中国医药科学
中國醫藥科學
중국의약과학
CHINA MEDICINE AND PHARMACY
2014年
12期
41-43
,共3页
施猛%刘恩桂%夏春森%张俊珺
施猛%劉恩桂%夏春森%張俊珺
시맹%류은계%하춘삼%장준군
阿加曲班%抗血栓%合成
阿加麯班%抗血栓%閤成
아가곡반%항혈전%합성
Argatroban%Antithrombotic%Synthesis
通过硝基-L-精氨酸与3-甲基喹啉-8-磺酰氯缩合,再与(2R,4R)-4-甲基-2-哌啶甲酸乙酯缩合,经过酯水解,氢化,精制共五步反应,高收率地合成了抗血栓药物阿加曲班,该合成方法操作简单,工艺稳定,产品纯度较好,适合工业化生产。
通過硝基-L-精氨痠與3-甲基喹啉-8-磺酰氯縮閤,再與(2R,4R)-4-甲基-2-哌啶甲痠乙酯縮閤,經過酯水解,氫化,精製共五步反應,高收率地閤成瞭抗血栓藥物阿加麯班,該閤成方法操作簡單,工藝穩定,產品純度較好,適閤工業化生產。
통과초기-L-정안산여3-갑기규람-8-광선록축합,재여(2R,4R)-4-갑기-2-고정갑산을지축합,경과지수해,경화,정제공오보반응,고수솔지합성료항혈전약물아가곡반,해합성방법조작간단,공예은정,산품순도교호,괄합공업화생산。
Argatroban,an antithrombotic drug,was synthesized in high yield through a five-step route including condensation reaction of N-nitro-L-arginine and quinolinesulfonyl chloride,condensing with piperidine carboxylate,hydrolysis of esters, hydrogenation and purification.This method was considered to obtain highly pure products by simple operation and stable technique,which was suitable for industrialization.