One-step synthesis of heteroaromatic-fused pyrrolidines via cyclopropane ring-opening reaction: application to the PKCbeta inhibitor JTT-010 |
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| Authors: | Tanaka Masahiro Ubukata Minoru Matsuo Takafumi Yasue Katsutaka Matsumoto Katsuya Kajimoto Yasuyuki Ogo Takashi Inaba Takashi |
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| Institution: | Central Pharmaceutical Research Institute, Japan Tobacco Inc., Takatsuki Osaka 569-1125, Japan. |
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| 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 dihydropyrrolo1,2-a]indole core. |
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