METHOD FOR PREPARING COMPLEX ETHERS OF SULPHOXIDE 7-ACYLAMINO-3-acyclic cime-DZ-CEFALOSPORIN1 The invention relates to an improved method for the production of cephalosporin derivatives, which can be used in the pharmaceutical industry. CO formulas where R is an acyl group; X is hydrogen or a nucleophilic group; R 'is hydrogen, a silyl group or an alkyl or aralkyl having from 1 to 20 carbon atoms, which means that the corresponding 7-acylamido-A ^ (or A ^ ) -cephalosporin It is recommended to oxidize with peracid or hydrogen peroxide in the presence of acid, and then isolate the products in a known manner. According to the present invention, to simplify the process, it was proposed to carry out the functionalization of the exocyclic oximethyl group at position 3 of the sulfoxide 10157-acylaminodemethyl cephalosporin without associating isomerization of the double bond with a ceraflosporomer cephalosporin-type antibiotics. Described method for preparing 7-acylamino-3-hydroxymethyl-A2-ce

摘要

1312175 Preparation of cephalosporins ELI LILLY & CO 13 Sept 1971 [14 Sept 1970] 42614/71 Heading C2A A process for preparing a 7-acylamido-3-acyloxymethyl #SP3/SP-cephalosporin sulphoxide ester comprises reacting a 7-acylamido #SP3/SP-desacetylcephalosporin sulphoxide ester with the anhydride of a saturated carboxylic acid under acid conditions. In such a process the 7-acylamido #SP3/SP-desacetylcephalosporin sulphoxide ester may have the Formula I wherein R is the residue of the 7-acylamido group and R 1 is the residue of an ester protecting group. The anhydride has the Formula II wherein R 2 is selected from H, C 1 to C 7 alkyl and cycloalkyl having the Formula III wherein n is zero or an integer from 1 to 4 and R 3 is C 1 to C 3 alkylene. The 7-acyl group may be selected from the group IV where n is zero or an integer from 1 to 6 and R may be aryl containing 6-14 carbon atoms, cycloalkyl containing 4 to 8 carbon atoms and heterocyclic groups wherein the hetero atom is selected from O, S, N and combinations thereof, and substituted derivatives thereof or the group V wherein R 3 is C 1 to C 8 alkyl, C 2 to C 8 alkenyl and substituted derivatives thereof, or a group VI wherein n is 0 or an integer from 1 to 5, X is O or S and R 4 is selected from the group consisting of R 2 , C 2 -C 8 alkenyl and substituted C 2 to C 8 alkenyl derivatives or a group VII where Y may be amino, protected amino, hydroxy, C 1 -C 3 alkoxy, carboxyl and C 1 -C 3 alkanoyloxy or the acyl group may be phenyl- ,-dimethylacetyl and substituted derivatives thereof.