Total synthesis of (+)-benzastatin E via diastereoselective Grignard addition to 2-acylindoline |
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| Authors: | Toda Narihiro Ori Mayuko Takami Kazuko Tago Keiko Kogen Hiroshi |
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| Institution: | Exploratory Chemistry Research Laboratories, Sankyo Co, Ltd, 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. |
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| Abstract: | reaction: see text] A stereoselective total synthesis of (+)-benzastatin E (1) is described. The synthesis involves a diastereoselective Grignard addition to 2-acylindoline 2, which is derived from commercially available (S)-2-indolinecarboxylic acid (3). The unknown absolute configuration of (+)-1 is determined as (9S,10R). |
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