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Paper | Regular issue | Vol 87, No. 9, 2013, pp.1881-1887
Published online, 7th August, 2013
DOI: 10.3987/COM-13-12778
A CONVENIENT SYNTHESIS OF 2-MERCAPTO-OXAZOLES VIA β-KETOAZIDE AND ITS APPLICATION TO A KEY INTERMEDIATE OF PI3Kγ INHIBITORS

Yusuke Oka,* Tetsuya Yabuuchi, and Yoshinori Sekiguchi

*Medicinal Chemistry Laboratories, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-Cho, Kita-ku, Saitama-city, Saitama 331-9530, Japan

Abstract

A convenient synthesis of 2-mercapto-oxazoles via the reaction of β-ketoazide with triphenylphosphine (TPP) and carbon disulfide and its application to the synthesis of a key intermediate of phosphoinositide 3-kinase γ (PI3Kγ) inhibitors are described.