(R)-Nifuratel, its use for the treatment of infections and synthesis of (R) and (S)-Nifuratel

摘要

(R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.

主权项

1. A process for the manufacture of (S)-Nifuratel which comprises the following steps:
(a) reacting (S)-2-(benzyloxymethyl)oxirane with hydrazine to obtain compound 1; (b) converting compound 1 into compound 2; (c) de-benzylating compound 2 to obtain compound 3; (d) converting compound 3 into compound 4; (e) converting compound 4 into (S)-Nifuratel.