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PROCESS FOR THE PREPARATION OF BIMOSIAMOSE
专利权人:
REVOTAR BIOPHARMACEUTICALS AG;레보타 바이오파마슈티컬스 아게
发明人:
KRANICH REMO,크라니히 레모,BOCK DANIEL,보크 다니엘
申请号:
KR1020127029201
公开号:
KR1020130056238A
申请日:
2011.05.04
申请国别(地区):
KR
年份:
2013
代理人:
摘要:
A process for the preparation of 1,6-Bis-[3-(3-carboxymethylphenyl)-4-(2-a-D-mannopyranosyloxy)-phenyl] hexane (I) which comprises the steps of converting the compound (2'-Methoxy-biphenyl-3-yl)-acetic acid (A) into the (2'-Methoxy-biphenyl-3-yl)-acetic acid ethyl ester, which is reacted with adipoyl chloride to 1,4-Bis-[3-(3-carboethoxymethylphenyl)-4-methoxybenzoyl]-butane (B) which is catalytically reduced to 1,6-Bis-[3-(3-carboethoxy-methylphenyl)-4-methoxy- phenyl] -hexane (C), which is reacted with boron tribromide in a solvent to 1,6-Bis-[3-(3- carboethoxy-methylphenyl)-4-hydroxyphenyl]-hexane (D), which is reacted with a mannopyranosyl derivative to obtain 1,6-Bis-[3-(3-carboethoxy-methylphenyl)-4-(tetra-0- pivaloyl-a-D-mannopyranosyloxy)-phenyl]-hexane (E), which is reacted to form 1,6-Bis- [3-(3-carboxymethyl-phenyl)-4-(2-a-D-mannopyranosyloxy)-phenyl] hexane, which is re- crystallized, leads to the product (I) with high purity.화합물 (2'-메톡시-바이페닐-3-일)-아세트산 (A) 를 (2'-메톡시-바이페닐-3-일)-아세트산 에틸 에스테르로 전환시키며, 이를 아디포일 클로라이드와 반응시켜 1,4-비스-[3-(3-카르보에톡시메틸페닐)-4-메톡시벤조일]-부탄 (B) 를 수득하며, 이를 촉매 환원시켜 1,6-비스-[3-(3-카르보에톡시-메틸페닐)-4-메톡시-페닐]-헥산 (C) 를 수득하며, 이를 용매 중에 보론 트리브로마이드와 반응시켜 1,6-비스-[3-(3-카르보에톡시-메틸페닐)-4-히드록시페닐]-헥산 (D) 를 수득하며, 이를 만노피라노실 유도체와 반응시켜 1,6-비스-[3-(3-카르보에톡시-메틸페닐)-4-(테트라-O-피발로일-α-D-만노피라노실옥시)-페닐]-헥산 (E) 를 수득하며, 이를 반응시켜 1,6-비스-[3-(3-카르복시메틸-페닐)-4-(2-α-D-만노피라노실옥시)-페닐] 헥산을 형성하며, 이를 재결정화하여 고순도의 생성물 (I) 을 유도하는 단계를 포함하는, 1,6-비스-[3-(3-카르복시메틸페닐)-4-(2-α-D-만노피라노실옥시)-페닐] 헥산 (I) 의 제조 방법.
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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