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...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%）.展开更多
文摘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%）.
