专利号:US-9518014-B2 优先权日:2012-07-20 标 题:Process for synthesis of ezetimibe and intermediates used in said process 发明人:DING KUILING; WANG XIAOMING; WANG ZHENG 权利人:SHANGHAI INST ORGANIC CHEMISTRY CAS 摘要:A process for the production of ezetimibe and intermediates used in said process are disclosed. A kind of Morita-Baylis-Hillman adduct can be altered to chiral carboxylic acid derivatives of β-arylamino α-methylene with high activity and selectivity by means of ally lamination reaction, and the above carboxylic acid derivatives of β-arylamino α-methylene can be altered to the chiral intermediates of ezetimibe by means of simple conversion and further synthesized into the chiral drug ezetimibe. The synthesis route introduces chirality through the use of a chiral catalysis method, thereby avoiding the use of the chiral auxiliary oxazolidinone; and the route is economical and eco-friendly.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:WO-2024163852-A1 优先权日:2023-02-03 标题:Histidine kinase inhibitors as antibacterial agents 发明人:CARLSON ERIN ELIZABETH; GOSWAMI MANIBARSHA; ESPINASSE ADELINE; JI YINDUO 权利人:UNIV MINNESOTA 摘要:The invention provides maleimide derivative compounds of Formula I, as histidine kinase inhibitors, useful for inhibiting bacterial histidine kinases, such as HK853 and AirS, for treating S. aureus bacterial infections, in particular methicillin-resistant S. aureus (MRSA). The invention further provides methods of treating bacterial infection with the. compounds of Formula I, either used alone or in combination with other agents in a therapeutic regimen. Further disclosed is the synthesis of the compounds of Formula I.
专利号:US-2015166479-A1 优先权日:2012-07-20 标 题 :Process for synthesis of ezetimibe and intermediates used in said process
专利号:CN-109678806-A 优先权日:2018-12-24 标题 :A kind of efficient monomethylation synthesis method of aromatic primary amine
专利号:US-6207836-B1 优先权日:1993-02-17 标 题 :Indolin-2-one derivatives 发明人:ESAKI TORU; EMURA TAKASHI; HOSHINO EIICHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:A compound represented by formula (I):wherein R1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, -OR5, -SR5 or -NR6R7 (wherein R5, R6, and R7 each represent a lower alkyl group, etc.); X and Y each represent -CH2-, -NH- or -O-; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.
[参考文献]: M G Boersma, Et Al. Role Of Cytochromes P-450 And Flavin-Containing Monooxygenase In The Biotransformation Of 4-Fluoro-N-Methylaniline. Drug Metab Dispos. 1993 Mar-Apr;21(2):218-30.
合成参考文献
摘要:Ipaktschi, J.; Saidi, M. R., Science of Synthesis Knowledge Updates, (2012) 4, 441. 摘要:Zhang, H.; Liu, C.; Lei, A., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 164.