The recent story of isepamicin…
Synthesis of isepamicin via regioselective N-formylation of
gentamicin B with 2-formylmercaptobenzothiazole.
Tann, Chou-Hong; Thiruvengadam, Tiruvettipuram K.;
Chiu, John S.; Colon, Cesar; Green, Michael D.
(Schering Corporation, USA). U.S. (1995)
An improved process for converting gentamicin B to isepamicin (I)
via 3,6'-di-N-formylgentamicin B, acylating the 1-amino group with
an N-protected (S)-isoserine compd. and removing all the blocking
groups under conditions which result in high yields of isepamicin.
A novel formylating agent, 2-formylmercaptobenzothiazole, and
intermediate compds. are also disclosed.