CAS: 1152311-62-0; (R)-1-(2,2-Difluorobenzo[d][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl)-6-Fluoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)Cyclopropanecarboxamide

上下游产品

CAS号1294504-68-9 (R)-N-(1-(3-(be... | CAS号2369-13-3 3-氟-4-硝基苯胺 | CAS号33070-32-5 5-溴-2,2-二氟-1,3-苯并二恶唑 | CAS号656-46-2 2,2-二氟-1,3-苯并二恶... | CAS号72768-97-9 (2,2-二氟苯并[d][1,... | CAS号476473-97-9 5-(氯甲基)-2,2-二氟苯... | CAS号862574-87-6 1-(2,2-二氟苯并二氧代-... | CAS号952664-69-6 2-溴-5-氟-4-硝基苯胺 | CAS号1092536-54-3 (((2,2-二甲基-丁-3-...

📜在 氢气体系中,用 乙腈 用作溶剂,40.0~45.0 °C,400.01 Kpa 条件下,反应 4.0H,以96.1%的收率获得vx-661/vx6611-(2,2-二氟-1,3-苯并二氧戊环-5-基)-N-[1-[(2R)-2,3-二羟基丙基]-6-氟-2-(2-羟基-1,1-二甲基乙基)-1H-吲哚-5-基]-环丙烷甲酰胺
参考文献:一种5-取代环丙基甲酰氨基吲哚衍生物的制 备方法
标题:一种5-取代环丙基甲酰氨基吲哚衍生物的制 备方法
摘要:本发明提供一种5‑取代环丙基甲酰氨基吲哚衍生物的制备方法,具体指一种tezacaftor的制备方法.利用2‑硝基‑4‑氟‑5‑卤代苯乙腈为起始原料,经氨取代反应,酰胺化反应,脱水缩合反应,还原环合反应‑消除反应,开环取代反应和催化氢解反应得到tezacaftor.本发明的方法原料廉价易得,反应步骤短,制备方法简便安全,易于实现,成本低;本发明路线的设计充分结合了官能团反应的固有特性,确保每步单元反应活性适宜,选择性高,为产品的高收率和高纯度提供了本质上的保证;本发明路线原子经济性高,产物收率和纯度高,废酸废水产生量少,绿色环保,适合工业化生产.

专利信息

专利号:US-9376461-B2
优先权日:2011-06-06
标 题:Non-enzymatic synthesis of O-acetyl-ADP-ribose and analogues thereof
发明人：KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B
权利人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B; GLAXOSMITHKLINE LLC
摘要:Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2′- and 3′-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-11434242-B2
优先权日:2017-12-04
标题:Dopamine-b-hydroxylase inhibitors
发明人：KISS LASZLO ERNO; BELIAEV ALEXANDER; ROSSI TINO; PALMA PEDRO NUNO LEAL; SOARES DA SILVA PATRÃ?CIO MANUEL VIEIRA ARAUJO; PINTO RUI; CARDONA FRANCISCO
权利人:BIAL PORTELA & Cª S A; BIAL—PORTELA & CA S A
摘要:This invention relates to: (a) compounds of formula Ia (with R1, R4 to R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions (comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:EP-1836163-B1
优先权日:2004-12-23
标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin
发明人：BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER
权利人:NOVARTIS AG
摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.

专利号:US-2007179100-A1
优先权日:2003-04-09
标 题:Protected monomers
发明人：MANOHARAN MUTHIAH
权利人:MANOHARAN MUTHIAH
摘要:This invention relates to protected monomers for the synthesis of iRNA agents.

专利号:US-8829014-B2
优先权日:2006-04-07
标题 :Thiazole and thiophene analogues, and their use in treating autoimmune diseases and cancers
发明人：GIORDANO ANTHONY; VASU KAMALA K; THAKAR HARDIK M; GIRI RAJAN S; SUDARSANAM VASUDEVAN; YERANDE SWAPNIL G; INAMDAR GAJANAN S
权利人:GIORDANO ANTHONY; VASU KAMALA K; THAKAR HARDIK M; GIRI RAJAN S; SUDARSANAM VASUDEVAN; YERANDE SWAPNIL G; INAMDAR GAJANAN S; UNIV LOUISIANA STATE; PATEL PHARMACEUTICAL EDUCATION & RES DEV PERD CT B V
摘要:Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.