CAS: 781649-09-0; N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-Oxo-1-(2,2,2-Trifluoroethyl)Azepan-3-Yl]-4-(2-Oxo-3H-Imidazo[4,5-B]Pyridin-1-yl)Piperidine-1-Carboxamide
该化合物是一种化学化合物,属于小分子类CGRP(与卡西通因基因有关的浸泡物)敌国,主要用于治疗偏头痛,其特点是它能够有选择地抑制CGRP受体,它在偏头痛的病理学中起着重要作用.该化合物的结构相对复杂,有多种功能组,有助于其药理活动.Telcagepant以其口服生物利用率为名,并研究其减少偏头痛袭击频率和严重程度的效果.其行动机制包括阻塞CGRP的血管血管效应,从而缓解偏头痛症状.尽管它在临床试验中显示出希望,但进一步发展已经停止,而且没有获准临床使用.
- 英文名称N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-Oxo-1-(2,2,2-Trifluoroethyl)Azepan-3-Yl]-4-(2-Oxo-3H-Imidazo[4,5-B]Pyridin-1-yl)Piperidine-1-Carboxamide
- 中文名称N-[(3R,6S)-6-(2,3-二氟苯基)六氢-2-氧代-1-(2,2,2-三氟乙基)-1H-氮杂卓-3-基]-4-(2,3-二氢-2-氧代-1H-咪唑并[4,5-b]吡啶-1-基)-1-哌啶甲酰胺
- IUPAC名称N-((3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl)-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide
- CAS编号781649-09-0
- MFCD编号:MFCD22741412
- FDA UNII编号:D42O649ALL
- 分子式:C26H27F5N6O3分子量:566.52
- 产品CID: 1776712
- 同类组份化合物CAS781649-09-0 (free base)953077-35-5 (potassium)
- 产品分类医药中间体 → 吡啶类化合物
物理性质
MSDS等安全信息
上下游产品
18H17F5N4O2C18H17F5N4O2 (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one 4-Nitrophenyl chloroformate 1,1'-carbonyldiimidazole合成工艺路线路线简述
📜4-(2-Oxo-2,3-Dihydroimidazo[4,5-B]Pyridin-1-yl)Piperidine-1-Carboxylic Acid Ethyl Ester置于盐酸,三乙胺体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 24.0H,反应生成 N-[(3R,6S)-6-(2,3-二氟苯基)六氢-2-氧代-1-(2,2,2-三氟乙基)-1H-氮杂卓-3-基]-4-(2,3-二氢-2-氧代-1H-咪唑并[4,5-B]吡啶-1-基)-1-哌啶甲酰胺
参考文献:Wo2007/120590
标题:Wo2007/120590
海关参考信息
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专利信息
专利号:WO-2010144293-A1
优先权日:2009-06-08
标 题 :Synthesis of telcagepant and intermediates thereof
发明人：XU FENG; DESMOND RICHARD; HOERRNER R SCOTT; HUMPHREY GUY R; ITOH TETSUJI; JOURNET MICHEL; YOSHIKAWA NAOKI; ZACUTO MICHAEL J
权利人:MERCK SHARP & DOHME; XU FENG; DESMOND RICHARD; HOERRNER R SCOTT; HUMPHREY GUY R; ITOH TETSUJI; JOURNET MICHEL; YOSHIKAWA NAOKI; ZACUTO MICHAEL J
摘要:Disclosed is an efficient synthesis for the manufacture of the caprolactam intermediate (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one: Formula and salts thereof, and an efficient preparation of telcagepant using the caprolactam intermediate.
专利号:US-9624478-B2
优先权日:2011-09-08
标题:Biocatalysts and methods for the synthesis of substituted lactams
发明人：CABIROL FABIEN LOUIS; CHEN HAIBIN; GOHEL ANUPAM; SALIM PAULINA ELENA; SMITH DEREK J; JANEY JACOB; KOSJEK BIRGIT; TANG WENG LIN; HSIEH HELEN; PHAM SON Q
权利人:CODEXIS INC
摘要:The present disclosure relates to transaminase polypeptides capable of aminating a dicarbonyl substrate, and polynucleotides, vectors, host cells, and methods of making and using the transaminase polypeptides.
专利号:US-2024208966-A1
优先权日:2021-04-13
标题 :Process for the synthesis of 1,3-dihydro-imidazo[4,5-b]pyridin-2-one and/or derivatives thereof
专利号:US-2023313155-A1
优先权日:2011-09-08
标题 :Biocatalysts and methods for the synthesis of substituted lactams
专利号:US-10858635-B2
优先权日:2011-09-08
标题 :Biocatalysts and methods for the synthesis of substituted lactams
专利号:US-11597918-B2
优先权日:2011-09-08
标题 :Biocatalysts and methods for the synthesis of substituted lactams
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📌 第三方产品分析报告
主要参考文献
1: Gottschalk PC. Telcagepant-almost gone, but not to be forgotten (invited editorial related to Ho et al., 2015). Cephalalgia. 2016 Feb;36(2):103-5. doi: 10.1177/0333102415584311. Epub 2015 May 5. doi: 10.1177/0333102415584308. Epub 2015 Apr 29. doi: 10.1212/WNL.0000000000000771. Epub 2014 Aug 8. doi: 10.1111/papr.12158. Epub 2013 Dec 30. doi: 10.1124/jpet.113.206458. Epub 2013 Aug 23. doi: 10.1177/0333102413494272. Epub 2013 Jun 24. doi: 10.3969/j.issn.1673-5374.2013.10.009.
8: Hopkins CR. ACS chemical neuroscience molecule spotlight on Telcagepant (MK-0974). ACS Chem Neurosci. 2011 Jul 20;2(7):334-5. doi: 10.1021/cn200059f. Review.
9: Chaitman BR, Ho AP, Behm MO, Rowe JF, Palcza JS, Laethem T, Heirman I, Panebianco DL, Kobalava Z, Martsevich SY, Free AL, Bittar N, Chrysant SG, Ho TW, Chodakewitz JA, Murphy MG, Blanchard RL. A randomized, placebo-controlled study of the effects of telcagepant on exercise time in patients with stable angina. Clin Pharmacol Ther. 2012 Mar;91(3):459-66. doi: 10.1038/clpt.2011.246. Epub 2012 Jan 25. doi: 10.1111/j.1526-4610.2011.02052.x. Epub 2012 Jan 6. doi: 10.1111/j.1526-4610.2011.01901.x. doi: 10.1111/j.1365-2125.2010.03869.x.
合成参考文献
参考文献:10.1186/s10194-021-01365-w
摘要:Wiggers A, Ashina H, Hadjikhani N, Sagare A, Zlokovic BV, Lauritzen M, Ashina M. Brain barriers and their potential role in migraine pathophysiology. The Journal of Headache and Pain. 2022 Jan 26;23(1):16. doi: 10.1186/s10194-021-01365-w.
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