专利号:US-11274081-B2 优先权日:2016-05-30 标 题:Process for the synthesis of ivacaftor 发明人:REDDY DUMBALA SRINIVASA; KULKARNI AMOL ARVIND; NATARAJAN VASUDEVAN; SHARMA MRITYUNJAY KESHAVPRASAD 权利人:COUNCIL SCIENT IND RES 摘要:The present disclosed an improved process for the synthesis of ivacaftor starting from indole acetic acid ester which can be performed in batch as well as continuous flow synthesis. The present invention further disclosed to a continuous process for the synthesis of compound of formula (II) or formula (III) from compound of formula (I) in continuous flow reactor.
专利号:US-10336703-B2 优先权日:2015-05-12 标题 :Process for the synthesis of ivacaftor and related compounds 发明人:REDDY DUMBALA SRINIVASA; NATARAJAN VASUDEVAN; JACHAK GORAKHNATH RAJARAM 权利人:COUNCIL SCIENT IND RES 摘要:The present patent discloses a novel one pot two-step process for the synthesis of ivacaftor and related compounds of [Formula (I)], wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and Ar 1 are as described above; its tautomers or pharmaceutically acceptable salts thereof starting from indole acetic acid amides.
专利号:US-6465653-B2 优先权日:1998-09-29 标题:Noncatalyzed synthesis of 4-hydroxyquinolines and/or tautomers thereof 发明人:DANG TAUN-PHAT; ROUSTAN ALAIN 权利人:RHODIA CHIMIE SA 摘要:The 4-hydroxyquinoline compounds and/or tautomers thereof, notably 4-hydroxy-5,7-dichchloroquinoline, are synthesized in very high yields by hydrolyzing/decarboxylating a 4-hydroxyquinolinecarboxylic acid ester in the presence of water, whether in liquid or vapor state, but in the absence of any catalyst for such reaction(s).
专利号:US-2010273787-A1 优先权日:2007-11-15 标题:Kynurenine-aminotransferase inhibitors 发明人:SCHWARCZ ROBERT; KAJII YASUSHI; ONO SHIN-ICHIRO 权利人:SCHWARCZ ROBERT; KAJII YASUSHI; ONO SHIN-ICHIRO 摘要:Compounds of formula (I): prodrug derivatives and/or pharmaceutically acceptable salt thereof, selectively inhibit the enzyme kynurenine aminotransferase, thereby reducing the synthesis of kynurenic acid. The compounds are used for the treatment of psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as schizophrenia, depression, bipolar illness, anxiety and Alzheimer's disease. Furthermore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly. Additionally, the compounds of the invention are also useful for treatment of patients suffering from malaria by preventing parasite gametogenesis and fertility based on reduction of xanthurenic acid formation from its bioprecursor 3-hydroxy kynurenine.
专利号:US-2018127373-A1 优先权日:2015-05-12 标题:Process for the synthesis of ivacaftor and related compounds
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