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邻硝基苯甲酸置于氯化亚砜,铁粉,氯化铵体系中,用 甲醇,水 作为反应溶剂,化学反应 7.0H,反应生成 2-氨基-N-甲基苯甲酰胺
参考文献:含磷酰胺的二苯基嘧啶类似物(pa-Dppys)作为有效的粘着斑激酶(fak)抑制剂,对胰腺癌细胞系具有增强的活性
标题:含磷酰胺的二苯基嘧啶类似物(pa-Dppys)作为有效的粘着斑激酶(fak)抑制剂,对胰腺癌细胞系具有增强的活性
摘要:合成了一系列含磷酰胺的二苯基嘧啶类似物(pa-Dppys)作为有效的粘着斑激酶(fak)抑制剂.当浓度低于10.69 Nm时,Pa-Dppy衍生物可以显着抑制fak的酶活性.其中,化合物7A和7E是两种活性最强的fak抑制剂,Ic 50值分别为4.25 Nm和4.65 Nm.特别地,化合物7E还显示出对aspc细胞系的强活性,Ic 50为1.66μm,但显示出对正常hpde6-C7细胞的低活性(ic 50 > 20μm),表明其细胞毒性低.此外,流式细胞仪分析表明7E(8μm,72 H),Aspc和panc细胞的生长几乎都被抑制,细胞存活率分别为16.8%和18.1%.总体而言,化合物7E可用作治疗胰腺癌的有价值的fak抑制剂.
DOI:10.1016/j.Bmc.2017.09.041

专利信息

专利号:EP-1431274-B1
优先权日:2002-12-18
标题 :Synthesis of mono-N-substituted functionalized anilines
发明人：SELVA MAURIZIO; TUNDO PIETRO
权利人:CONSORZIO INTERUNIVERSITARIO N
摘要:The present invention relates to a process for direct and selective synthesis of mono-N-substituted functionalized anilines by using alkylating agents selected from the class of organic carbonates, preferably of the dialkyl, dibenzyl and diallyl types, in the presence of suitable catalysts that are chemically related to the class of aluminosilicates.

专利号:US-9505719-B2
优先权日:2010-06-30
标 题 :Synthesis and use of kinase inhibitors
发明人：LEI YIXIONG; BEHRENS CARL HENRY; LI HUI-YIN; SUN CONNIE L
权利人:VERASTEM INC
摘要:An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis.

专利号:CN-113185468-B
优先权日:2021-04-30
标题 :A kind of method of photocatalytic synthesis of quinazolinone

专利号:US-2004127747-A1
优先权日:2002-12-18
标题:Synthesis of mono-N-substituted functionalized anilines

专利号:EP-1431274-A1
优先权日:2002-12-18
标 题:Synthesis of mono-N-substituted functionalized anilines

专利号:CN-113698358-A
优先权日:2021-08-27
标 题 :A kind of method for visible light-induced synthesis of quinazolinone compounds