of the major life burdens and around 18.1 million new cancer cases and 9.6 million deaths have been estimated in 2018 globally. Recent reports of the World Health Organization (WHO) stated that about one in six death cases globally is mainly due to cancer. Hence, the development of efficacious drugs with novel mechanisms is necessary for various cancer types. The chemotherapy drug resistance and non-selectivity toward targets have turned the current cancer research on to the highly emerging selective targets for the development of potential anticancer agents. Benzimidazole is regarded as an essential pharmacophore of the cancer research because of wide anticancer potentials with versatile mechanisms to inhibit the tumor progression and also facile synthetic strategies for an easy synthesis of various benzimidazole derivatives. The selective anticancer potentials also depend on the substitution of the benzimidazole nucleus. Therefore, it would lead to providing a path for the development of novel target-specific and highly effective benzimidazole-based anticancer agents.
{"title":"Recent Developments of Target-Based Benzimidazole Derivatives as Potential Anticancer Agents","authors":"N. S. Goud, Pardeep Kumar, R. Bharath","doi":"10.5772/intechopen.90758","DOIUrl":"https://doi.org/10.5772/intechopen.90758","url":null,"abstract":"Cancer is one of the major life burdens and around 18.1 million new cancer cases and 9.6 million deaths have been estimated in 2018 globally. Recent reports of the World Health Organization (WHO) stated that about one in six death cases globally is mainly due to cancer. Hence, the development of efficacious drugs with novel mechanisms is necessary for various cancer types. The chemotherapy drug resistance and non-selectivity toward targets have turned the current cancer research on to the highly emerging selective targets for the development of potential anticancer agents. Benzimidazole is regarded as an essential pharmacophore of the cancer research because of wide anticancer potentials with versatile mechanisms to inhibit the tumor progression and also facile synthetic strategies for an easy synthesis of various benzimidazole derivatives. The selective anticancer potentials also depend on the substitution of the benzimidazole nucleus. Therefore, it would lead to providing a path for the development of novel target-specific and highly effective benzimidazole-based anticancer agents.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131545168","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-12-17DOI: 10.5772/intechopen.90002
L. Kayukova, U. Jussipbekov, K. Praliyev
О ur task in the field of new derivatives of amidoximes was the elaboration for new medication with increased activity and lower toxicity than medications used in practice. Here are the results of the search for new painkillers and antitubercular and antidiabetic drugs in the class of amidoxime derivatives. Nitrous derivatives of α -chloro- α -isonitrosoacetone, O -aroyl- β -aminopropioamidoximes, and 3-[ β -(piper-idine-1-yl)]ethyl-5-aryl-1,2,4-oxadiazoles were tested for conduction, infiltration, and terminal anesthesia. Among them hit compounds were discovered. The search for new anti-TB drugs is executed in the world. Salts and bases of O -aroylation products of β -(thiomorpholin-1-yl) and β -(4-methylpiperazin-1-yl) propioamidoximes during in vitro antitubercular screening for DS, DR, and MDR strains of M. tuberculosis manifest themselves as highly active competitive compounds. In the series of the derivatives of β -aminopropioamidoximes, a search for new antidiabetic drugs was done. The compounds with pronounced antidiabetic properties were revealed. The obtained data of the most promising samples with a preliminary assessment of their average toxic dose in animals can be used in further in vivo testing of infiltration anesthesia conditions, of antidiabetic properties, and at the development of doses and new treatment regimens for TB.
{"title":"Amidoxime Derivatives with Local Anesthetic, Antitubercular, and Antidiabetic Activity","authors":"L. Kayukova, U. Jussipbekov, K. Praliyev","doi":"10.5772/intechopen.90002","DOIUrl":"https://doi.org/10.5772/intechopen.90002","url":null,"abstract":"О ur task in the field of new derivatives of amidoximes was the elaboration for new medication with increased activity and lower toxicity than medications used in practice. Here are the results of the search for new painkillers and antitubercular and antidiabetic drugs in the class of amidoxime derivatives. Nitrous derivatives of α -chloro- α -isonitrosoacetone, O -aroyl- β -aminopropioamidoximes, and 3-[ β -(piper-idine-1-yl)]ethyl-5-aryl-1,2,4-oxadiazoles were tested for conduction, infiltration, and terminal anesthesia. Among them hit compounds were discovered. The search for new anti-TB drugs is executed in the world. Salts and bases of O -aroylation products of β -(thiomorpholin-1-yl) and β -(4-methylpiperazin-1-yl) propioamidoximes during in vitro antitubercular screening for DS, DR, and MDR strains of M. tuberculosis manifest themselves as highly active competitive compounds. In the series of the derivatives of β -aminopropioamidoximes, a search for new antidiabetic drugs was done. The compounds with pronounced antidiabetic properties were revealed. The obtained data of the most promising samples with a preliminary assessment of their average toxic dose in animals can be used in further in vivo testing of infiltration anesthesia conditions, of antidiabetic properties, and at the development of doses and new treatment regimens for TB.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114527790","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-08-07DOI: 10.5772/INTECHOPEN.88547
Rohit Singh, S. Ganguly
Imidazole analogs have proved to be a very good source of medicinal agents. The various activities associated with these moieties include antibacterial, antifungal, anthelmintic, Anti HIV activity, anticancer, antihypertensive, analgesic, anti-inflammatory, anticonvulsant, sedative and other pharmacological activities.
{"title":"Azoles as Potent Antimicrobial Agents","authors":"Rohit Singh, S. Ganguly","doi":"10.5772/INTECHOPEN.88547","DOIUrl":"https://doi.org/10.5772/INTECHOPEN.88547","url":null,"abstract":"Imidazole analogs have proved to be a very good source of medicinal agents. The various activities associated with these moieties include antibacterial, antifungal, anthelmintic, Anti HIV activity, anticancer, antihypertensive, analgesic, anti-inflammatory, anticonvulsant, sedative and other pharmacological activities.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"122006942","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-29DOI: 10.5772/INTECHOPEN.88243
D. Jangid, Dr. Surbhi Dhadda
An environmentally friendly, economic synthetic protocol was advanced for synthesis of biologically and pharmacologically vital five- and six-membered heterocycles containing nitrogen, sulphur and oxygen as heteroatom. A series of thiazole derivatives was prepared by the reaction of substituted phenacyl halides and phenyl thiourea in the presence of TiO 2 nanoparticles (NPs) as nanocatalyst in DCM. Similarly, another series of six-membered heterocyclic compounds were synthesized by the reaction of phenacyl halides with phenylenediamine, 2-amino-phenol, 2-aminobenzenethiol to produce corresponding products (1,4-quinoxaline, benzoxazine, benzothiazine) under catalytic effect of TiO 2 nanocatalyst. Analytical and spectral (FTIR, 1 H and 13 C NMR and SEM) techniques were employed for the structural elucidation of the synthesized compounds.
{"title":"Phenacyl Bromide: An Organic Intermediate for Synthesis of Five- and Six-Membered Bioactive Heterocycles","authors":"D. Jangid, Dr. Surbhi Dhadda","doi":"10.5772/INTECHOPEN.88243","DOIUrl":"https://doi.org/10.5772/INTECHOPEN.88243","url":null,"abstract":"An environmentally friendly, economic synthetic protocol was advanced for synthesis of biologically and pharmacologically vital five- and six-membered heterocycles containing nitrogen, sulphur and oxygen as heteroatom. A series of thiazole derivatives was prepared by the reaction of substituted phenacyl halides and phenyl thiourea in the presence of TiO 2 nanoparticles (NPs) as nanocatalyst in DCM. Similarly, another series of six-membered heterocyclic compounds were synthesized by the reaction of phenacyl halides with phenylenediamine, 2-amino-phenol, 2-aminobenzenethiol to produce corresponding products (1,4-quinoxaline, benzoxazine, benzothiazine) under catalytic effect of TiO 2 nanocatalyst. Analytical and spectral (FTIR, 1 H and 13 C NMR and SEM) techniques were employed for the structural elucidation of the synthesized compounds.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134539486","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-17DOI: 10.5772/INTECHOPEN.88139
Dattatraya N. Pansare, Rohini N. Shelke
A highly efficient protocol was developed for the synthesis of 3-(indoline-1-carbonyl)-N-(substituted) benzene sulfonamide analogs with excellent yields. The new 3-(indoline-1-carbonyl)-N-(substituted) benzene sulfonamide derivatives (4a-g and 5a-g) were evaluated in vitro anticancer activity against a series of different cell lines like A549 (lung cancer cell), HeLa (cervical), MCF-7 (breast cancer cell) and Du-145 (prostate cancer cell) respectively. The results of the anticancer activity data revealed that most of the tested compounds showed IC 50 values from 1.98 to 9.12 μ M in different cell lines. Compounds 4b, 4d, 5d, and 5g were the most potent, with IC 50 values ranging from 1.98 to 2.72 μ M in different cell lines.
建立了一种合成3-(吲哚-1-羰基)- n -(取代)苯磺酰胺类似物的高效方法，收率高。新的3-(吲哚-1-羰基)- n -(取代)苯磺酰胺衍生物(4a-g和5a-g)分别对A549(肺癌细胞)、HeLa(宫颈癌细胞)、MCF-7(乳腺癌细胞)和Du-145(前列腺癌细胞)等不同细胞系进行了体外抗癌活性评价。抗肿瘤活性数据显示，大部分化合物在不同细胞系中的ic50值在1.98 ~ 9.12 μ M之间。化合物4b、4d、5d和5g对不同细胞系的ic50值在1.98 ~ 2.72 μ M之间。
{"title":"Synthesis and Anticancer Evaluation of Benzenesulfonamide Derivatives","authors":"Dattatraya N. Pansare, Rohini N. Shelke","doi":"10.5772/INTECHOPEN.88139","DOIUrl":"https://doi.org/10.5772/INTECHOPEN.88139","url":null,"abstract":"A highly efficient protocol was developed for the synthesis of 3-(indoline-1-carbonyl)-N-(substituted) benzene sulfonamide analogs with excellent yields. The new 3-(indoline-1-carbonyl)-N-(substituted) benzene sulfonamide derivatives (4a-g and 5a-g) were evaluated in vitro anticancer activity against a series of different cell lines like A549 (lung cancer cell), HeLa (cervical), MCF-7 (breast cancer cell) and Du-145 (prostate cancer cell) respectively. The results of the anticancer activity data revealed that most of the tested compounds showed IC 50 values from 1.98 to 9.12 μ M in different cell lines. Compounds 4b, 4d, 5d, and 5g were the most potent, with IC 50 values ranging from 1.98 to 2.72 μ M in different cell lines.","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121314230","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-12DOI: 10.5772/INTECHOPEN.88026
H. Venkatachalam, N. V. Kumar
The oxygen-containing heterocycles are an important class of compounds in organic chemistry. These compounds are used as drugs (coumarin and oxa-zole), solvent (tetrahydrofuran), flavors, and fragrances (lactones). The fusion of aromatic ring to the oxygen-heterocycle will change the electron density; thereby, the physical/chemical/biological properties will alter. Also, the preparation of these fused molecules will require a different strategy/method/reaction condition. The topics covered in this chapter are the general synthetic methods and uses of fused heterocyclic compounds containing oxygen as a heteroatom. The derivatization of the primary scaffold is excluded from this chapter. Some of the fused compounds are coumarin (benzopyrans) and piclozotan (benzoxazepines).
{"title":"The Oxygen-Containing Fused Heterocyclic Compounds","authors":"H. Venkatachalam, N. V. Kumar","doi":"10.5772/INTECHOPEN.88026","DOIUrl":"https://doi.org/10.5772/INTECHOPEN.88026","url":null,"abstract":"The oxygen-containing heterocycles are an important class of compounds in organic chemistry. These compounds are used as drugs (coumarin and oxa-zole), solvent (tetrahydrofuran), flavors, and fragrances (lactones). The fusion of aromatic ring to the oxygen-heterocycle will change the electron density; thereby, the physical/chemical/biological properties will alter. Also, the preparation of these fused molecules will require a different strategy/method/reaction condition. The topics covered in this chapter are the general synthetic methods and uses of fused heterocyclic compounds containing oxygen as a heteroatom. The derivatization of the primary scaffold is excluded from this chapter. Some of the fused compounds are coumarin (benzopyrans) and piclozotan (benzoxazepines).","PeriodicalId":385289,"journal":{"name":"Heterocycles - Synthesis and Biological Activities","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128308802","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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