2H-[1]benzothiepino [5,4-b]pyran derivatives with local anesthetic and antiarrhythmic activities
Longobardi, M.; Bargagna, A.; Mariani, E.; Schenone, P.; Vitagliano, S.; Stella, L.; Di Sarno, A.; Marmo, E.
Farmaco 45(4): 399-404
1990
ISSN/ISBN: 0014-827X PMID: 2400514 Document Number: 353357
The synthesis of some N,N-disubstituted 4-amino-5,6-dihydro-3-phenyl-2H-[1]benzothiepino [5,4-b]pyran-2-ones by reaction of phenylchloroketene with a series of N,N-disubstituted (E)-4-aminomethylene-3,4-dihydro-1-benzothiepin-5(2H)-ones, followed by dehydrochlorination of the primary adducts with DBN, is described. The 4-methylphenylamino derivative showed a local anesthetic activity in mice superior to that of lidocaine and the 4-morpholino derivative showed an antiarrhythmic activity in rats comparable to that of quinidine.