A new and practical boronic acid catalyzed intramolecular cyclodehydration of ureas for the synthesis of LFA-1 antagonists

Rogelio P. Frutos,Thomas Tampone,Jason A. Mulder,Yibo Xu,Diana Reeves,Xiao-Jun Wang,Li Zhang,Dhileepkumar Krishnamurthy,Chris H. Senanayake

Tetrahedron Letters（2011）

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摘要

A streamlined and practical approach to 1H-imidazo[1,2-α]imidazol-2-one LFA-1 antagonist (1) that features as the key step a novel intramolecular boronic acid catalyzed cyclocondensation of a urea and an amide is reported.

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关键词

practical boronic acid,intramolecular cyclodehydration,ureas,synthesis

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