Synthesis method of 2-substituted benzoxazole, 2-substituted benzothiazole and derivatives thereof

Abstract

The invention provides a synthesis method of 2-substituted benzoxazole, 2-substituted benzothiazole and derivatives thereof. In the method, through ortho-aminophenol / 2-aminothiophenol cyclization catalyzed by imidazole hydrochloride, synthesis of functionalized 2-substituted benzoxazole and 2-substituted benzothiazole is realized; the method is simple, economical and high in practicality. No othercatalysts or additives are used, the synthesis method ensures good functional group tolerance and excellent yield and purity, the reaction time is short, no harsh reaction conditions are needed, andthe method is suitable for industrial production.

Description

Technical field

[0001] The present invention relates to 2-substituted benzoxazole and 2-substituted benzothiazole and their derivatives, in particular to the synthesis of a 2-substituted benzoxazole and 2-substituted benzothiazole and their derivatives method. Background technique

[0002] 2-substituted benzoxazole compounds are a class of benzoheterocyclic compounds containing one nitrogen atom and one oxygen atom, 2-substituted benzothiazole compounds are a class of benzene containing one nitrogen atom and one sulfur atom Heterocyclic compounds, these compounds are the structural unit of many drugs (Kaplancikli ZA, Gülhan Turan Zitouni, Revial ​​G, Guven K, Archives of Pharmacal Research. 2004:27:1081; Viirre RD, Evindar G, Batey RA. Journal of Organic Chemistry. 2008:39:3452.). The traditional synthesis method of benzoxazoles and benzothiazoles is mainly through the condensation of o-aminophenol / thiophenol with aldehydes, acids, amides, acid chlorides, nitriles, esters or th...

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