title: Synthesis of new N,N-disubstituted 4-amino-5,6-dihydro-3-phenyl-2H-thieno[2,3-h]-1-benzopyran-2-ones.
abstract: The synthesis of some N,N-disubstituted 4-amino-5,6-dihydro-3-phenyl-2H-thieno[2,3-h]-1-benzopyran-2-ones (4a-f), by reaction of phenylchloroketene with a series of N,N-disubstituted (E)-5-aminomethylene-6,7-dihydrobenzo[b]thiophen-4(5)-ones, followed by dehydrochlorination in situ of the primary adducts with DBN, is described. A moderate local anaesthetic activity was observed in the title compounds, particularly in 4e.
authors.affiliation: Dipartimento di Scienze Farmaceutiche dell'Università di Genova, Italy. longobar@unige.it
authors.forename: M
authors.initials: M
authors.lastname: Longobardi
authors.forename: E
authors.initials: E
authors.lastname: Mariani
authors.forename: A
authors.initials: A
authors.lastname: Bargagna
authors.forename: F
authors.initials: F
authors.lastname: Mazzeo
authors.forename: M R
authors.initials: MR
authors.lastname: Vitelli
authors.forename: L
authors.initials: L
authors.lastname: Giordano
authors.forename: G
authors.initials: G
authors.lastname: Falcone
mesh_terms: D000698:Analgesia; D000779:Anesthetics, Local / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000779:Anesthetics, Local; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans