PROCESSES FOR THE PREPARATION OF 'beta'-LACTAM DERIVATIVE

Title:

PROCESSES FOR THE PREPARATION OF 'beta'-LACTAM DERIVATIVE

Document Type and Number:

WIPO Patent Application WO/1996/029334

Kind Code:

A1

Abstract:

A process for the preparation of an allenyl-'beta'-lactam compound which comprises reacting the hydroxyl group of a 'beta'-lactam compound of general formula (1) with a reactive functional derivative of a sulfonic acid of the general formula (2): R5-SO2-X to form a 'beta'-lactam compound of general formula (3) and reacting the formed compound with a basic anion-exchange resin containing a tertiary organic base immobilized thereon to attain the preparation of an allenyl-'beta'-lactam compound of general formula (4) and the stable isolation thereof from the reaction mixture in a high yield at a high purity. Another process for the preparation of an allenyl-'beta'-lactam compound which comprises reacting the hydroxyl group of a 'beta'-lactam compound of general formula (1) with a reactive functional derivative of a sulfonic acid of the general formula (2): R5-SO2-X to form a 'beta'-lactam compound of general formula (3), reacting the formed compound with a tertiary organic base to form an allenyl-'beta'-lactam compound of general formula (4) and treating the resulting reaction mixture with both an acidic cation-exchange resin and a basic anion-exchange resin either alternately or simultaneously to isolate the compound of general formula (4) from the reaction mixture stably. A process of preparing a 3-halocephem derivative of general formula (6) by reacting an allenyl-'beta'-lactam compound of general formula (4) with a halogenating agent in the presence of a sulfinate or thiolate ion scavenger.

More Like This:

WO/1997/021675	MONOCYCLIC BETA-LACTAME DERIVATIVES FOR TREATMENT OF ATHEROSCLEROSIS
JPS5559193	BBLACTAM COMPOUND
WO/1994/021250	TAXANES HAVING ALKOXY, ALKENOXY OR ARYLOXY SUBSTITUTED SIDE-CHAIN AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Inventors:

TORII SIGERU (JP)
TANAKA HIDEO (JP)
SASAOKA MICHIO (JP)
KAMEYAMA YUTAKA (JP)
WADA ISAO (JP)
AMANO YASUHISA (JP)

Application Number:

PCT/JP1996/000575

Publication Date:

September 26, 1996

Filing Date:

March 08, 1996

Export Citation:

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Assignee:

OTSUKA KAGAKU KK (JP)
TORII SIGERU (JP)
TANAKA HIDEO (JP)
SASAOKA MICHIO (JP)
KAMEYAMA YUTAKA (JP)
WADA ISAO (JP)
AMANO YASUHISA (JP)

International Classes:

C07D205/09; C07D205/095; C07D501/00; C07D501/08; C07D513/04; (IPC1-7): C07D501/08; C07D205/08

Foreign References:

JPH04282387A	1992-10-07
CH616685A5	1980-04-15

Other References:

SYNLETT, No. 12, p. 888-890, (1991).
J. ORG. CHEM., Vol. 41, No. 13, p. 2276-2279.

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