Review
doi: 10.1016/s0968-0896(02)00239-0.
5-Substituted-1H-tetrazoles as carboxylic acid isosteres: medicinal chemistry and synthetic methods
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- PMID: 12213451
- DOI: 10.1016/s0968-0896(02)00239-0
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Review
5-Substituted-1H-tetrazoles as carboxylic acid isosteres: medicinal chemistry and synthetic methods
Bioorg Med Chem.
2002 Nov.
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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