专利号:US-5945414-A 优先权日:1996-12-03 标 题:Process for the preparation of new intermediates useful in the synthesis of cephalosporins 发明人:SOGLI LORIS; TERRASSAN DANIELE; BERNASCONI ERMANNO; SALTO FRANCISCO 权利人:ANTIBIOTICOS SPA 摘要:Cefazolin, cefazedone, cefoperazone, cefamandole, cefatrizine or ceftriaxone is prepared by reacting glutaryl 7-ACA of the formula: with a compound of formula (II): R-SH(II) wherein R is 5-methyl-1,3,4-thiadiazol-2-yl, 1H-1,2,3-triazol-4-yl, 1-methyl-tetrazol-5-yl or 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl group, and R1 and R2 are both hydrogen and the other is an acyl group, in an aqueous solution in an amount of 3-5 mols per mol of glutaryl 7-ACA to about 90 DEG C. and for a time from about 2 to about 10 hours; optionally recovering the excess of the compound of formula (II), thereby preparing a compound of formula (III) in an aqueous solution: wherein R is as above defined and optionally deacylating said compound of formula (III); and converting the resulting compound of formula (I) wherein R, R1 and R2 are as defined above in the presence of a non-chlorinated solvent into one of said cephalosporins.
专利号:US-9006421-B2 优先权日:2013-03-14 标题 :Cephalosporin compositions and methods of manufacture 发明人:LAI JAN-JI; PATHARE PRADIP M; KOLLA LAXMA; SORET ADRIEN F 权利人:CUBIST PHARM INC 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
专利号:EP-0846695-A1 优先权日:1996-12-03 标题:Process for the preparation of new intermediates useful in the synthesis of cephalosporins