Cephalosporine desacetoxy esters and salts thereof

Details Cephalosporine desacetoxy esters and salts thereof Cephalosporine desacetoxy esters and salts thereof

1981-03-04

1983-06-14

Coughlan, Jr., Paul M.

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

Organic compounds

Chalcogen in the nitrogen containing substituent

544 30, C07D50122

Patent

active

043884601

ABSTRACT:
Cephalosporine desacetoxy esters having the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and R.sub.1 is selected from the group consisting of ##STR3## Such esters and salts thereof having antibiotic activity are prepared by reacting 7-ADCA with bromophthalide or chloromethyl pivalate in the presence of an alkylamine at a temperature in the range of 0.degree.-70.degree. C. The reaction product is reacted with chloride chlorohydrate of D(-)dihydrophenylglycine or D(-)p-hydroxy phenylgycine.
A salt of the compound of formula (I) is isolated from the reaction mixture, which after washing with acidic water and addition of a pharmaceutically acceptable acid is obtained by treatment with suitable solvent.

REFERENCES:
patent: 4107433 (1978-08-01), Bentley et al.
patent: 4172198 (1979-10-01), Kamiya et al.

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