在 盐酸,水体系中,化学反应生成4,4-二氟环己甲酸 参考文献:Substituted Isoindolones And Their Use As Metabotropic Glutamate Receptor Potentiators 标题:Substituted Isoindolones And Their Use As Metabotropic Glutamate Receptor Potentiators 摘要:本发明涉及的是具有以下化学式i的化合物:其中r1,R2,R3,R4,R5,R6,R7,R8,R9和n的定义如描述中所定义的化合物.该发明还涉及制备这些化合物的过程,以及用于制备的新中间体,含有这些化合物的药物组合物,以及这些化合物在治疗中的使用.
专利号:WO-2008132128-A3 优先权日:2007-04-27 标 题:Synthesis of a pharmaceutically active compound 发明人:WIESENHOEFER WOLFGANG; BUYLE OLIVIER; CALLENS ROLAND; GIRE ROMAN; POUSSET CYRILLE; JEANNIN LAURENT 权利人:SOLVAY; WIESENHOEFER WOLFGANG; BUYLE OLIVIER; CALLENS ROLAND; GIRE ROMAN; POUSSET CYRILLE; JEANNIN LAURENT 摘要:Process for the manufacture of UK- 427,857 ( Maraviroc ) which comprises a step wherein enantiopure (S)-3-amino-3-phenylpropan-1-ol is manufactured from a mixture of its enantiomers by crystallizing or precipitating from a solution containing the mixture of enantiomers of 3-amino-3-phenylpropan-1-ol, an enantiopure resolving agent and a solvent, a diastereomeric salt or complex of 3-amino-3-phenylpropan-1-ol with the resolving agent, said salt or complex being enriched in the (S)-enantiomer of 3-amino-3-phenylpropan-1-ol. Difluorocyclohexan oic acid derivatives useful in the process can be obtained by a process comprising subjecting an oxocyclohexanoic acid ester to reaction with an activated fluorocarboxylic acid derivative and fluorinating the obtained intermediate to obtain a difluorocyclo hexanoic acid ester.
专利号:US-2022363662-A1 优先权日:2021-04-20 标题 :Compounds as lxr agonists 发明人:PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V 权利人:INTEGRAL BIOSCIENCES PRIVATED LTD 摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.
专利号:EP-2989099-A1 优先权日:2013-04-26 标题 :A process for the synthesis of maraviroc
专利号:WO-2008132128-A2 优先权日:2007-04-27 标 题 :Synthesis of a pharmaceutically active compound
专利号:WO-2014173375-A1 优先权日:2013-04-26 标题 :A process for the synthesis of maraviroc
专利号:RU-2727723-C1 优先权日:2016-09-29 标 题 :Method for synthesis of novel chiral ligand, metal chelate, various unnatural amino acids, maraviroc and main intermediate compounds thereof
参考标题:Design And Synthesis Of Novel Dasatinib Analogues 作者:G. Buchappa,K. Durgaprasad,B. Suneelkumar,P. Baby Rani,K. Ravi Babu,A.K.S. Bhujanga Rao,P. Aparna 摘要:Design, Synthesis, Characterization And In Vitro Biological Assay Of A Series Of Novel Carboxylic Acid And Amino Acid Analogs Of Dasatinib (1) As Anticancer Agents Are Reported. Some Of The Synthesized Analogs Were Identified As Potent Src/abl Kinase Inhibitors With Greater Antiproliferative Activity Against K652 And T315I Cancer Cell Lines. The Synthetic Process Involves Condensation Of N-(2-Chloro-6-Methylphenyl)-2-[[6-[4(-1-Pipearazinyl]-2-Methyl-4-Pyrimidinyl]Amino]-5-Thiazolecarboxamide With Carboxylic Acids In The Presence Of Dicyclohexylcarbodiimide And Oxyma In Organic Solvent Medium. Compounds Were Characterized And Tested For Anticancer Activity On Leukemia Cancer Cell Lines K562 And Baf3/t315. Analogues Of Lactic Acid, Mandalic Acid, Leucine And Proline Have Shown Promising Antiproliferative Activity Compared To Dasatinib.