still for framstellning of 7 (alpha - amino - p - hydroxifenylacetamido) - 3 - (1 - methyl - 5 - tetrazolyltiometyl) - 3 - cefem acid and 7 (alpha - amino - p - hydroxifenylacetamido) - 3 - (5 - methyl - 1,3,4 - tiadiazol - 2 - yltiometyl) - 3 - cefem...

摘要

1363833 3-Triazolylthiomethyl cephalsporins SMITHKLINE CORP 21 Feb 1973 [14 June 1972 15 Sept 1972] 8511/73 Headings C2A and C2C Novel cephalosporins having the Formula (I) wherein R is 1,2,3-triazolyl which may be substituted with 1 or 2 groups selected from C 1 -C 4 alkyl and trifluoromethyl are prepared by (a) N-acylating an appropriate 7-amino-3- (1,2,3 - triazolylthiomethyl) - cephem - carboxylic acid with an amino-protected phydroxyphenylglycine or N-acylating derivative thereof; or (b) reacting. 7--amino-p-hydroxyphenylacetamidocephalosporanic acid having the -amino group protected, with an appropriate mercaptomethyl-1,2,3-triazole. Alternatively 7-aminocephalosporanic acid may be reacted according to both of (a) and (b). The amino-protecting group is then removed to give the compound of formula (I). The inventive compounds (I) may be used in pharmaceutical compositions having antibiotic activity, admixed with a pharmaceutical diluent or carrier. The sodium salt of 5-mercapto-4-methyl-1,2,3- triazole is prepared by refluxing 5-benzamido-4- methyl-1,2,3-thiadiazole with aqueous NaOH, and treating an ethyl acetate extract of the product with sodium 2-ethylhexanoate to precipitate the said sodium salt.