Traceless solid-phase synthesis of 1,2,4-triazoles using a novel amine resin |
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Authors: | Larsen S D DiPaolo B A |
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Institution: | Combinatorial and Medicinal Chemistry Research, Pharmacia Corporation, Kalamazoo, Michigan 49007, USA. scott.d.larsen@pharmacia.com |
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Abstract: | reaction: see text]. A solid-phase route to 5-aryl-3-arylthiomethyl-1,2,4-triazoles has been developed that permits the incorporation of two elements of diversity. The heterocycle was constructed upon a novel 4-benzyloxy-2-methoxybenzylamine (BOMBA) resin, from which traceless cleavage could be effected with dilute TFA. A library of 96 triazoles was produced with an average yield of 26% (84% yield per step) and an average purity of 80%. In a direct comparison, the new BOMBA resin proved to be markedly superior to Rink Amide resin for this application. |
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