Practical asymmetric synthesis of a selective endothelin a receptor (ETA) antagonist

…, R Volante, PJ Reider, Y Kato, S Okada, T Nemoto…

文献索引：Song, Zhiguo J.; Zhao, Matthew; Frey, Lisa; Li, Jing; Tan, Lushi; Chen, Cheng Y.; Tschaen, David M.; Tillyer, Richard; Grabowski, Edward J. J.; Volante, Ralph; Reider, Paul J.; Kato, Yoshiaki; Okada, Shigemitsu; Nemoto, Takayuki; Sato, Hiroki; Akao, Atsushi; Mase, Toshiaki Organic Letters, 2001 , vol. 3, # 21 p. 3357 - 3360

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被引用次数: 32

摘要

A practical, chromotography-free asymmetric synthesis was developed for the large scale preparation of an endothelin receptor antagonist 2. This synthesis includes a new efficient process for the preparation of 6-bromo-2, 3-dihydrobenzofuran, a stereoselective conjugate addition of an aryllithium followed by stereospecific addition of the Grignard reagent of the top aryl bromide, and an aminophosphate-mediated sterospecific intramolecular enolate ...