1246213-45-5 = 873054-44-5 反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water; 5 H,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2 - 3,Rt 标题:Breaking And Making Of Rings: A Method For The Preparation Of 4-Quinolone-3-Carb-Oxylic Acid Amides And The Expensive Drug Ivacaftor 作者:Vasudevan,N.; Jachak,Gorakhnath R.; Reddy,D. Srinivasa 参考文献:European Journal Of Organic Chemistry 日期:2015 卷标:2015(34) 页码:7433-7437]
13721-01-2 + 873055-58-4 = 873054-44-5 反应条件:1.1 Reagents: Triethylamine,1-Hydroxybenzotriazole,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt 标题:An Efficient Synthesis Of Ivacaftor 作者:Zhang,Rui; Han,Guanyu; Jiang,Luobin; Shen,Yao; Yang,Rui; Et Al 参考文献:Journal Of Heterocyclic Chemistry 日期:2017 卷标:54(6) 页码:3169-3173]
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-2023002411-A1 优先权日:2019-12-20 标 题:Deuterated analogues of selenophenochromenes, synthesis thereof, and methods of using same agents 发明人:ARSENJANS PAVELS 权利人:LATVIAN INST ORGANIC SYNTHESIS 摘要:The present invention relates to a novel cancer curing deuterated selenopheno [h] chromene derivatives, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of cancer by administration of such substances.
专利号:US-12252473-B2 优先权日:2022-04-18 标 题:Preparation methods of quinolone compounds and intermediates thereof 发明人:LEI JIE; CHEN ZHONGZHU; XU ZHIGANG; TANG DIANYONG; XU JIAYU; ZHOU HAOYI; XIA DANDAN; LIU YAO; CAO YIHUA; LUO JIE 权利人:UNIV CHONGQING ARTS & SCIENCES 摘要:The present application relates to processes for the preparation of quinolone compounds and intermediates thereof, particularly to processes for the preparation of quinolones and pharmaceutical intermediates of the quinolones. In particular, the present application provides a process for the preparation of a compound of Formula I, and a process for the synthesis of quinolone compounds using the compound of Formula I as an intermediate. The process for the preparation of the compound of Formula I comprises the steps of:reacting a compound of Formula A with R5NH2 and R6Cl in the presence of a base to form the compound of Formula I,
专利号:WO-2017208253-A9 优先权日:2016-05-30 标 题:An improved process for the synthesis of ivacaftor
专利号:US-2018127373-A1 优先权日:2015-05-12 标题:Process for the synthesis of ivacaftor and related compounds
1: Hoy SM. Elexacaftor/Ivacaftor/Tezacaftor: First Approval. Drugs. 2019 Dec;79(18):2001-2007. doi: 10.1007/s40265-019-01233-7. Review. doi: 10.18773/austprescr.2019.060. Epub 2019 Sep 13. Review. 3: Lumacaftor/ivacaftor for cystic fibrosis. Aust Prescr. 2019 Oct;42(5):170-171. doi: 10.18773/austprescr.2019.058. Epub 2019 Sep 13. Review. 4: Lommatzsch ST, Taylor-Cousar JL. The combination of tezacaftor and ivacaftor in the treatment of patients with cystic fibrosis: clinical evidence and future prospects in cystic fibrosis therapy. Ther Adv Respir Dis. 2019 Jan-Dec;13:1753466619844424. doi: 10.1177/1753466619844424. Review.
合成参考文献
参考文献:10.1007/s00109-011-0787-6 摘要:Rowe SM, Sloane P, Tang LP, Backer K, Mazur M, Buckley-Lanier J, Nudelman I, Belakhov V, Bebok Z, Schwiebert E, Baasov T, Bedwell DM. Suppression of CFTR premature termination codons and rescue of CFTR protein and function by the synthetic aminoglycoside NB54. Journal of Molecular Medicine. 2011 Jul 22;89(11):1149. doi: 10.1007/s00109-011-0787-6.