Current organic synthesis最新文献

Aims: The small organic molecular compounds with biological activity containing C-C and C-N or C-O bonding were efficiently prepared without catalyst and solvent in the hydrothermal synthesis reactor.

Objectives: Our goal was to explore new applications for the more environmentally friendly and efficient synthesis of bis(indolyl)methyl, xanthene, quinazolinone, and N-heterocyclic derivatives in hydrothermal synthesis reactors under solvent-free and catalyst-free conditions.

Methods: A greener and more efficient method was successfully developed for the synthesis of bis(indolyl)methyl, heteroanthracene, quinazolinone, and N-heterocyclic derivatives using a hydrothermal synthesis reactor in a solvent- and catalyst-free manner.

Results: In a hydrothermal synthesis reactor, bis(indoyl)methyl, xanthene, quinazolinone, and N-heterocyclic derivatives were synthesized without catalysts and solvents.

Conclusion: Overall, it is proved once again that the catalyst-free and solvent-free synthesis method has universal value and is a more ideal and environmentally friendly new method, especially the hydrothermal reactor for synthesis.

Introduction: An efficient procedure was reported for the synthesis of novel hybrid dithiazoles 7 and thiazoles 15, in good yields, by applying hydrazonyl chlorides 4 with thiocarbohydrazone derivatives 3 and 12.

Methods: The thiazole derivatives were evaluated for their antimicrobial and antioxidant activities.

Results: According to the results, thiazoles revealed marked potency as antimicrobial and antioxidant agents. Thus, 7a's DPPH radical scavenging activity was excellent (38.19±0.33 and 14.37±0.4) at concentrations of 2.0 and 1.0 mg/mL, respectively. In addition, compound 3 exhibited activity against all bacterial strains tested, as evidenced by inhibition zones measuring that ranged from 8.5±0.43 mm for E. faecalis to 16.5±0.43 mm for S. mutans.

Conclusion: The MIC results showed that compound 3 was effective against E. coli, S. aureus, E. faecalis, P. aeruginosa, and S. mutans at concentrations of 1.0, 1.0, 2.0, 1.0, and 1.0 mg/mL, respectively. Furthermore, molecular docking has shown lower binding energy with different types of interactions at the active sites of Dihydropteroate synthase, Sortase A, LasR, and penicillin-binding protein pockets, indicating that these compounds could inhibit the enzyme and cause promising antimicrobial effects.

Background: Ripasudil hydrochloride or 4-Fluoro-5-{[(2S)-2-Methyl-1,4- diazepan-1-yl] sulfonyl isoquinoline hydrochloride known as K-115 is used for the treatment of glaucoma and ocular hypertension. In the API industry, to achieve and ensure the quality of drug substances, there is a need for impurity identification, synthesis, and characterization. The impurities are formed during the process, either side reaction or degradation or carried over from the starting material.

Objectives: The present study explores two new process impurities of Ripasudil Hydrochloride dihydrate, specifically Impurity-1(4-fluoro-5-{[(3R)-3-methyl-4-(2- nitrolbenzenesulfonyl)-1,4-diazepan-1-yl] sulfonyl} isoquino line) and Impurity-2 (4- fluoro-N, N-dimethyl isoquinoline-5-sulfonamide). These impurities are critical to the quality of both the drug substance and the final drug product.

Methods: The API crude samples were subjected to LC-mass spectrometry for the identification of unknown impurities and further based on the observed mass values, a strategic synthetic route was designed for the synthesis of unknown impurities. The synthetic routes for these impurities were developed to avoid column purification, achieving high yields and purity.

Results: The above synthesized impurities were subjected to spectral analysis like mass spectrometry, 1H NMR, and 13C NMR and confirmed the desired structure of the unknown impurities. So, as far as we know, the two impurities are new process impurities and have not been reported in the literature.

Conclusion: The two new process impurities have been prepared and used as impurities for the method development and quality evaluation of the Ripasudil drug substance. Given the regulatory significance of Ripasudil hydrochloride, our successful synthesis and characterization efforts have proven to be valuable. This research offers valuable insights into the generic pharmaceutical industry.

The author has identified an error in the department of the authors in the article titled "Highly Efficient Bimetallic Catalyst for the Synthesis of N-substituted Decahydroacridine-1,8-diones and Xanthene-1,8-diones: Evaluation of their Biological Activity" published in Current Organic Synthesis, 2024, 21(3) [1]. Details of the error and a correction are provided here. ORIGINAL 1. SANDEEP T. ATKORE Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, 431004, Maharashtra, India 2. PRANITA V. RAITHAK Department of Clinical Biochemistry, Dr. Baba Saheb Ambedkar Marathwada University, Aurangabad, 431004, Maharashtra, India CORRECTED 1. SANDEEP T. ATKORE Department of Biochemistry, Dr. Baba Saheb Ambedkar Marathwada University, Aurangabad, 431004, Maharashtra, India 2. PRANITA V. RAITHAK Department of Botany, Dr. Baba Saheb Ambedkar Marathwada University, Aurangabad, 431004, Maharashtra, India We regret the error and apologize to readers. The original article can be found online at: https://www.benthamscience.com/article/136681.

1,4-Dihydropyridines (1,4-DHPs) are highly versatile and bioactive compounds known for their pharmacological properties, including cardiovascular, anticancer, and antioxidant activities. Traditional synthesis methods often involve harsh conditions, such as high temperatures, toxic reagents, and lengthy reaction times, leading to poor yields and environmental concerns. Consequently, there has been a growing focus on developing more sustainable, efficient, and eco-friendly alternatives for their synthesis. Among these, the catalytic one-pot multicomponent reaction (MCR) method has emerged as a promising strategy, offering high efficiency. Catalysts play a crucial role in enhancing reaction efficiency and selectivity, with various systems-metal-based, organocatalysts, polymer-supported catalysts, and enzymatic catalysts-each offering unique advantages. Metal catalysts provide high reactivity and selectivity, organocatalysts are more environmentally benign, polymer-supported catalysts offer improved stability and sustainability, and enzymatic catalysts enable highly specific reactions under mild conditions. However, challenges such as catalyst cost, reusability, scalability, and substrate scope remain. This review examines catalytic strategies for 1,4-DHPs synthesis from 2016 to 2024, highlighting reaction conditions, substrates, and yields. The analysis aims to inspire further exploration of new catalytic methods, expanding the application of 1,4-DHPs in medicinal chemistry.