5-Substituted-1H-tetrazoles as carboxylic acid isosteres: medicinal chemistry and synthetic methods
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1Medicinal Chemistry Department, Albany Molecular Research, Inc., PO Box 15098, Albany, NY 12212-5098, USA. rjasonh@albmolecular.com
Abstract:
5-Substituted-1H-tetrazoles (RCN4H) are often used as metabolism-resistant isosteric replacements for carboxylic acids (RCO2H) in SAR-driven medicinal chemistry analogue syntheses. This review provides a brief summary of the medicinal chemistry of tetrazolic acids and highlights some examples of tetrazole-containing drug substances in the current literature. A survey of representative literature procedures for the preparation of 5-substituted-1H-tetrazoles, focusing on preparations from aryl and alkyl nitriles, is presented in sections by generalized synthetic methods.
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