AI Article Synopsis
- 5-Substituted-1H-tetrazoles are used in medicinal chemistry as stable alternatives to carboxylic acids in drug development.
- The review summarizes their medicinal chemistry and showcases examples of drugs containing tetrazole from recent literature.
- It also discusses common synthetic methods for creating 5-substituted-1H-tetrazoles, particularly from various nitriles.
Article 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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| http://dx.doi.org/10.1016/s0968-0896(02)00239-0 | DOI Listing |
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