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N-(丁基磺酰基)-L-酪氨酸甲酯 N-Butanesulfonyl-L-Tyrosine Methyl Ester 142374-01-4

N-(丁基磺酰基)-L-酪氨酸甲酯置于lithium Hydroxide,盐酸体系中,用 水 用作溶剂,化学反应 3.0H,以99%的收率获得l-N-丁基磺酰基-P-羟基苯基丙氨酸
参考文献:一种盐酸替罗非班中间体iii的合成方法
标题:一种盐酸替罗非班中间体iii的合成方法
摘要:本发明属于医药合成领域,具体涉及一种盐酸替罗非班中间体iii的合成方法.采用硼氢化钠还原体系作用下,还原中间体ⅰ得到中间体ii,中间体ii在lewis酸氯化物存在下和socl2发生氯化反应,得中间体iii,再与n‑丁磺酰基‑l‑酪氨酸在碘化试剂存在下醚化后氢化,成盐制得盐酸替罗非班.本发明反应条件温和,工艺操作简单,中间步骤无需过柱纯化,提高了反应收率,产品纯度高,符合药典标准原料药用于注射剂使用要求,显著提高了临床用药的安全性,适于工业化生产.

专利信息

专利号:RU-2114105-C1
优先权日:1992-02-28
标题 :N-sulfonyltyrosine 4-(4-pyridyl)-butyl ester or its pharmaceutically acceptable salts and a method of synthesis of n-sulfonyltyrosine 4-(4-pyridyl)-butyl ester or its pharmaceutically acceptable salts

专利号:RU-2097377-C1
优先权日:1992-02-28
标题 :Method of synthesis of tyrosine derivatives

专利号:US-5206373-A
优先权日:1992-02-28
标题 :Process for preparing fibrinogen receptor antagonists
发明人：CHUNG JOHN Y L; HUGHES DAVID L; ZHAO DALIAN
权利人:MERCK & CO INC
摘要:The invention is a highly efficient synthesis for making compounds of the formula: ##STR1## wherein: R 1 is a six member saturated or unsaturated heterocyclic ring containing one or two heterocyclic atoms wherein the heteroatoms are N; or NR 6 , wherein R 6 is H or C 1-10 alkyl; n m is an integer from two to six; and n R 4 is aryl, C 1-10 alkyl, or C 4-10 aralkyl.