Enantioselective synthesis of piperidine diamine derivatives as novel fXa inhibitors.

[摘要]：Previously, it was reported that racemic cis-piperidine diamine derivs. (?-I (R = COMe, COCH2OMe) showed high anti-fXa, anticoagulation activity and oral activities. To confirm the active enantiomer, (3R,4S)-piperidine diamine derivs. (-)-I were synthesized enantioselectively from Boc-D-serine. These synthetic routes and intermediates could be utilized for the optimization of these derivs. From a comparison of the activities of (-)-I to racemic samples, the (3R,4S)-isomer was confirmed to be the active enantiomer.

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