摘要:
The present invention relates to a process for preparing a key intermediate of cefprozil and use of this intermediate in the preparation of cefprozil thereby avoiding impurity-causing self-acylation. [R-(Z)]-[4-hydroxy-α-[(3-methoxy-l-methyl-3-oxo-1-propenyl)amino]] benzeneacetic acid, mono potassium salt is reacted with ethyl chloroformate to obtain mixed anhydride which is then silylated with N,O-bis(trimethylsilyl)acetamide. The silylated compound obtained is reacted with [7-trimethylsilylamino-3-(Z/E-propen-1-yl)-3-cephem-4-carboxylic acid]trimethylsilyl ester and deprotected with aqueous hydrochloric acid to give cefprozil.
摘要:
A 3-(Z)-propenyl cephem compound is selectively prepared by reacting a phosphoranylidene cephemcompound with acetaldehyde in the presence of a base in a solvent mixture comprising diethyl ether, formula (I), wherein R is a carboxyl protecting group; R1 is hydrogen or R2CH2CO-; and R2 is ethyl, 2-thiophenyl, phenyl, p-hydroxyphenyl or phenoxy.
摘要:
A process for the preparation of a 3-vinylcephem compound, characterized by treating a protected 3-vinylcephem derivative of the general formula (1) in an organic solvent in the presence of a perhalogenic acid and an organic protonic acid to thereby obtain a 3-vinylcephem compound of formula (2). In general formula (1), R?1, R2 and R3¿ are each hydrogen or optionally substituted arylmethyl, with the proviso that all of R?1, R2 and R3¿ must not be hydrogen.
摘要:
A method of improving the stability of a quaternary ammonium salt; and a process for efficiently producing the quaternary ammonium salt having improved stability.
摘要:
High purity cefdinir is prepared in a high yield by a process comprising the steps of: treating a cefdinir intermediate with a formic acid-sulfuric acid mixture or a formic acid-methanesulfonic acid mixture to obtain a crystalline salt of cefdinir and reacting the crystalline salt with a base in a solvent.
摘要:
A process for the preparation of 3-sulfonyloxy-3-cephem compounds of general formula (3), characterized by reacting a 3-hydroxy-3-cephem compound of general formula (1) with a sulfonic acid halide of general formula (2) :R4SO2x, in an organic solvent in the presence of an alkali metal carbonate or an alkaline earth metal carbonate wherein R1 to R4 and X are each as defined in the description.