专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-8058477-B2 优先权日:2006-03-21 标 题 :Process for the synthesis of arylamines from the reaction of an aromatic compound with ammonia or a metal amide 发明人:HARTWIG JOHN F; SHEN QILONG 权利人:HARTWIG JOHN F; SHEN QILONG; UNIV YALE 摘要:A catalytic process for the synthesis of aromatic primary amines, reagent compositions for effecting the process, and transition metal complexes useful in the process, are provided.
专利号:US-6500954-B1 优先权日:1998-06-22 标 题:Synthesis of 5- or 8-bromoisoquinoline derivatives 发明人:GOULIAEV ALEX HAAHR; HANSEN WILLIAM 权利人:NEUROSEARCH AS 摘要:The present invention is directed to a method of preparing bromoisoquinoline derivatives, in particular 5- or 8-bromoisoquinoline derivatives. Bromoisoquinoline derivatives, and in particular 5-bromoisoquinoline and 5-bromo-8-nitroisoquinoline derivatives, are key intermediates in the synthesis of pharmaceutical compounds.
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-10125226-B2 优先权日:2013-06-05 标 题 :Scale-up process of bifunctionalized triblock copolymers with secondary and tertiary amines, with application in dewatering and desalting of heavy crude oils 发明人:FLORES SANDOVAL CESAR ANDRES; FLORES OROPEZA EUGENIO ALEJANDRO; LOPEZ ORTEGA ALFONSO; HERNANDEZ CORTEZ JOSE GONZALO; ESTRADA BUENDIA ARISTEO; CASTRO SOTELO LAURA VERONICA; REYES MARTINEZ REYNA; ALVAREZ RAMIREZ FERNANDO; ESTRADA MARTINEZ ARQUIMEDES; VAZQUEZ MORENO FLAVIO SALVADOR 权利人:MEXICANO INST PETROL 摘要:A chemical synthesis process is provided for the functionalization of monodispersed triblock copolymer (POEw-POPy-POEw) with secondary or tertiary amines at a semi-industrial level in glass reactors having a capacity between 1 L and 100 L. The process includes two stages where the first stage uses an alkylsulfonyl or arylsulfonyl chloride to obtain better leaving groups, and the second stage is the nucleophilic substitution with secondary or tertiary amines, to obtain the bifunctionalized triblock copolymers. The main advantage for this process is to reduce the quantity of unitary process done in each stage, the optimization of reaction times, and the stoichiometric relationships.
专利号:US-2009234126-A1 优先权日:2006-03-21 标 题:Process for the Synthesis of Arylamines from the Reaction of an Aromatic Compound with Ammonia or a Metal Amide
[参考文献]: Qilong Shen, Et Al. Palladium-Catalyzed Coupling Of Ammonia And Lithium Amide With Aryl Halides. J Am Chem Soc. 2006 Aug 9;128(31):10028-9.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 355. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 289. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 293. 摘要:Shaabani, A.; Sarvary, A.; Shaabani, S., Science of Synthesis: Multicomponent Reactions, (2013) 2, 103. 摘要:Molander, G. A.; Ryu, D., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 61.