Manufacture of semi-synthetic penicillin antibiotics

Details Manufacture of semi-synthetic penicillin antibiotics Manufacture of semi-synthetic penicillin antibiotics

1978-06-09

1980-01-01

Schwartz, Gerald A.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07D49968

Patent

active

041816560

ABSTRACT:
A process for preparing semi-synthetic penicillin antibiotics, especially ampicillin, is disclosed which comprises silylating 6-aminopenicillanic acid using a silylating agent which generates a primary or secondary carboxamide base, and then acylating the silylated 6-aminopenicillanic acid in situ using the primary or secondary carboxamide base as hydrogen halide acceptor. No further base needs to be added, and the products may be obtained in good yield and high purity with the amount of toxic contaminants in the products significantly reduced. Unpleasant side-effects may thus be substantially eliminated.

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