会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 7. 发明申请
    • PROCESS FOR THE PREPARATION OF 3-ARYL-2-HYDROXY PROPANOIC ACID DERIVATIVES
    • 制备3-芳基-2-羟基丙酸衍生物的方法
    • WO02024625A3
    • 2002-06-27
    • PCT/IB2001/001699
    • 2001-09-17
    • C07C67/00C07C67/10C07C67/11C07C69/734
    • C07C67/10C07C67/00C07C67/11C07C69/734
    • The present invention relates to an improved process for the preparation of 3-aryl-2-hydroxy propanoic acid derivatives of formula (1) where R represents hydrogen atom or (C1-C6)alkyl group and R represents (C1-C6)alkyl group which comprises: (i) selectively benzylating L-tyrosine to yield compound of formula (15); (ii). diazotising the compound of formula (15) to produce compound of formula (8); (iii) simultaneous etherification and esterification of compound of formula (8) to obtain crude compound of formula (9) with ee>90 %; (iv) hydrolysing the crude compound of formula (9) to produce compound of formula (9a) acid; (v) treating the compound of formula (9a) with chiral base to produce pure salt of formula (16); (vi) converting the compound of formula (16) to pure compound of formula (9a); (vii) esterifying pure compound of formula (9a) to produce pure compound of formula (9); (viii) debenzylating the compound of formula (9) to yield pure compound of formula (1).
    • 本发明涉及制备式(1)的3-芳基-2-羟基丙酸衍生物的改进方法,其中R 1表示氢原子或(C1-C6)烷基,R 2表示( C1-C6)烷基,其包括:(i)选择性苄化L-酪氨酸以产生式(15)化合物; (ⅱ)。 重氮化式(15)化合物以制备式(8)化合物; (iii)式(8)化合物的同时醚化和酯化得到ee> 90%的粗制式(9)化合物; (iv)水解式(9)的粗制化合物以产生式(9a)酸的化合物; (v)用手性碱处理式(9a)化合物以制备式(16)的纯盐; (vi)将式(16)化合物转化成纯的式(9a)化合物; (vii)将纯的式(9a)化合物酯化以制备纯的式(9)化合物; (viii)使式(9)化合物脱苄酯化,得到纯的式(1)化合物。