SYNTHESIS AND ANTI α-ADRENOCEPTOR ACTIVITY IN VITRO OF 4-((4-((2-SUBSTITUTEDPHENOXY)ETHYL)-1-PIPERAZINYL) METHYL)-1,2-DIHYDRO-QUINOLINE-2-ONE COMPOUNDS

AIMTo study the synthesis and anti α-adrenoceptor activity of 1,2-dihydro-quinoline-2-one compounds. METHODSAcylation, bromination and cyclization, and substitute reactions were used in the synthesis of the title compounds IV. A proposed mechanism was showed to explain the unusual compounds 5 and 6 in the route C. The inhibition activity of the six target compounds were tested. RESULTSTwelve new compounds were synthesized (II_1～6 and IV_1～6). Among them, six new compounds (IV_1～6) are the title compounds. Structure of the title compounds were determined by IR, ¹HNMR, MS and HRMS. CONCLUSIONCompounds IV₃, IV₄ and IV₆ showed inhibiiton activity, and were worth further studying.