CAS: 302964-08-5; 2-((6-Chloro-2-Methylpyrimidin-4-yl)Amino)-N-(2-Chloro-6-Methylphenyl)Thiazole-5-Carboxamide

相似化合物

302964-24-5 910297-51-7 302964-27-8

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N-(4-Methoxybenzyl)-2-(6-Chloro-2-Methylpyrimidin-4-Ylamino)-N-(2-Chloro-6-Methylphenyl)-1,3-Thiazole-5-Carboxamide置于三氟甲磺酸,三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 3.0H,以99%的收率获得产物n-(2-氯-6-甲基苯基)-2-[(6-氯-2-甲基-4-嘧啶基)氨基]-5-噻唑甲酰胺
参考文献:2-氨基噻唑作为新型激酶抑制剂模板.结构活性关系研究对发现n-(2-氯-6-甲基苯基)-2-[[[6-[4-(2-羟乙基)-1-哌嗪基)]-2-甲基-4-嘧啶基的发现氨基]]-1,3-噻唑-5-羧酰胺(dasatinib,Bms-354825)作为有效的pan-Src激酶抑制剂.
标题:2-氨基噻唑作为新型激酶抑制剂模板.结构活性关系研究对发现n-(2-氯-6-甲基苯基)-2-[[[6-[4-(2-羟乙基)-1-哌嗪基)]-2-甲基-4-嘧啶基的发现氨基]]-1,3-噻唑-5-羧酰胺(dasatinib,Bms-354825)作为有效的pan-Src激酶抑制剂.
摘要:通过筛选我们的内部化合物集合,发现了2-氨基噻唑(1)作为一种新型src家族激酶抑制剂模板.通过连续的结构-活性关系迭代进行的优化确定了类似物2(dasatinib,Bms-354825)和12M是在生化和细胞分析中具有纳摩尔至亚纳摩尔浓度的pan-Src抑制剂.分子模型被用来构建推定的结合模型,以抑制这类化合物对lck的抑制作用.该模型提出的关键氢键相互作用的框架与随后公布的与结构相似的abl激酶结合的2的晶体结构一致.此类抑制剂的口服药效为12M,可在小鼠体内体外抑制促炎细胞因子il-2(ed50约为5 Mg / Kg),并在急性小鼠炎症模型中降低tnf水平(lps抑制90%) Lps给药前2小时以60 Mg / Kg口服给药时,Tnf-α诱导的tnfα产生).当每天两次以0.3和3 Mg / Kg口服给药时,在已确诊疾病的大鼠的慢性佐剂性关节炎模型中进一步证明了12M的口服功效.达沙
DOI:10.1021/jm060727J

专利信息

专利号:US-9115124-B1
优先权日:2014-03-11
标题 :Process and intermediates for the preparation of dasatinib
发明人：BARUTO ALESSANDRO; GABOARDI MAURO; CASTALDI MARTA; CASTALDI GRAZIANO
权利人:CERBIOS PHARMA SA
摘要:The present invention relates to a process for the synthesis of dasatinib and to intermediates useful for its preparation.

专利号:WO-2011095125-A1
优先权日:2010-02-02
标 题:Synthesis methods and purification methods of dasatinib
发明人：YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG
权利人:NAN JING CAVENDISH BIO ENGINEERING TECHNOLOGY CO LTD; YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG
摘要:Synthesis methods of dasatinib are provided, which comprise the following steps: reacting a compound of formula I with a compound of formula II to obtain a compound of formula III, and then connecting the compound of formula III with 2-chloro-6-methylaniline and 1-(2-hydroxyethyl)piperazine in any order to give dasatinib. Furthermore, purification methods of dasatinib are also provided.

专利号:US-9108954-B2
优先权日:2010-02-02
标 题:Synthesis process of dasatinib and intermediate thereof
发明人：YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG
权利人:YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG; NAN JING CAVENDISH BIO ENGINEERING TECHNOLOGY CO LTD
摘要:Synthesis process of dasatinib is disclosed, which includes the step of reacting the compound of formula I with that of formula II to obtain the compound of formula III. Also disclosed is the compound of formula III which is used as an intermediate for synthesizing dasatinib. The substituents of R1, R2, R3 or R4 in formulae I, II or III are defined as in the description.

专利号:WO-2011095126-A1
优先权日:2010-02-02
标题:Synthesis process of dasatinib and intermediate thereof

专利号:US-2013030177-A1
优先权日:2010-02-02
标题:Synthesis process of dasatinib and intermediate thereof

专利号:EP-2532662-A1
优先权日:2010-02-02
标题 :Synthesis process of dasatinib and intermediate thereof