PROCESSES FOR THE PRODUCTION OF 2-ISOCEPHEM DERIVATIVES

Title:

PROCESSES FOR THE PRODUCTION OF 2-ISOCEPHEM DERIVATIVES

Document Type and Number:

WIPO Patent Application WO/1996/028453

Kind Code:

A1

Abstract:

A process for producing a 2-isocephem derivative which comprises treating, in a water-containing organic solvent, a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by general formula (1) with a thioacetic acid derivative showing basicity per se or a mixture of a base with a thioacetic acid derivative to thereby give a 3-halomethyl-2-isocephem derivative represented by general formula (2); and a process for producing a 2-oxaisocephem derivative which comprises treating, in a water-containing organic solvent, a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by general formula (1) with a base to thereby give a 3-halomethyl-2-oxaisocephem derivative represented by general formula (3); in formula (1), R1 represents hydrogen or optionally protected amino; R2 represents hydrogen or lower alkoxy, or R1 and R2 may form together a cyclic amino protecting group; R3 represents hydrogen or a carboxyl protecting group; W represents a leaving group; and X and Y may be the same or different and each represents halogeno; in formula (2), R1, R2, R3 and X are each as defined above; in formula (3), R1, R2, R3 and X are each as defined above.

Inventors:

SASAOKA MICHIO (JP)
SUZUKI DAISUKE (JP)
SUH DELSOO (JP)
TOKUMARU YOSHIHISA (JP)

Application Number:

PCT/JP1996/000538

Publication Date:

September 19, 1996

Filing Date:

March 06, 1996

Export Citation:

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Assignee:

OTSUKA KAGAKU KK (JP)
SASAOKA MICHIO (JP)
SUZUKI DAISUKE (JP)
SUH DELSOO (JP)
TOKUMARU YOSHIHISA (JP)

International Classes:

A61K31/54; A61P31/04; C07D513/04; C07D205/08; C07D498/04; C07D501/00; C07D507/08; (IPC1-7): C07D513/04

Foreign References:

JPS63211283A

1988-09-02

Other References: