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916791-07-6 1082843-70-6 1206249-40-2欧盟法规
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2-hydroxy-5-bromopyrazine 4-(5-bromopyrazin-2-yl)morpholine 合成工艺路线路线简述
- 36070-80-1 = 912773-21-8
反应条件:1.1 Reagents: 1,3-Dibromo-5,5-Dimethylhydantoin,Pyridinium,1-Fluoro-2,4,6-Trimethyl-,Tetrafluoroborate(1-) (1:1) Catalysts: Tetrakis(Acetonitrile)Copper(1+) Tetrafluoroborate Solvents: Acetonitrile; 6 H,Rt1.2 Reagents: Tetrasodium Edta Solvents: Diethyl Ether,Pentane,Water; 15 Min,Rt
标题:Unified Approach To Decarboxylative Halogenation Of (Hetero)Aryl Carboxylic Acids
作者:Chen,Tiffany Q.; Pedersen,P. Scott; Dow,Nathan W.; Fayad,Remi; Hauke,Cory E.; Et Al
参考文献:Journal Of The American Chemical Society 日期:2022 卷标:144(18) 页码:8296-8305
5-氯吡嗪-2-羧酸置于tetrakis(Acetonitrile)Copper(I)Tetrafluoroborate,1,3-二溴-5,5-二甲基海因,1-Fluoro-2,4,6-Trimethylpyridin-1-Ium Tetrafluoroborate体系中,用 乙腈 作为反应溶剂,化学反应 6.0H,以51%的收率获得产物2-溴-5-氯吡嗪
参考文献:(杂)芳基羧酸脱羧卤化的统一方法
标题:(杂)芳基羧酸脱羧卤化的统一方法
摘要:芳基卤化物是合成化学中的基本基序,在金属介导的交叉偶联反应中起着关键作用,并在药物发现中充当重要的支架.尽管芳基羧酸的热脱羧官能化已得到广泛探索,但现有的卤代脱羧方法的范围仍然有限,并且目前不存在提供从芳基羧酸前体获得任何类型的芳基卤化物的统一策略.在此,我们报告了一种通过配体到金属电荷转移对(杂)芳基羧酸进行直接脱羧卤化的通用催化方法.该策略适用于极其广泛的底物范围.我们利用芳基自由基中间体实现不同的功能化途径:(1) 原子转移以获取溴代或碘代(杂)芳烃或(2)自由基被铜捕获并随后还原消除以反应生成氯代或氟代(杂)芳烃.所提出的配体到金属的电荷转移机制得到了一系列光谱研究的支持.
DOI:10.1021/jacs.2C02392
专利信息
专利号:US-2024239799-A1
优先权日:2021-04-02
标 题:(s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo [1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer
发明人:DI FABIO ROMANO; MONTALBETTI CHRISTIAN; PETROCCHI ALESSIA; GRILLO ALESSANDRO; RANDAZZO PIETRO; ROSSETTI ILARIA; CIAMMAICHELLA ALINA
权利人:C N C C S S C A R L COLLEZIONE NAZ DEI COMPOSTI CHIMICI E CENTRO SCREENING; IRBM S P A
摘要:The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-41H,6′H-spiro[piperidine-4,5′-pyrrolo[1,2-b]pyrazol]-41-amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.
专利号:US-9744173-B2
优先权日:2014-04-10
标题 :2-amino 6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides
发明人:BRODNEY MICHAEL AARON; BECK ELIZABETH MARY; BUTLER CHRISTOPHER RYAN; ZHANG LEI; O'NEILL BRIAN THOMAS; BARREIRO GABRIELA; LACHAPELLE ERIK ALPHIE; ROGERS BRUCE NELSEN
权利人:PFIZER
摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nand the variable R 1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:WO-2024068976-A1
优先权日:2022-09-29
标 题 :Azole derivatives as shp2 inhibitors
发明人:PETROCCHI ALESSIA; MONTALBETTI CHRISTIAN; DI FABIO ROMANO; CIAMMAICHELLA ALINA; ROSSETTI ILARIA
权利人:IRBM S P A; C N C C S S C A R L COLLEZIONE NAZ DEI COMPOSTI CHIMICI E CENTRO SCREENING
摘要:The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase. Compounds of the invention can be used for the treatment of disorders associated with SHP2 deregulation. The present invention also relates to pharmaceutical compositions containing said compounds and to their method of synthesis.
专利号:CN-215783303-U
优先权日:2021-06-09
标题 :A kind of chemical intermediate 2-bromo-5-chloropyrazine synthesis kettle device
专利号:WO-2023280237-A1
优先权日:2021-07-07
标题 :Synthesis and application of phosphatase degrader
专利号:CN-106632094-A
优先权日:2016-11-23
标题 :Synthesis method of 2-amino-3-chlorine-5-bromopyrazine