发明授权
- 专利标题: PROCESS FOR THE PREPARATION OF BASIC ANTIBIOTIC-INORGANIC ACID ADDITION SALTS AND INTERMEDIATE OXALATES
- 专利标题(中): 用于生产抗生素与无机酸和碱加成盐,草酸盐中间体
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申请号: EP00948257.1申请日: 2000-07-27
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公开(公告)号: EP1201665B1公开(公告)日: 2004-09-29
- 发明人: KAYANO, Akio , CHIBA, Hiroyuki , NAKAMURA, Taiju , SAKURAI, Shin , ISHIZUKA, Hiroyuki , SAITO, Hiroyuki , KOMATSU, Yuuki , SASHO, Manabu , SATO, Nobuaki , NEGI, Shigeto
- 申请人: Eisai Co., Ltd.
- 申请人地址: 6-10, Koishikawa 4-chome, Bunkyo-ku Tokyo 112-8088 JP
- 专利权人: Eisai Co., Ltd.
- 当前专利权人: Eisai Co., Ltd.
- 当前专利权人地址: 6-10, Koishikawa 4-chome, Bunkyo-ku Tokyo 112-8088 JP
- 代理机构: HOFFMANN - EITLE
- 优先权: JP21680699 19990730; JP21680799 19990730
- 国际公布: WO2001009135 20010208
- 主分类号: C07D477/02
- IPC分类号: C07D477/02 ; C07D477/20 ; C07D463/00 ; C07D499/00 ; C07D501/00
摘要:
An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an inorganic acid salt (III) of an alkaline earth metal, wherein A is a basic antibiotic; R10 is a protected functional group to be used in organic synthesis; Ak-E is an alkaline earth metal; and B is an inorganic acid; carbapenem derivative-oxalic acid addition salts represented by general formula (II-I) and being useful as intermediates for the preparation of hydrochlorides of antimicrobial agents; and a process for preparing the same, (II-I) wherein A is a three- to seven-membered ring having at least one nitrogen atom; R1 is hydrogen or the like; R?2 and R5¿ are each hydrogen or a protecting group; R3 is a protecting group; R4 is hydrogen or the like; and R6 is hydrogen or the like.
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