One-Step Synthesis of
Heteroaromatic-Fused Pyrrolidines via
Cyclopropane Ring-Opening Reaction: 
Application to the PKCβ Inhibitor
JTT-010

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

doi:10.1021/ol071336h.s003

One-Step Synthesis of Heteroaromatic-Fused Pyrrolidines via Cyclopropane Ring-Opening Reaction: Application to the PKCβ Inhibitor JTT-010

journal contribution

posted on 2007-08-16, 00:00 authored by Masahiro Tanaka, Minoru Ubukata, Takafumi Matsuo, Katsutaka Yasue, Katsuya Matsumoto, Yasuyuki Kajimoto, Takashi Ogo, Takashi Inaba

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-β inhibitor JTT-010, which possesses a dihydropyrrolo[1,2-a]indole core.

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Pyrrolidine Application Cyclopropane protein synthesis dihydropyrrolo indole core pyrrolidine kinase PKC heteroaromatic Synthesi JTT cyclopropane Inhibitor inhibitor

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One-Step Synthesis of Heteroaromatic-Fused Pyrrolidines via Cyclopropane Ring-Opening Reaction: Application to the PKCβ Inhibitor JTT-010

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