One-step synthesis of heteroaromatic-fused pyrrolidines via cyclopropane ring-opening reaction: application to the PKCbeta inhibitor JTT-010.

作者信息

Tanaka Masahiro, Ubukata Minoru, Matsuo Takafumi, Yasue Katsutaka, Matsumoto Katsuya, Kajimoto Yasuyuki, Ogo Takashi, Inaba Takashi

机构信息

Central Pharmaceutical Research Institute, Japan Tobacco Inc., Takatsuki Osaka 569-1125, Japan.

出版信息

Org Lett. 2007 Aug 16;9(17):3331-4. doi: 10.1021/ol071336h. Epub 2007 Jul 26.

DOI:10.1021/ol071336h

PMID:17655251

Abstract

A ring-opening reaction of cyclopropanes with five-membered heteroaromatics having a leaving group at C(2) was found to provide heteroaromatic-fused pyrrolidines in one step. This reaction was successfully applied to the synthesis of the protein kinase C-beta inhibitor JTT-010, which possesses a dihydropyrrolo[1,2-a]indole core.

摘要