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    • 3. 发明公开
    • (Z) 이성질체가 풍부한 7-PACA의 제조방법
    • 制备具有全长(Z)异构体的7-PACA的方法
    • KR1020130108939A
    • 2013-10-07
    • KR1020120030796
    • 2012-03-26
    • 투윈파마 주식회사
    • 서락석오창현
    • C07D501/14C07D501/22C07D501/10B01J31/04
    • Y02P20/55C07D501/04B01J31/04C07D501/22
    • PURPOSE: A method for preparing 3-[(Z/E)-propen-1-yl]-7-amino-cephalosporin acid (7-PACA) containing rich (Z) isomers is provided to obtain 7-PACA with proper Z/E ratio and high yield. CONSTITUTION: A method for preparing 7-PACA of chemical formula I comprises the steps of: making a compound of chemical formula III react with cresol at 10-30°C for 5-20 hours according to reaction formula 3 and deprotecting a carboxyl protection group; and adding enzyme to a compound of chemical formula IV according to reaction formula 4 and deprotecting an amino protection group. Cresol is used in a quantity of 15-50 equivalents with respect to 1 equivalent of the compound of chemical formula III. [Reference numerals] (AA) Enzyme
    • 目的:提供一种制备含有富(Z)异构体的3 - [(Z / E) - 丙烯-1-基] -7-氨基 - 头孢菌素酸(7-PACA)的方法,以获得具有适当Z / E比和高产量。 构成:制备化学式I的7-PACA的方法包括以下步骤:使化学式III的化合物根据反应式3在10-30℃与甲酚反应5-20小时,并使羧基保护基团脱保护 ; 并根据反应式4向化学式IV的化合物中加入酶,并使氨基保护基脱保护。 相对于1当量的化学式III的化合物,甲酚的用量为15-50当量。 (标号)(AA)酶