专利号:US-2023399302-A1 优先权日:2020-10-29 标题:Process for the preparation of heteroaryl-substituted sulfur(vi) compounds 发明人:LOPCHUK JUSTIN M; SHULTZ ZACHARY P; SCATTOLIN THOMAS 权利人:H LEE MOFFITT CANCER CT & RES 摘要:The present disclosure provides processes for the synthesis of organic compounds, in particular processes for the synthesis of heteroaryl-substituted sulfur(VI) compounds by nucleophilic aromatic substitution.
专利号:US-6608199-B2 优先权日:2000-07-07 标题 :Synthesis of chlorinated pyrimidines 发明人:DOYLE TIMOTHY JOHN; BENKE ALAN HENRY; WEHRENBERG PETER KARL; NADY LOUIE AKOS 权利人:SYNGENTA LTD 摘要:The invention provides a process for synthesizing chlorinated pyrimidines. The process includes reacting imidoyl chloride compounds with phosgene (COCl2). The imidoyl chloride compounds can be supplied as starting materials or can be produced by reacting organic amides with phosgene or reacting organic nitrites with hydrogen chloride. The chlorinated pyrimidines, such as 4,6-dichloropyrimidine, can be used to synthesize other compounds useful in a variety of compositions, such as fungicides, pesticides, and pharmaceuticals.
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:US-6982331-B2 优先权日:2001-06-08 标 题 :Synthesis of chlorinated pyrimidines 发明人:DOYLE TIMOTHY J; BENKE ALAN H; WEHRENBERG PETER K; NADY LOUIE A; RODRIGUEZ GILBERT 权利人:SYNGENTA CROP PROT INC 摘要:The invention provides a process for synthesizing chlorinated pyrimidines. The process includes reacting imidoyl chloride compounds with phosgene (COCl 2 ). The imidoyl chloride compounds can be supplied as starting materials or can be produced by reacting organic amides with phosgene or reacting organic nitrites with hydrogen chloride. Phosgene may be replaced by equivalent reagents. The chlorinated pyrimidines, such as 4,6-dichloropyrimidine, can be used to synthesize other compounds useful in a variety of compositions, such as fungicides, pesticides, and pharmaceuticals.
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.
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.
合成参考文献
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