Cephalosporine desacetoxy esters, salts thereof and...

C - Chemistry – Metallurgy – 07 – D

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C07D 501/22 (2006.01) A61K 31/545 (2006.01) C07D 501/00 (2006.01) C07D 501/28 (2006.01)

Patent

CA 1171405

ABSTRACT OF THE DISCLOSURE Cephalosporine desacetoxy esters having the formula Image (I) wherein R is selected from the group consisting of Image and R1 is selected from the group consisting of Image and -CH2-OCOC (CH3)3 Such esters and salts thereof having antibiotic activity are prepared by reacting 7-amino-desacetoxycephalosporanic acid (7-ADCA)with bromophtalide or chloromethyl pivalate in the presence of an alkylamine at a temperature in the range of 0°-70°C. The rsaction product is reacted with chloride chlorohydrate of D(-)dihydrophenyl glycine or D(-) p-hydroxy phenylglycine . A salt of the compound of formula (I) is isolated from the reaction mixturer which after washing with acidic water and addition of a pharmaceutically acceptable acid is obtained by treatment with suitable solvent.

372576

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