REACTION OF KETENES WITH N,N-DISUBSTITUTED ALPHA-AMINOMETHYLENEKETONES .24. 2H-PYRANO[3,2-D]-1-BENZOXEPIN DERIVATIVES WITH PLATELET ANTIAGGREGATING AND OTHER ACTIVITIES

The synthesis of some N,N-disubstituted 4-amino-5,6-dihydro-3-phenyl-2H-pyrano[3,2-d]-1-benzoxepin-2-ones by reaction of phenylchloroketene with a series of N,N-disubstituted (E)-4-aminomethylene-3,4-dihydro-1-benzoxepin-5(2H)-ones, followed by dehydrochlorination of the primary adducts with DBN, is described. Some of these compounds showed a platelet antiaggregating activity in vitro slightly superior to that of acetylsalicylic acid, as well as weak local anesthetic and antiinflammatory activities in mice and rats, respectively.