Penicillins

C - Chemistry – Metallurgy – 07 – D

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260/118.5

C07D 499/04 (2006.01) C07D 499/00 (2006.01)

Patent

CA 1140916

ABSTRACT Title: "Penicillins" 6-? and 6- ? -substituted penicillanic acid derivatives of the formula: Image --- (I) wherein R is H or a conventional penicillin carboxy protecting group or an ester forming residue readily hydrolysable in vivo and R1 is a perhaloalkyl group of from 1 to 4 carbon atoms wherein the halogen atoms are fluorine or chlorine, undergo SN2 nucleophilic displacement with inversion of configuration at C-6 to yield the corresponding 6- .beta. or 6- ? -substituted product. The compounds are therefore valuable intermediates particularly for the preparation of 6- ?- halo-penicillanic acid derivatives.

352042

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