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Paper | Regular issue | Vol 83, No. 7, 2011, pp.1587-1602
Published online, 19th May, 2011
DOI: 10.3987/COM-11-12224
Efficient Synthesis of 5-Amino-6-dialkylamino-4-hydroxypentanamide Derivatives for Renin Inhibitors

Yuji Nakamura,* Yasuyuki Ogawa, Chie Suzuki, Teppei Fujimoto, Shojiro Miyazaki, Kazuhiko Tamaki, Takahide Nishi, and Hiroshi Suemune

*Lead Discovery and Optimization Research Laboratories, Daiichi Sankyo Co., Ltd, 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan


We report an efficient synthetic method for 5-amino-6-dialkylamino-4-hydroxypentanamide derivatives using Shi Asymmetric Epoxidation and the ring opening of N-(2-nitrobenzenesulfonyl)aziridine with hindered secondary amine as key steps.