發(fā)布時間：2018-07-10 20:26

  本文選題：雄激素受體拮抗劑 + MDV�。� 參考：《精細(xì)化工中間體》2012年01期

【摘要】：以3-三氟甲基-4-腈基-苯胺和二硫化碳為原料制備異硫氰酸酯4-異硫氰基-2-三氟甲基苯腈(2),以2-氟-4-硝基甲苯為原料,經(jīng)氧化、酰胺化、催化氫化制得N-甲基-2-氟-4-氨基苯甲酰胺(5),5與2-溴異丁酸乙酯反應(yīng)得到2-(3-氟-4-甲胺甲酰苯基)胺基苯胺-2-甲基丙酸乙酯(6),2和6在無水N,N-二甲基甲酰胺溶液中縮合得到MDV3100(1),結(jié)構(gòu)經(jīng)MS和1H NMR確證,總收率18%(以2-氟-4-硝基苯甲酸計,n/n)。
[Abstract]:Isothiocyanate 4-isothiocyano-2-trifluoromethylbenzonitrile (2) was prepared from 3-trifluoromethyl-4-nitriline and carbon disulfide. Catalytic hydrogenation of N-methyl-2-fluoro-4-aminobenzoamide (5) -5 to ethyl 2-bromoisobutyrate to give ethyl 2- (3-fluoro-4-methylaminophenyl) aminoaniline (6) -2-methylpropionate in anhydrous N-dimethylformamide solution by condensation of 2- (3-fluoro-4-methylaminophenyl) aminoaniline (6) 2 and 6 in anhydrous N- N-dimethylformamide solution MDV3100 (1) was obtained and its structure was confirmed by MS and 1H NMR. The total yield was 18% (n / n based on 2-fluoro-4-nitrobenzoic acid).
【作者單位】： 中國藥科大學(xué)藥物化學(xué)教研室;
【分類號】：R914
，

本文編號：2114608