Jin Ning-ren
2011
Citations
0
Influential Citations
0
Citations
Journal
Guangzhou Chemical Industry
Abstract
Diphenylmethyl 7-(4-tolysulfenylimino)-3-[(1-methyl-1H-tetrazo-5-yl) thiomethyl]-3-cephem-4-carboxylate(7-DTMC) was the important intermediates for the synthesis of 7α-Methoxy-7β-Amino-3-[(1-Methyl-1-H-tetrazo-5-yl) thiomethyl]-3-cephem-4-carboxylic acid diphenylmethyl ester(7-MAC) and 7-MAC was the key intermediate for preapring 7α-methoxycephalosporins.7-DTMC was synthesized by using 7β-amino-3-[(1-methyl-1-H-tetrazo-5-yl) thiomethyl]-3-cephem-4-carboxylate(7-DAMC) and 4-tolysulfenyl chloride(TSC) as the materials,the dichloromethane used as the solvent,the 1,2-propylene oxide as the catalyst.The main four influential factors of nucleophilic substitution reaction such as the molar ratio,the amount of catalysis,the reaction time and temperature were studied.By using orthogonal quadratic regression design,the mathematic model was established and the optimization experimental conditions were obtained.The yield of 7-DTMC was 89.71%,the purity of HPLC was 99.34%,and its molecular structure was exactly identified by 1H-NMR and FT-IR.