Processes for making cephems from allenylazetidinone derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

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Other Related Categories

540215, 540222, 540228, 540230, C07D20595, C07D50108, C07D41712

Type

Patent

Status

active

Patent number

051625245

Description

ABSTRACT:
This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.
This invention also relates to an intermediate represented by formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3 and n are as defined above.

REFERENCES:
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Conway et al., Canadian Journal of Chemistry, "Nuclear Analogs of .beta.-Lactam Antibiotics", 56, p. 1335 (1978).
Fleming et al., Tetrahedron, "The Silyl-Cupration and Stannyl-Cupration of Allenes", 45, No. 2, p. 413 (1989).
Corey et al., Tetrahedron Letters, "Synthesis of a New Series of Potent Inhibitors of Thromboxane A.sub.2 Biosynthesis", 24, No. 32, p. 3291 (1983).
Ohmori et al., Tetrahedron Letters, "Stereocontrolled Synthesis of Steroid Side Chain", 23, No. 45, p. 4709 (1982).
Clinet et al., Nouveal Journal de Chemie, "An Efficient Method for the Preparation of Conjugated Allenic Carbonyl Compounds", 1, p. 373 (1977).

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