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CN101643757B 光学纯N-取代-吗啉-3-酮-2-乙酸的制备方法 失效 - 权利终止

  • Patent Title: 光学纯N-取代-吗啉-3-酮-2-乙酸的制备方法
  • Patent Title (English): Preparation method of optically pure N-substitute-morpholine-3-ketone-2-acetic acid
  • Application No.: CN200910102396.X
    Application Date: 2009-09-07
  • Publication No.: CN101643757B
    Publication Date: 2011-10-19
  • Inventor: 林贤福 , 叶海朋 , 吴起
  • Applicant: 浙江大学
  • Applicant Address: 浙江省杭州市西湖区浙大路38号
  • Assignee: 浙江大学
  • Current Assignee: 浙江大学
  • Current Assignee Address: 浙江省杭州市西湖区浙大路38号
  • Agency: 杭州天勤知识产权代理有限公司
  • Agent 胡红娟
  • Main IPC: C12P17/14
  • IPC: C12P17/14
光学纯N-取代-吗啉-3-酮-2-乙酸的制备方法
Abstract:
本发明公开了一种光学纯N-取代-吗啉-3-酮-2-乙酸的制备方法，包括如下步骤：以脂肪酶为催化剂，在水/有机溶剂体系中，水解拆分外消旋的式(I)所示的N-取代-吗啉-3-酮-2-乙酸酯底物，经后处理制得式(II)所示的(R)-N-取代-吗啉-3-酮-2-乙酸或(S)-N-取代-吗啉-3-酮-2-乙酸；本发明采用的酶促方法通过改变反应条件，可以调控水解产物的选择性，实现两种构型产物的可控制备；本发明方法与其它化学法合成相比产物光学纯度高、副反应少、底物产物易分离、反应条件温和，对环境友好。
Abstract(English):

The invention discloses a preparation method of optically pure N-substitute-morpholine-3-ketone-2-acetic acid, including the following steps: dl-N-substitute-morpholine-3-ketone-2-acetic ester substrate shown in formula (I) is hydrolyzed by resolution in water/organic solvent system by taking lipase as catalyst; and (R)-N-substitute-morpholine-3-ketone-2-acetic acid or (S)-N-substitute-morpholine-3-ketone-2-acetic acid shown in formula (II) is prepared through post processing. Enzymatic method adopted by the invention can control selectivity of hydrolysate by changing reaction condition, so as to realize controllable preparation of products in two configurations. Compared with other chemical synthesis methods, the method of the invention has the advantages that optical purity of product is high, side reaction is less, substrate product is easy to be separated, reaction condition is mild, and the method is environmentally friendly.

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