CAS: 102429-07-2; 2-Bromo-1-(2,4-Difluorophenyl)Ethanone

相似化合物

56159-89-8 655-15-2 1555526-76-5

上下游产品

CAS号364-83-0 2,4-二氟苯乙酮 | CAS号372-18-9 1,3-二氟苯 | CAS号598-21-0 溴乙酰溴 | CAS号86404-63-9 2,4-二氟-α-(1H-1,... | CAS号71682-95-6 24-二氟苯甲酰乙腈 | CAS号122263-03-0 2-乙酰氧基-2’,4’-二氟苯乙酮 | CAS号887625-49-2 2,4-DIFLUOROPHE... | CAS号887625-50-5 2-BROMO-4-(2,4-...

2',4'-二氟苯乙酮置于氢溴酸,溴,溶剂黄146体系中,用 水 用作溶剂,以80%的收率获得2-溴-2',4'-二氟苯乙酮
参考文献:取代的4-苯基噻唑:开发有效和选择性的a1,A3和双重a1 / A3腺苷受体拮抗剂.
标题:取代的4-苯基噻唑:开发有效和选择性的a1,A3和双重a1 / A3腺苷受体拮抗剂.
摘要:腺苷通过四个不同的g蛋白偶联受体(称为a1,A2A,A2B和a3腺苷受体(ars))充当强大的信号分子.A2A和a2B Ars是gs偶联的,而a1和a3 Ars通过gi蛋白抑制camp的产生.A1和a3 Ars的拮抗剂可用于治疗(神经)炎性疾病,包括急性肾损伤和肾衰竭,肺部疾病和阿尔茨海默氏病.在本研究中,我们通过在n2和c5处引入取代基来获得包括双重靶标化合物的a1和a3 Ar拮抗剂,从而优化了通用的2-氨基-4-苯基噻唑支架.产生了具有(亚)纳摩尔效价的选择性a1拮抗剂,例如11和13.这些化合物显示,与人的a1 Ar相比,物种差异在大鼠处的效价明显更高,并且被表征为反向激动剂.制备了几种有效的和选择性的a3 Ar拮抗剂,例如7,8,17和22(人a3 Ar的ki值为5-9 Nm),它们在大鼠直系同源物上的效力要低得多.此外,开发了双重a1 / A3拮抗剂(10,18),显示ki值在8到42
Doi:10.1016/j.Ejmech.2019.111879

专利信息

专利号:US-8178672-B2
优先权日:2004-10-19
标 题:Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase
发明人：ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC
权利人:ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC; ARQULE INC
摘要:An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.

专利号:US-2009111985-A1
优先权日:2004-10-19
标 题 :Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 map kinase

专利号:JP-2012072177-A
优先权日:2004-10-19
标 题 :Synthesis of imidazooxazole and imidazothiazole inhibitors of P38 MAP kinase

专利号:US-8148370-B2
优先权日:2008-03-21
标题 :Polysubstituted derivatives of 2-aryl-6-phenyl-imidazo[1,2-a]pyridines, and preparation and therapeutic use thereof
发明人：DE PERETTI DANIELLE; EVANNO YANNICK
权利人:DE PERETTI DANIELLE; EVANNO YANNICK; SANOFI AVENTIS
摘要:Compounds of formula (I): n nwherein R 1 , R 2 , R 3 , R 4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

专利号:EP-2258704-A1
优先权日:2004-10-19
标题:Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 map kinase

专利号:JP-2008517064-A
优先权日:2004-10-19
标题:Synthesis of imidazooxazole and imidazothiazole inhibitors of P38 MAP kinase