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摘要：Potassium benzylpenicillin (PGK), benzophenone hydrazone (BPH), and peracetic acid (PAA) were used as raw materials to synthesize penicillin G sulfoxide diphenyl methyl ester (I) by the esterification and oxidation. Then, thiazolidine azepine derivatives (II) were synthesized from I and trimethyl phosphite II underwent ozonation, sulfonylation, and amidation to give thiazoline enol ester (III). Finally, 3-hydroxycephalosporin (CBG) was obtained from III through bromination and hydrolysis. The effects of substrate equivalents, reaction temperature, time, concentration, and solvent on the yield of product were investigated, the optimal reaction conditions were obtained. The total yield of the process was 60.4% using PGK as raw material. For Compound I, the yield was 93.2%, under the condition of n (PGK): n (BPH): n (PAA) = 1:1.15:2.4 (n is amount of substance). The yield of compound II was 90.8%, under the conditions of n (compound I): n (trimethyl phosphite) =1: 1.4, m (toluene): m (1,2-dichloroethane) = 4:1 (m is mass), and the reaction time was 6 h. Under the condition of m (II): m (methanol): m (methylene chloride) =1:1:8, the yield of compound III was 79.1%. For the CBG, under the condition of n (III): n (quinoline): n (bromine) = 1:1:1.1, at temperature of -15 degrees C, the yield of CBG reached 90.3%.

卷号：32

期号：4

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