Process for 3-chloro cephalosporin nucleus

Details Process for 3-chloro cephalosporin nucleus Process for 3-chloro cephalosporin nucleus

1980-09-04

1981-07-28

Rizzo, Nicholas S.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

424246, C07D50104

Patent

active

042811171

ABSTRACT:
7-Amino-3-hydroxy-3-cephem esters react with a chlorinating agent, e.g. phosgene, thionyl chloride and preferably PCl.sub.3 -DMF to provide 7.beta.-[(dimethylaminomethylene)amino]-3-chloro-3-cephem esters which on reaction with a carboxylic acid, a percarboxylic acid, or a phenol, having a pH in water of about 2-5, afford 7.beta.-formamido-3-chloro-3-cephem esters, and corresponding 2-cephem esters. Percarboxylic acids provide 7.beta.-formamido-3-chloro-3-cephem ester 1-oxides. The 7-formamido derivatives provide the 7-amino-3-chloro-3-cephem ester on acid hydrolysis. The 7-amino-3-chloro esters are useful for preparing antibiotics.

REFERENCES:
patent: 4064343 (1977-12-01), Chauvette
patent: 4115643 (1978-09-01), Kukolja et al.
patent: 4223133 (1980-09-01), Bunnell
patent: 4226986 (1980-10-01), Matfield et al.
J. Altman et al., "7-N-Amidinocephalosporins", J. Med. Chem., 1975, vol. 18, _No. 6, pp. 627-630.
F. J. Lund, "6.beta.-Amidinopenicillanic Acids-Synthesis and Antibacterial Properties", Recent Advances in the Chemistry of .beta.-Lactam Antibiotics, Ed. J. Elks, Specialist Publication-Chemical Society, No. 28, 1977, pp. 25-45.
B. Baltzer et al., "Degradation of Mecillinam in Aqueous Solution", J. Pharm. Sci., 68, No. 10, Oct. 1979, pp. 1207-1215.

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