4-(3-吡啶基)-2-氯嘧啶置于ammonium Hydroxide体系中,用 水 作为反应溶剂,化学反应 16.0H,以87%的收率获得产物4-(3-吡啶基)-2-氨基嘧啶 参考文献: Benzimidazole Derivatives As Selective Proteine Kinase Inhibitors[fr] Dérivés De Benzimidazole à Utiliser En Tant Qu'Inhibiteurs Sélectifs De Protéine Kinase 标题: Benzimidazole Derivatives As Selective Proteine Kinase Inhibitors[fr] Dérivés De Benzimidazole à Utiliser En Tant Qu'Inhibiteurs Sélectifs De Protéine Kinase 摘要:本发明涉及式(I)的化合物或其药用可接受的盐.其中n,R1,R2,R3,R4,R5,A,Q和x如描述中所定义.这些化合物选择性地调节,调控和/或抑制信号传导,该信号传导由涉及多种人类和动物疾病的某些天然和/或突变的蛋白激酶介导,如细胞增殖,代谢,过敏和退行性疾病.更具体地说,这些化合物是有效且选择性的天然和/或突变的c-Kit抑制剂.
专利号:WO-2013035102-A1 优先权日:2011-09-05 标 题 :Processes for the preparation of imatinib base and intermediates thereof 发明人:KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD; KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 摘要:The invention relates to an improved process for the preparation of highly pure imatinib base (99.99% HPLC purity) of formula (I) and the pharmaceutically acceptable acid addition salts thereof. This invention also relates to processes for the preparation of the intermediates in the synthesis of imatinib base.
专利号:US-2023065387-A1 优先权日:2019-10-14 标题:Synthesis of tyrosine kinase inhibitors
专利号:CN-114315595-B 优先权日:2021-11-30 标题 :Preparation method of a carbon-supported iron-based catalyst and its application in the synthesis of anti-cancer inhibitor intermediates
专利号:US-10738028-B2 优先权日:2016-05-11 标题:Spiro three-membered ring, spiro five-membered ring peptide deformylase inhibitor and use thereof in antibacteria and anti-tumor 发明人:HU WENHAO; LV FENGPING; TANG YANG; LI ZIYAN; CHEN CHEN; WEI JIANHAI; DONG SUZHEN; QIAN YU 权利人:RUDONG RUIEN PHARMACEUTICAL TECH CO LTD 摘要:Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, can affect the energy balance of the cancer cells through inhibiting the peptide deformylase of the mitochondria in the cells, so that the mitochondrial membrane is depolarized, ATP is exhausted and cell apoptosis is promoted, and has good inhibitory activities on many cancer cell strains such as colorectal cancer, leukemia, lung cancer, gastric cancer, cervical cancer, breast cancer, prostatic cancer, liver cancer and osteosarcoma at relatively lower concentrations. The structure of exemplary invention spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitors are represented by one or more of:
专利号:WO-2021074138-A1 优先权日:2019-10-14 标题:Synthesis of 6-methyl-n1-(4-(pyridin-3-yl)pyrimidin-2-yl)benzene-1,3-diamine
专利号:EP-4045494-B1 优先权日:2019-10-14 标 题 :Synthesis of 6-methyl-n1-(4-(pyridin-3-yl)pyrimidin-2-yl)benzene-1,3-diamine 发明人:ABRAHAM RAJKUMAR GURUBATHAM; LIN XIANGLIANG 权利人:ESCO ASTER PTE LTD
摘要:Ramesh, S.; Cherkupally, P.; Govender, T.; Kruger, H. G.; de la Torre, B. G.; Albericio, F., Science of Synthesis Knowledge Updates, (2017) 1, 371. 摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 160. 摘要:Beingessner, R. L.; Longstreet, A. R.; McTeague, T. A.; Kelly, L. P.; Seo, H.; Tran, T. H.; Wicker, A. C.; Jamison, T. F., Science of Synthesis: Flow Chemistry in Organic Synthesis, (2018) 1, 433. 摘要:Ley, S. V.; Browne, D. L.; OʼBrien, M., Science of Synthesis: Flow Chemistry in Organic Synthesis, (2018) 1, 296. 摘要:Solorio-Alvarado, C. R., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) .