Pub Date : 2022-01-01DOI: 10.12677/hjmce.2022.102016
珊 刘
Peficitinib is a novel Janus kinase 1 and Janus kinase 3 inhibitor developed by Astellas, a Japa-nese company. Peficitinib mainly treats the moderate or severe rheumatoid arthritis with in-刘珊 adequate response to methotrexate. At present, there are very few papers on the synthesis route of Peficitinib. In this paper, a complete synthesis route is designed, and then each step of the reaction is studied and optimized. Starting from 7-azindole, the target compound was obtained through seven steps including halogenation, substitution (upper protection), esterification, de-protection, ester hydrolysis, amidation and then substitution. By providing catalyst or changing other reaction conditions such as solvent, temperature and molar ratio of reactants, a reasona-ble route, high yield, short time and simple operation of Peficitinib synthesis process was suc-cessfully obtained, and the synthesis of Peficitinib can reach industrial production. The struc-tures of the target compounds and intermediates were confirmed by 1 H NMR, and the total yield of the route was 32.8%.
{"title":"Study on Synthesis and Optimization of Syn-thesis Technology of JAK Inhibitor Peficitinib","authors":"珊 刘","doi":"10.12677/hjmce.2022.102016","DOIUrl":"https://doi.org/10.12677/hjmce.2022.102016","url":null,"abstract":"Peficitinib is a novel Janus kinase 1 and Janus kinase 3 inhibitor developed by Astellas, a Japa-nese company. Peficitinib mainly treats the moderate or severe rheumatoid arthritis with in-刘珊 adequate response to methotrexate. At present, there are very few papers on the synthesis route of Peficitinib. In this paper, a complete synthesis route is designed, and then each step of the reaction is studied and optimized. Starting from 7-azindole, the target compound was obtained through seven steps including halogenation, substitution (upper protection), esterification, de-protection, ester hydrolysis, amidation and then substitution. By providing catalyst or changing other reaction conditions such as solvent, temperature and molar ratio of reactants, a reasona-ble route, high yield, short time and simple operation of Peficitinib synthesis process was suc-cessfully obtained, and the synthesis of Peficitinib can reach industrial production. The struc-tures of the target compounds and intermediates were confirmed by 1 H NMR, and the total yield of the route was 32.8%.","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66075281","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 : 2022-01-01DOI: 10.12677/hjmce.2022.102017
婕 刘
{"title":"Research on Formulation Process of Ginkgo biloba Extract Sodium Chloride Injection","authors":"婕 刘","doi":"10.12677/hjmce.2022.102017","DOIUrl":"https://doi.org/10.12677/hjmce.2022.102017","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66076290","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 : 2022-01-01DOI: 10.12677/hjmce.2022.103026
文颖 郑
{"title":"Process Study on the Preparation of Probiotic Oral Tablets Based on Microencapsulation","authors":"文颖 郑","doi":"10.12677/hjmce.2022.103026","DOIUrl":"https://doi.org/10.12677/hjmce.2022.103026","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66076620","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 : 2022-01-01DOI: 10.12677/hjmce.2022.102010
倩 曾
{"title":"Determination of Lupanone and Stigmasterol in the Roots, Stems and Leaves of Musa japonica by HPLC","authors":"倩 曾","doi":"10.12677/hjmce.2022.102010","DOIUrl":"https://doi.org/10.12677/hjmce.2022.102010","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"41 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66074824","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 : 2022-01-01DOI: 10.12677/hjmce.2022.103030
腾荣 黄
{"title":"Research Progress of the Pharmacological Action of the Effective Components in Centipeda minima on Allergic Rhinitis","authors":"腾荣 黄","doi":"10.12677/hjmce.2022.103030","DOIUrl":"https://doi.org/10.12677/hjmce.2022.103030","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66076840","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 : 2022-01-01DOI: 10.12677/hjmce.2022.104032
双扣 陈
{"title":"Virtual Screening of Bursaphelenchus xylophilus AChE Inhibitors Based on Molecular Docking from the Natural Products Database","authors":"双扣 陈","doi":"10.12677/hjmce.2022.104032","DOIUrl":"https://doi.org/10.12677/hjmce.2022.104032","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66077048","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 : 2022-01-01DOI: 10.12677/hjmce.2022.104033
思 唐
{"title":"Virtual Screening of Phosphoethanolamine Methyltransferase, PEAMT Inhibitors Based on Molecular Docking","authors":"思 唐","doi":"10.12677/hjmce.2022.104033","DOIUrl":"https://doi.org/10.12677/hjmce.2022.104033","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66077165","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 : 2022-01-01DOI: 10.12677/hjmce.2022.104036
特 姜
{"title":"Advances in Chemical Constituents and Pharmacological Effects of Polygonum capitatum","authors":"特 姜","doi":"10.12677/hjmce.2022.104036","DOIUrl":"https://doi.org/10.12677/hjmce.2022.104036","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66077291","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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