Chemo-enzymatic synthesis of N-(4-(Amino (imino) -methyl) benzyl) -2-((R)-4-benzyl-3-oxo-morpholin-2-yl)-acetamide(酶促-化学法合成(R)-N-苄基吗啉-3-酮-2-乙酰（4-脒基）苄胺)

Chemo-enzymatic synthesis of N-(4-(Amino (imino) -methyl) benzyl) -2-((R)-4-benzyl-3-oxo-morpholin-2-yl)-acetamide(酶促-化学法合成(R)-N-苄基吗啉-3-酮-2-乙酰（4-脒基）苄胺)

报道了一种酶促-化学法合成光学纯吗啉酮凝血酶抑制剂的新途径.以马来酸酐和氨基醇为起始原料，一锅法合成N-苄基吗啉-3-酮-2-乙酸甲酯；再用脂肪酶CAL-B在甲基叔丁基醚/水（体积分数=1/9）混合溶剂中将其选择性水解，制备光学纯(R)-N-苄基吗啉-3-酮-2-乙酸；经过酰胺化、还原/胺解，得到(R)-N-苄基吗啉-3-酮-2-乙酰（4-脒基）苄胺；所得化合物结构经IR，1H NMR，13C NMR表征确证.文中还讨论了酶源、溶剂、含水量、反应时间等因素对水解拆分的影响....

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Bibliographic Details
Main Authors: YEHai-peng(叶海朋), QIANXue-qi(钱学启), LIUBo-kai(刘博凯), WUQi(吴起), LINXian-fu(林贤福)
Format: Article
Language:zho
Published: Zhejiang University Press 2011-01-01
Series:Zhejiang Daxue xuebao. Lixue ban
Subjects:
酶促-化学法合成
n-苄基吗啉-3-酮
脂肪酶
凝血酶抑制剂
Online Access:https://doi.org/10.3785/j.issn.1008-9497.2011.01.016

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