C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 477/20 (2006.01) C07D 463/02 (2006.01) C07D 463/22 (2006.01) C07D 477/08 (2006.01) C07D 499/04 (2006.01) C07D 499/21 (2006.01) C07D 499/68 (2006.01) C07D 501/02 (2006.01) C07D 501/22 (2006.01) C07D 501/34 (2006.01) C07D 501/36 (2006.01) C07D 501/38 (2006.01) C07D 519/06 (2006.01)
Patent
CA 2379650
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: (SEE ABOVE FORMULA) (wherein the ring A means the basic antibiotic; R10 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: (SEE FORMULA II-I) (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 R6; R1 represents hydrogen or methyl group; R2 and R5 are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R3 representsacarboxyl -protecting group; R4 representshydrogen, a lower alkyl group or an amino-protecting group; R6 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: (SEE ABOVE FORMULA) (wherein R7 and R8 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. 39
La présente invention concerne un nouveau procédé excellent sur le plan industriel permettant de préparer des sels d'addition d'antibiotiques de base à partir d'acides inorganiques (comme par exemple l'acide chlorhydrique), en soumettant un sel d'addition acide d'oxalique antibiotique (II) à un échange de sel avec un sel acide inorganique (III) d'un métal de terre alcalin, (où A représente un antibiotique de base; R<10> représente un groupe fonctionnel protégé s'utilisant en synthèse organique; Ak-E représente un métal de terre alcalin; et B représente un acide inorganique); des sels d'addition acides oxaliques dérivés de carbapenem représentés par la formule générale (II-I) et utilisés comme intermédiaires dans la préparation de chlorhydrates d'agents antimicrobiens; ainsi qu'un procédé de préparation de ceux-ci; (II-I) (où A représente un cycle de trois à sept chaînons comportant au moins un atome d'azote; R<1> représente hydrogène ou analogue; R<2> et R<5> représentent chacun hydrogène ou un groupe de protection; R<3> représente un groupe de protection; R<4> représente hydrogène ou analogue; et R<6> représente hydrogène ou analogue).
Chiba Hiroyuki
Ishizuka Hiroyuki
Kayano Akio
Komatsu Yuuki
Nakamura Taiju
Eisai Co. Ltd.
Eisai R&d Management Co. Ltd.
Smart & Biggar
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