3 - (1 - methyl--5 - methylthio-1-H-tetrazole) - Aminocephalosporanic acid phenyl methyl ester Study.docVIP

 PAGE \* MERGEFORMAT 19 3 - (1 - methyl--5 - methylthio-1-H-tetrazole) - Aminocephalosporanic acid phenyl methyl ester Study 【Abstract】 The ACA was synthesized from 3 - (1 - methyl--5 - methylthio-1-H-tetrazole) - Aminocephalosporanic acid phenyl ester purpose of the study through the optimization of reaction conditions, streamline operations, improve yield and reduce the cost of synthesis. Through the solvent, catalyst, feed ratio, reaction temperature and reaction conditions, such as optimization of concentration to about 80% of two-step preparation of synthetic yield of 3 - (1 - methyl--5 - methylthio-1-H-4 N-yl) - Aminocephalosporanic acid phenyl ester. Keywords: cephalosporins; ACA; 3 - (1 - methyl--5 - methylthio-1-H-tetrazole) - Aminocephalosporanic acid phenyl ester; Synthetic ABSTRACT The synthesis process of 7-ATCA-diPh from 7-ACA was explored in this paper. By optimizing the reaction conditions, such as catalyst quantity, substrates  ratio, temperature and solution concentration, the two-step overall yield of 7-ATCA -diPh reached 80%. KEY WORDS Cephalosporin; 7-ACA; 7-ATCA-diPh; Preparation 3 - (1 - methyl--5 - methylthio-1-H-tetrazole) - Aminocephalosporanic acid phenyl ester (7-ATCA-diPh, 5) is a widely used drug intermediate to the compound as the raw material can be synthesized a series of cephalosporin drugs, such as third-generation cephalosporin antibiotics, cefotetan, cefmetazole, and cefoperazone and other cephalosporins Domino. At present, the 7 - ACA (7-ACA, 1) was synthesized from 7-ATCA-diPh (5) the method for the first multi-compound 1, 7 amino substituted later by a 3 side chain modification of and 4-carboxylic acid esterification, the reaction conditions, harsh, post-processing complex, and the low yield [1,2]. We went on to 7 - ACA (7-ACA, 1) was synthesized from 3 - (1 - methyl--5 - methylthio-1-H-tetrazole) - Aminocephalosporanic acid phenyl methyl ester (7-ATCA-diPh, 5) reaction of hope that th