4-氨基-2-三氟甲基苯甲腈置于4-甲基苯磺酸吡啶,二异丁基氢化铝体系中,用 四氢呋喃,正己烷,乙酸乙酯 作为反应溶剂,化学反应 2.25H,反应生成 3-三氟甲基-4-[(4-甲基哌嗪-1-基)甲基]苯胺 参考文献:Insights Into The Modular Design Of Kinase Inhibitors And Application To Abl And Axl 标题:Insights Into The Modular Design Of Kinase Inhibitors And Application To Abl And Axl 摘要:选择性分析和生物测试一个匹配的激酶抑制剂集合,导致鉴定出abl(野生型和t315I)和axl激酶的有效,选择性抑制剂. DOI:10.1039/d1Md00296A
专利号:US-2023183246-A1 优先权日:2020-05-19 标题 :Continuous flow sonogashira coupling synthesis method 发明人:THOMPSON DAVID HARLEY; SINTIM HERMAN O; QI QINGQING; BIYANI SHRUTI 权利人:PURDUE RESEARCH FOUNDATION 摘要:The present disclosure relates to a telescoped continuous flow Sonogashira coupling synthesis for some lead compounds to support in vivo studies and pre-clinical evaluation. The application of high throughput tools combined with the telescoped continuous synthesis method can enable an efficient and safe synthesis of compounds of interest involving hazardous coupling reagents such as HATU, while minimizing by-product formation.
专利号:US-2008096883-A1 优先权日:2004-08-11 标题 :Trifluoromethyl substituted benzamides as kinase inhibitors 发明人:CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO 权利人:CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO 摘要:The invention relates to trifluoromethyl substituted benzamide compounds of the formula (I), pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.
专利号:US-8030311-B2 优先权日:2005-04-14 标题:Phenylacetamides suitable as protein kinase inhibitors 发明人:BOLD GUIDO; FURET PASCAL; GUAGNANO VITO; MCCARTHY CLIVE; VAUPEL ANDREA 权利人:NOVARTIS AG 摘要:The invention relates to compounds of the formula (I) wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof, as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.
参考文献:10.1007/s00280-017-3240-x 摘要:Ye YE, Woodward CN, Narasimhan NI. Absorption, metabolism, and excretion of [14C]ponatinib after a single oral dose in humans. Cancer Chemotherapy and Pharmacology. 2017 Feb 09;79(3):507–18. doi: 10.1007/s00280-017-3240-x. 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2014).