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    PROCESS FOR THE PREPARATION OF BASIC ANTIBIOTIC-INORGANIC ACID ADDITION SALTS AND INTERMEDIATE OXALATES
    1.
    发明公开
    PROCESS FOR THE PREPARATION OF BASIC ANTIBIOTIC-INORGANIC ACID ADDITION SALTS AND INTERMEDIATE OXALATES 有权
    用于生产抗生素与无机酸和碱加成盐，草酸盐中间体

    公开(公告)号：EP1201665A1

    公开(公告)日：2002-05-02

    申请号：EP00948257.1

    申请日：2000-07-27

    申请人： Eisai Co., Ltd.

    发明人： KAYANO, Akio ,  CHIBA, Hiroyuki ,  NAKAMURA, Taiju ,  SAKURAI, Shin ,  ISHIZUKA, Hiroyuki ,  SAITO, Hiroyuki ,  KOMATSU, Yuuki ,  SASHO, Manabu ,  SATO, Nobuaki ,  NEGI, Shigeto

    IPC分类号： C07D477/02 ,  C07D477/20 ,  C07D463/00 ,  C07D499/00 ,  C07D501/00

    CPC分类号： C07D477/20 ,  C07D477/02 ,  C07D477/08 ,  Y02P20/55

    摘要： The present invention provides:

    an industrially-excellent and novel process for producing a basic antibiotic·inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic·oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid:
    (wherein the ring A means the basic antibiotic; R 10 means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively);
    a novel oxalate useful as a production intermediate for producing an antibiotic·hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula:
    (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R 6 ; R 1 represents hydrogen or methyl group; R 2 and R 5 are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R 3 represents a carboxyl-protecting group; R 4 represents hydrogen, a lower alkyl group or an amino-protecting group; R 6 represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula:
    (wherein R 7 and R 8 are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and
    a process for producing its.

    摘要翻译： 本发明提供：在工业上优和新方法用于生产基本antibiotic.inorganic酸的盐，例如，优良的生产过程用于制备盐酸盐在工业上，所做的是，一个生产过程，它包括使一个基本antibiotic.oxalate （II）盐交换与碱土金属盐（III）的无机酸的：（worin环的装置的基本抗生素; R <10>表示在有机合成中使用的保护的官能基团; AK- E表示碱土金属;且B是指无机酸，分别地）; 一种新颖的草酸作为生产用于在antibiotic.hydrochloride生产工业上，做了中间有用是草酸盐（II-I）由下式表示的碳代青霉烯化合物：（ worin环A darstellt 3-至7- 具有元环的至少一个氮原子，且环A可与其它除R <6> R上substituiertem <1> darstellt氢或甲基; R <2>和R <5>是相同的或不同 形成，且分别darstellt氢或羟基保护基; R <3>表示羧基保护基; R <4> darstellt氢，低级烷基或氨基保护基的; R <6> darstellt（1 ）氢，（2）任选被保护的羟基，氨基甲酰基，亚胺甲基，acetoimidoyl或可被由下式表示的取代基所substituiertem的低级烷基：（worin - [R <7>和R <8>是 相同或彼此和各darstellt氢，低级烷基或氨基保护基），或者（3个不同的 ）氨基保护基或亚氨基保护的基团; 且m是0或1）; 和用于生产其的过程。