Process for producting 7-acylamido-7-alkoxycephalosporins

Details Process for producting 7-acylamido-7-alkoxycephalosporins Process for producting 7-acylamido-7-alkoxycephalosporins

C - Chemistry, Metallurgy

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C07D 501/00 (2006.01) A61K 31/545 (2006.01) C07D 501/04 (2006.01) C07D 501/18 (2006.01) C07D 501/20 (2006.01) C07D 501/57 (2006.01) C07D 501/60 (2006.01) C07F 9/24 (2006.01)

Patent

CA 1042421

ABSTRACT OF THE DICLOSURE The present invention relates to a proce3s for the preparation of 7-acvlamido-7-alkoxycephalosporins which comprises reacting a 7-(5-amino-5-carboxyvaleramido)- 7-methoxycephalosporin with amino and acid groups protected, with PCl5 or other agent capable of forming an imino halide; thereafter reacting the resulting imino halide under essentially non-aqueous conditions with a primary lower- alkanol of C1-C4 or with methan-d3-ol, to yield a nucleus bearing a 7-alkoxv group derived from the primary lower- alkanol or methan-d3-ol. In situ acylation of the nucleus affords 7-acylamido-7-alkoxycephalosporins in good yield. These products can he deesterified to yield the corresponding acids, which exhihit antibacterial activity.

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