发明公开
- 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申请日: 2000-07-27
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公开(公告)号: EP1201665A4公开(公告)日: 2002-10-23
- 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
- 专利权人: EISAI CO LTD
- 当前专利权人: EISAI CO LTD
- 优先权: JP21680699 1999-07-30; JP21680799 1999-07-30
- 主分类号: C07D477/02
- IPC分类号: C07D477/02 ; C07D477/08 ; C07D477/20 ; C07D499/68 ; C07D501/22 ; C07D501/36 ; C07D501/46 ; 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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