CAS: 911297-02-4; 4-(Boc-Amino)-3-Fluoro-Phenol

上下游产品

tert-butyl dicarbonatedi-tert-butyl dicarbonate 4-amino-3-fluorophenol 3-fluoro-4-nitrophenol(S)-{4-[2-(4-cyano-3-trifluoromethylphenylcarbamoyl)-2-hydroxypropoxy]-2-fluorophenyl}carbamic acid tert-butyl ester (S)-{2-fluoro-4-[2-hydroxy-2-(4-nitro-3-trifluoromethylphenylcarbamoyl)propoxy]phenyl}carbamic acid tert-butyl ester (S)-3-(4-amino-3-fluorophenoxy)-2-hydroxy-2-methyl-N-(4-cyano-3-trifluoromethylphenylcarbamoyl)propionamide N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide3-(4-amino-3-fluoro-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide

📜3-氟-4-硝基苯酚置于palladium On Activated Charcoal 氢气,三乙胺体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 4-(Boc-氨基)-3-氟苯酚
参考文献:前列腺癌的芳基异硫氰基选择性雄激素受体调节剂(sarm).
标题:前列腺癌的芳基异硫氰基选择性雄激素受体调节剂(sarm).
摘要:制备了一系列新的雄激素受体靶向剂(arta),并在雄激素依赖性和非依赖性前列腺癌细胞系中进行了测试.这些试剂是具有异硫氰酸根基取代的b环的比卡鲁胺类似物.同样,R-比卡鲁胺的连接基砜被保持或替换为几个可选的连接基,包括醚,胺,N-甲胺,硫醚和亚甲基(在这种情况下,该产品是外消旋混合物)在x位置的官能团.为了扩大这些芳基异硫氰酸根基ar配体的结构活性关系(sar),还制备并测试了b环卤代芳基异硫氰酸根基配体.芳基异硫氰酸根基ar配体对ar的结合亲和力范围为0.6到54 Nm.其中,硫醚和醚键表现出高结合亲和力(0.6和4.6 Nm,与雄激素非依赖性前列腺癌细胞系(du145,Pc-3和ppc-1)相比,对lncap(一种雄激素依赖性前列腺癌细胞系)分别具有选择性和选择性的细胞生长抑制作用(约3至6倍),并且膀胱细胞系(tsu-Pr1).但是,配体在正常猴肾细胞系(cv-1)中是无活性的(ic50>
DOI:10.1016/j.Bmc.2006.06.019

专利信息

专利号:US-9708317-B2
优先权日:2013-11-25
标 题 :Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-B]pyrazin-3-one derivatives
发明人：ZAMBON ALFONSO; NICULESCU-DUVAZ DAN; CHUBB RICHARD; SPRINGER CAROLINE JOY
权利人:CANCER RES TECH LTD; INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE); OXY SCIENT LTD; THE INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
摘要:The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.