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2H-[1]benzothiepino [5,4-b]pyran derivatives with local anesthetic and antiarrhythmic activities
Authors:M Longobardi  A Bargagna  E Mariani  P Schenone  S Vitagliano  L Stella  A Di Sarno  E Marmo
Affiliation:Istituto di Farmaceutiche dell'Università, Genova, Italy.
Abstract: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.
Keywords:
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