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Paper | Regular issue | Vol 75, No. 7, 2008, pp.1659-1671
Published online, 18th March, 2008
DOI: 10.3987/COM-08-11341
Enantioselective Synthesis of Piperidine Diamine Derivatives as Novel fXa Inhibitors

Akiyoshi Mochizuki,* Hiroyuki Naito, Yumi Nakamoto, Kouichi Uoto, and Toshiharu Ohta

*Medicinal Chemistry Research Laboratory I, Daiichi Sankyo Co., Ltd, 1-2-58, Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan


Previously, we reported that racemic cis-piperidine diamine derivatives (±)-1 showed high anti-fXa, anticoagulation activity and oral activities. To confirm the active enantiomer, (3R,4S)-piperidine diamine derivatives (-)-1A and (-)-1B were synthesized enantioselectively from Boc-D-serine. These synthetic routes and intermediates could be utilized for the optimization of these derivatives. From the activities of (-)-1A and (-)-1B, (3R,4S)-isomer was confirmed to be the active enantiomer.