摘要
A route for the synthesis of nefazodone is reported. Nefazodone was obtained with an overall yield of 37.2% from phenol. The key steps involve the improved synthesis of 5-ethyl-4-( 2- phenoxyethyl)-1, 2, 4-triazol-3 (2H)-one, a key intermediate in the synthesis of nefazodone. The phenol was etherified with 1, 2-dichloroethane (75%), followed by iodination-amination with Nal and CH3OH-NH3( 85.7%), acylation with ethyl chloroformate (95.7%) and cyclization with propionyl hydrazine ( 83.6%).
为 nefazodone 的合成的一条线路被报导。Nefazodone 从酚与 37,2% 的全面收益被获得。关键步包含改进合成 of5-ethyl-4-(2-phenoxyethyl )-1, 2, 4-triazol-3 (2H )-one, 在合成 ofnefazodone 的关键中介。酚是有 1 的 etherified, 2-dichioroethane (75%) ,有 Nal 和 CH_3OH-NH_3 (85.7%) 的跟随的 byiodination 胺化作用,氯仿吃了的有乙醇的酰化作用(95.7%) 和有 propionyl 肼(83.6%) 的环合。