RO-098246
Chemical Name: 2(R)-(2,4-Fluorophenyl)-3(R)-[3-[4-(1,2,3-thiadiazol-4-yl)phenyl]-1,2,4-thiadiazol-5-yl]-1-(1H-1,2,4-triazol-1-yl)butan-2-ol
CAS No. 368421-38-9
项目整合开发状态: Biological Testing
项目研究机构: Basilea Pharmaceutica (Originator)
合成路线:Addition of trimethylsilyl cyanide to the known epoxide (I) produced the hydroxy nitrile (II).This was converted to the thioamide (III) upon treatment with diethyl dithiophosphate.Condensation between thioamide (III) and thiadiazolyl thiobenzamide (IV) in the presence of iodine furnished the target thiadiazole derivative.
📌 参考资料/链接：
参考文献标题:Azole derivs.
文献作者:Shimma,N.; Tsukuda,T.; Komiyama,S.(Basilea Pharmaceutica AG)
参考来源:US 6319933; WO 0179196
📄 详细内容
合成路线:Addition of trimethylsilyl cyanide to the known epoxide (I) produced the hydroxy nitrile (II).This was converted to the thioamide (III) upon treatment with diethyl dithiophosphate.Condensation between thioamide (III) and thiadiazolyl thiobenzamide (IV) in the presence of iodine furnished the target thiadiazole derivative.
参考文献标题:Parallel synthesis of azole antifungals and identification of novel thiadiazole-containing antifungals
文献作者:Fujii,T.; Tsukuda,T.; Shimma,N.; Komiyama,S.
参考来源:223rd ACS Natl Meet (April 7 2002,Orlando) 2002,Abst MEDI 175