Process for the preparation of hydroxy-.alpha.-amino- benzyl...

C - Chemistry – Metallurgy – 07 – D

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260/114.7

C07D 499/68 (2006.01) C07D 499/00 (2006.01)

Patent

CA 1100484

ABSTRACT This invention is related to a process for the pre- paration of hydroxy-.alpha.-amino-benzyl penicillin, whereby the conversion product resulting from D(-) p-hydroxy-C-phenyl- glycine with ethyl or methyl acetylacetate and triethylamine is made to react with 3-trimethylsilyl-2-oxazolidinone to obtain a compound which is reacted with pivalyl chloride, 2-ethylhexanoyl chloride and alkyl chloroformiate and the product is then reacted with a triethylamine salt or with the trimethylsilyl ester of 6-aminopenicillanic acid. The re- sultant product is treated with water and acid to pH 6 to produce a solution of amoxicillin from which the antibiotic is isolated by precipitation at pH 3.30 to 4.20.

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