CAS: 1332524-01-2; Methyl 2-((3-Fluoro-4-(Methylcarbamoyl)Phenyl)Amino)-2-Methylpropanoate

相似化合物

1289942-66-0 1258638-92-4 1242137-20-7

上下游产品

CAS号1289942-66-0 N-(3-氟-4-((甲基氨基... | CAS号74-88-4 碘甲烷 | CAS号112704-79-7 4-溴-2-氟苯甲酸 | CAS号151982-51-3 4-溴-2-氟苯甲酰氯 | CAS号749927-69-3 N-甲基-4-溴-2-氟-苯甲酰胺 | CAS号915087-33-1 恩杂鲁胺

4-溴-2-氟苯甲酸置于氯化亚砜,Potassium Carbonate,Copper(L) Chloride体系中,用 醋酸异丙酯,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 19.25H,反应生成N-[3-氟-4-[(甲基氨基)羰基]苯基]-2-甲基-丙氨酸甲酯
参考文献:带有五氟硫烷基(sf 5)和五氟乙基(c 2 F 5)取代基的比卡鲁胺,恩杂鲁胺和enobosarm衍生物的新系列:改进的抗前列腺癌抗增殖剂
标题:带有五氟硫烷基(sf 5)和五氟乙基(c 2 F 5)取代基的比卡鲁胺,恩杂鲁胺和enobosarm衍生物的新系列:改进的抗前列腺癌抗增殖剂
摘要:提出了用多氟基团官能化的比卡鲁胺,烯醇和恩杂鲁胺类似物的sar研究.在合成的新型比卡鲁胺和enobosarm衍生物中,有几种显示出显着改善的体外抗癌活性,对四种不同的前列腺癌细胞系(lncap,Vcap,Du-145和22Rv1)的ic 50值在低微摩尔范围内,最高显示48与父代结构相比增加了三倍.特别地,发现sf 5 Enobosarm类似物是最有效的化合物,完全的ar拮抗剂并且具有有利的adme特性.对最有前途的化合物(48A)进行了体内评估 在pc异种移植小鼠模型(22Rv1)中的功效,其结果可与护理标准多西紫杉醇相媲美.
Doi:10.1016/j.Ejmech.2019.07.001

专利信息

专利号:US-9174943-B2
优先权日:2010-02-24
标 题 :Processes for the synthesis of diarylthiohydantoin and diarylhydantoin compounds
发明人：JAIN RAJENDRA PARASMAL; ANGELAUD REMY; THOMPSON ANDREW; LAMBERSON CAROL; GREENFIELD SCOTT
权利人:JAIN RAJENDRA PARASMAL; ANGELAUD REMY; THOMPSON ANDREW; LAMBERSON CAROL; GREENFIELD SCOTT; MEDIVATION PROSTATE THERAPEUTICS INC
摘要:Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.

专利号:US-10626091-B2
优先权日:2014-10-01
标 题 :Process for the preparation of enzalutamide
发明人：CHIVUKULA KAMESWAR RAO; KARUTURI VEERA VENKATESWARA RAO; BENDA SRINIVAS; ANKE RAMACHANDRA; GAJULA DHARMAPURI; MOTURU VENKATA RAMA KRISHNA MURTHY; INDUKURI VENKATA SUNIL KUMAR; GORANTLA SEETA RAMA ANJANEYULU; CHAVA SATYANARAYANA
权利人:LAURUS LABS LTD
摘要:The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave irradiation and noxious reagents. The present invention also relates to an improved process for preparation of 4-isothiocyanato-2-(trifluoromethyl) benzonitrile, which is an intermediate in the synthesis of Enzalutamide.

专利号:US-2017190670-A1
优先权日:2014-07-11
标题:Improved process for the preparation of enzalutamide
发明人：HIRPARA SANJAY; SHRAWAT VIMAL KUMAR; POTHURAJU RAJU; TRIPATHI CHANDRESH KUMAR; AKSHAYKANT CHATURVEDI
权利人:SHILPA MEDICARE LTD
摘要:The present application relates to an improved process for preparation of Enzalutamide (I). n n n n n n n n n n The present application also relates to an improved process for the preparation of substantially pure Enzalutamide (I) having purity of greater than 99.5%. n The present application also relates to a novel process for the preparation of Enzalutamide intermediate useful in the industrially viable synthesis of Enzalutamide.

专利号:JP-2013520519-A
优先权日:2010-02-24
标题:Process for the synthesis of diarylthiohydantoin compounds and diarylhydantoin compounds

专利号:ES-2880354-T3
优先权日:2010-02-24
标 题 :Processes for the synthesis of diarylthiohydantoin and diarylhydantoin compounds

专利号:WO-2011106570-A1
优先权日:2010-02-24
标 题 :Processes for the synthesis of diarylthiohydantoin and diarylhydantoin compounds