CAS: 1360828-80-3; (1R,2R)-1-Amino-2-(Difluoromethyl)-N-(1-Methylcyclopropylsulfonyl)Cyclopropanecarboxamide Hcl

相似化合物

630421-48-6 1360997-58-5 630421-49-7

在 2,6-二甲基吡啶,盐酸,4-二甲氨基吡啶,Potassium Dihydrogenphosphate,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate,Lithium Hydroxide,[双(2-甲氧基乙基)胺]三氟化硫体系中,用 四氢呋喃,氘代氯仿,乙醇,正庚烷,二氯甲烷,醋酸异丙酯,水,异丙醇,乙腈 用作溶剂,化学反应 66.0H,反应生成(1R,2R)-1-氨基-2-(二氟甲基)-N-[(1-甲基环丙基)磺酰基]环丙烷甲酰胺盐酸盐
参考文献:通过环复分解开发格列卡韦的赋能途径
标题:通过环复分解开发格列卡韦的赋能途径
摘要:Glecaprevir被鉴定为有效的hcv Ns3 / 4A蛋白酶抑制剂,需要进行有效的合成以支持临床前评估和随后的i期临床试验.通过进一步发展药物化学途径,确立了格列卡韦的赋能途径.合成中的关键步骤涉及闭环复分解(rcm)反应以形成18元大环,而挑战性的氟化步骤则是形成关键氨基酸.该成功途径已成功用于生产41千克格列卡韦韦,足以支持临床前评估和早期临床开发.
Doi:10.1021/acs.Oprd.9B00469

专利信息

专利号:US-9440991-B2
优先权日:2013-12-23
标 题:Synthesis of an antiviral compound
发明人：CAGULADA AMY; CHAN JOHANN; CHAN LINA; COLBY DENISE A; KARKI KAPIL KUMAR; KATO DARRYL; KEATON KATIE ANN; KONDAPALLY SUDHA; LEVINS CHRIS; LITTKE ADAM; MARTINEZ RUBEN; PCION DOMINIKA; REYNOLDS TROY; ROSS BRUCE; SANGI MICHAEL; SCHRIER ADAM J; SENG PAMELA; SIEGEL DUSTIN; SHAPIRO NATHAN; TANG DONALD; TAYLOR JAMES G; TRIPP JONATHAN; WALTMAN ANDREW W; YU LAWRENCE
权利人:GILEAD SCIENCES INC
摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

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专利号:US-2015175626-A1
优先权日:2013-12-23
标 题 :Synthesis of an antiviral compound