雄激素受体拮抗剂MDV3100的合成研究

发布时间：2018-07-10 20:26

  本文选题：雄激素受体拮抗剂 + MDV　； 参考：《精细化工中间体》2012年01期

【摘要】：以3-三氟甲基-4-腈基-苯胺和二硫化碳为原料制备异硫氰酸酯4-异硫氰基-2-三氟甲基苯腈(2),以2-氟-4-硝基甲苯为原料,经氧化、酰胺化、催化氢化制得N-甲基-2-氟-4-氨基苯甲酰胺(5),5与2-溴异丁酸乙酯反应得到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在无水N,N-二甲基甲酰胺溶液中缩合得到MDV3100(1),结构经MS和1H NMR确证,总收率18%(以2-氟-4-硝基苯甲酸计,n/n)。
[Abstract]:Isothiocyanate 4- isothiocyanate -2- three fluoromethylbenzonitrile (2) was prepared from 3- three fluoromethyl -4- nitrile base aniline and carbon disulfide, and 2- fluorine -4- nitrotoluene was used as raw material to produce N- methyl -2- fluorine -4- aminophenoformamide (5) by oxidation, amidation and catalytic hydrogenation, and 2- (3- fluorine methylamine methylamine) amine group was obtained from 5 and 2- bromide. Ethyl aniline -2- methyl propionate (6), 2 and 6 were condensed into MDV3100 (1) in the aqueous N, N- two methyl formamide solution, and the structure was confirmed by MS and 1H NMR, with a total yield of 18% (with 2- fluoro -4- Nitrobenzoic Acid, n/n).
【作者单位】： 中国药科大学药物化学教研室;
【分类号】：R914
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本文编号：2114607