| 摘要 |
The present invention relates to a process for the enantioselective enzymatic aminolysis of racemic 2-[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]acetate ((R/S)-I) by methyl Nalpha-Boc-L-alpha,beta-diaminoproprionate .p-toluenesulfonic acid. More specifically, this invention pertains to a process for the enantioselective enzymatic aminolysis of racemic isobutyl 2-[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]-acetate by methyl Nalpha-Boc-L-alpha,beta-diaminoproprionate .p-toluene sulfonic acid to produce (R)-methyl-3-[[[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]acetyl]amino]-N-(butoxycarbonyl)-L-alanine, an intermediate in the preparation of roxifiban, an isoxazoline-based platelet glycoprotein IIb/IIIa antagonist which has activity as an antithrombotic agent.
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