硫脲置于n-溴代丁二酰亚胺(Nbs)体系中,用 1,4-二氧六环,水 用作溶剂,化学反应 5.0H,以94.9%的收率获得2-氨基-N-(2-氯-6-甲基苯基)噻唑-5-甲酰胺 参考文献: Process For Preparing 2-Aminothiazole-5-Aromatic Carboxamides As Kinase Inhibitors[fr] Procede De Preparation De Carboxamides 2-Aminothiazole-5-Aromatiques Utiles Comme Inhibiteurs De Kinases 标题: Process For Preparing 2-Aminothiazole-5-Aromatic Carboxamides As Kinase Inhibitors[fr] Procede De Preparation De Carboxamides 2-Aminothiazole-5-Aromatiques Utiles Comme Inhibiteurs De Kinases
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
参考标题:Design And Synthesis Of Novel Dasatinib Analogues 作者:G. Buchappa,K. Durgaprasad,B. Suneelkumar,P. Baby Rani,K. Ravi Babu,A.K.S. Bhujanga Rao,P. Aparna 摘要:Design, Synthesis, Characterization And In Vitro Biological Assay Of A Series Of Novel Carboxylic Acid And Amino Acid Analogs Of Dasatinib (1) As Anticancer Agents Are Reported. Some Of The Synthesized Analogs Were Identified As Potent Src/abl Kinase Inhibitors With Greater Antiproliferative Activity Against K652 And T315I Cancer Cell Lines. The Synthetic Process Involves Condensation Of N-(2-Chloro-6-Methylphenyl)-2-[[6-[4(-1-Pipearazinyl]-2-Methyl-4-Pyrimidinyl]Amino]-5-Thiazolecarboxamide With Carboxylic Acids In The Presence Of Dicyclohexylcarbodiimide And Oxyma In Organic Solvent Medium. Compounds Were Characterized And Tested For Anticancer Activity On Leukemia Cancer Cell Lines K562 And Baf3/t315. Analogues Of Lactic Acid, Mandalic Acid, Leucine And Proline Have Shown Promising Antiproliferative Activity Compared To Dasatinib.