An Efficient Green Multi-Component Reaction Strategy for the Synthesis of Highly Functionalised Pyridines and Evaluation of Their Antibacterial Activities
An efficient green multi-component reaction (MCR) method has been developed for the synthesis of 2-amino-4-aryl/heteroaryl-6-(pyridin-2-ylthio)pyridine-3,5-dicarbonitrile(s) via a 3-component reaction of aryl aldehyde(s), malononitrile and 2-mercaptopyridine in the presence of K2CO3 under solvent fr...
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Published in: | Chemical & pharmaceutical bulletin Vol. 61; no. 11; pp. 1114 - 1120 |
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Main Authors: | , , , , , |
Format: | Journal Article |
Language: | English |
Published: |
Japan
The Pharmaceutical Society of Japan
01-11-2013
Japan Science and Technology Agency |
Subjects: | |
Online Access: | Get full text |
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Summary: | An efficient green multi-component reaction (MCR) method has been developed for the synthesis of 2-amino-4-aryl/heteroaryl-6-(pyridin-2-ylthio)pyridine-3,5-dicarbonitrile(s) via a 3-component reaction of aryl aldehyde(s), malononitrile and 2-mercaptopyridine in the presence of K2CO3 under solvent free reaction conditions (SFRC) using grinding technique at room temperature in a single step. The advantages of the present protocol is operationally simple, environmentally benign, solvent-free reaction conditions (SFRC), simple work up, excellent isolated yields of desired products and viable method for large scale applications in pharmaceutical industry. Interestingly, the synthesized compounds showed moderate to excellent antibacterial activities against Gram-positive and Gram-negative bacterial strains. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0009-2363 1347-5223 |
DOI: | 10.1248/cpb.c13-00412 |