Title:
PROCESS FOR THE PREPARATION OF 3-HALOGENOCEPHEM DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/1997/017353
Kind Code:
A1
Abstract:
A process for the preparation of 3-halogenocephem derivatives of general formula (2), characterized by reacting an allenyl-'beta'-lactam of general formula (1) with a halogenating agent in the presence of a cuprous or cupric salt: [wherein R1 is hydrogen, amino, or protected amino; R2 is hydrogen, halogeno, lower alkoxy, lower acyl, lower alkyl, lower alkyl having at least one group selected between hydroxyl and protected hydroxyl groups as a substituent, hydroxyl, or protected hydroxyl; R3 is hydrogen or a carboxyl-protecting group; R4 is a residue of an optionally substituted aromatic or nitrogeneous heteroaromatic compound; and n is an integer of 0 to 2] [wherein R1, R2 and R3 are each as defined above; and X is halogeno].
Inventors:
SASAOKA MICHIO (JP)
TORII SHIGERU (JP)
TANAKA HIDEO (JP)
KIKUCHI RYO (JP)
KAMEYAMA YUTAKA (JP)
SORAJO KOUICHI (JP)
TORII SHIGERU (JP)
TANAKA HIDEO (JP)
KIKUCHI RYO (JP)
KAMEYAMA YUTAKA (JP)
SORAJO KOUICHI (JP)
Application Number:
PCT/JP1996/003298
Publication Date:
May 15, 1997
Filing Date:
November 08, 1996
Export Citation:
Assignee:
OTSUKA KAGAKU KK (JP)
SASAOKA MICHIO (JP)
TORII SHIGERU (JP)
TANAKA HIDEO (JP)
KIKUCHI RYO (JP)
KAMEYAMA YUTAKA (JP)
SORAJO KOUICHI (JP)
SASAOKA MICHIO (JP)
TORII SHIGERU (JP)
TANAKA HIDEO (JP)
KIKUCHI RYO (JP)
KAMEYAMA YUTAKA (JP)
SORAJO KOUICHI (JP)
International Classes:
A61K31/545; A61K31/546; A61P31/04; B01J27/055; B01J27/122; B01J31/20; C07B61/00; C07D501/00; C07D501/08; C07D501/18; C07D501/59; (IPC1-7): C07D501/08; C07D501/18
Foreign References:
| JPH08245575A | 1996-09-24 | |||
| JPH04282387A | 1992-10-07 |
Other References:
BULL. CHEM. SOC. JPN., 1996, Vol. 69, No. 5, H. TANAKA, R. KIKUCHI, S. TORII, "Synthesis os 3-Chloro-3-cephem-4-carboxylate by Addition/Cyclization of Allenecarboxylate. Copper (II)-Promoted Aerobic Oxidation of Arenesulfinic Acids", pages 1391-1396.
SYNLETT., 1991, No. 12, H. TANAKA, Y. KAMEYAMA, S. SUMIDA, T. YAMADA, Y. TOKUMARU, T. SHIRIO, M. SASAOKA, M. TANIGUCHI, S. TORII, "A New Short-Cut Route to 3-Cephalosporins", pages 888-890.
See also references of EP 0803506A4
SYNLETT., 1991, No. 12, H. TANAKA, Y. KAMEYAMA, S. SUMIDA, T. YAMADA, Y. TOKUMARU, T. SHIRIO, M. SASAOKA, M. TANIGUCHI, S. TORII, "A New Short-Cut Route to 3-Cephalosporins", pages 888-890.
See also references of EP 0803506A4
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