CAS: 1374248-77-7; (S)-N-((3S,5S,6R)-6-Methyl-2-Oxo-5-Phenyl-1-(2,2,2-Trifluoroethyl)Piperidin-3-yl)-2'-Oxo-1',2',5,7-Tetrahydrospiro[cyclopenta[b]Pyridine-6,3'-Pyrrolo[2,3-B]Pyridine]-3-Carboxamide

上下游产品

(S)-1'-(Tert-Butyl)-2'-Oxo-1',2',5,7-Tetrahydrospiro[cyclopenta[b]Pyridine-6,3'-Pyrrolo[2,3-B]Pyridine]-3-Carboxylic Acid 1455358-16-3
(6S)-2'-Oxo-1',2',5,7-Tetrahydrospiro[cyclopenta[b]Pyridine-6,3'-Pyrrolo[2,3-B]Pyridine]-3-Carboxylic Acid 1375541-21-1
Methyl (6S)-2'-Oxo-1'-{[2-(Trimethylsilyl)Ethoxy]Methyl}-1',2',5,7-Tetrahydrospiro[cyclopenta[b]Pyridine-6,3'-Pyrrolo[2,3-B]Pyridine]-3-Carboxylate 1375542-65-6
(3'S)-3-氯-1'-(1,1-二甲基乙基)-5,7-二氢螺[6H-环戊[b]吡啶-6,3'-[3H]吡咯并[2,3-B]吡啶]-2'(1'H)-酮 (S)-1'-(Tert-Butyl)-3-Chloro-5,7-Dihydrospiro[cyclopenta[b]Pyridine-6,3'-Pyrrolo[2,3-B]Pyridin]-2'(1'H)-One 1455358-14-1
(6S)-3-Amino-5,7-Dihydrospiro[cyclopenta[b]Pyridine-6,3'-Pyrrolo[2,3-B]Pyridin]-2'(1'H)-One 1059186-43-4
1-(Tert-Butyl)-3-((5-Chloro-3-(((Tetrahydro-2H-Pyran-2-yl)Oxy)Methyl)Pyridin-2-yl)Methyl)-1,3-Dihydro-2H-Pyrrolo[2,3-B]Pyridin-2-One 1456804-09-3
1-(Tert-Butyl)-3-((5-Chloro-3-(Chloromethyl)Pyridin-2-yl)Methyl)-1H-Pyrrolo[2,3-B]Pyridin-2(3H)-One 1455358-12-9
1-(Tert-Butyl)-3-((5-Chloro-3-(Hydroxymethyl)Pyridin-2-yl)Methyl)-1H-Pyrrolo[2,3-B]Pyridin-2(3H)-One 1455358-11-8 Tert-Butyl [(3S,5S,6R)-5-(3-Chlorophenyl)-6-Methyl-2-Oxo-1-(2,2,2-Trifluoroethyl)Piperidin-3-Yl]Carbamate 1375477-14-7 Methyl 1-Tert-Butyl-2-Oxo-1H,2H,3H-Pyrrolo[2,3-B]Pyridine-3-Carboxylate 1455358-36-7

4-溴苯基丙酮置于盐酸,Potassium Phosphate,2-羟基吡啶-N-氧化物,Palladium On Activated Charcoal,磷酸吡哆醛,Transaminase Ata-426,Potassium Formate,Potassium Carbonate,Caesium Carbonate,异丙胺,Sodium Hydroxide,Lithium Tert-Butoxide体系中,用 四氢呋喃,甲醇,甲基叔丁基醚,醋酸异丙酯,水,二甲基亚砜,N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应生成乌布吉泮
参考文献:Ubrogepant. Calcitonin Gene-Related Peptide (Cgrp) Receptor Antagonist,Treatment Of Migraine
标题:Ubrogepant. Calcitonin Gene-Related Peptide (Cgrp) Receptor Antagonist,Treatment Of Migraine
摘要:Migraineis Ranked As The Sixth Cause Of Years Lost Due To Disability,With Around 1.04 Billion Migraine Sufferers Globally. Triptans Are Considered The Standard For Acute Migraine Treatment,But An Important Number Of Migraineurs Do Not Respond To Them And These Drugs Are Contraindicated In Patients With Cardiovascular Disease. Migraine Therapy Is Currently Undergoing Tremendous Development,I.E.,5-Ht1F Receptor Agonists (Ditans),Anti-Calcitonin Gene-Related Peptide (Cgrp) Monoclonal Antibodies,And Small-Molecule Cgrp Receptor Antagonists (Gepants). Ubrogepant (Mk-1620) Is A Small-Molecule,Potent And Selective Cgrp Receptor Antagonist. In Two Phase Iii Clinical Trials (Achieve I And Ii),Ubrogepant Showed,At 2 Hours,Significant Percentages Of Pain Freedom,And Absence Of The Most Bothersome Symptoms In Migraine Patients. In A Phase Iii Study To Assess The Long-Term (52-Week) Safety And Tolerability,Ubrogepant Displayed Good Tolerability,And No Signs Of Hepatic Toxicity. In March 2019,The U.S. Food And Drug Administration Accepted The New Drug Application (Nda) For Ubrogepant For The Acute Treatment Of Migraine.
Doi:10.1358/dof.2019.44.11.3035581

专利信息

专利号:US-2025188502-A1
优先权日:2022-03-10
标 题 :Biocatalyst and method for the synthesis of ubrogepant intermediates
发明人：CHEN HAIBIN; HU HU; CAI BAOQIN; XU JUNPENG; LIU SITONG; JIN LUPING; WU XINWEI; CUI QINYAN; ZHANG CHENGXIAO; ZHU KAILONG
权利人:ENZYMASTER NINGBO BIO ENG CO LTD
摘要:This application provides engineered transaminase polypeptides for the synthesis of Ubrogepant intermediates with high stereoselectivity, high catalytic activity and good stability. This application also provides a reaction process for the asymmetric synthesis of Ubrogepant intermediates using the transaminase polypeptide.

专利号:WO-2023169184-A1
优先权日:2022-03-10
标 题:Biocatalyst and method for the synthesis of ubrogepant intermediates

专利号:CN-117425728-A
优先权日:2022-03-10
标 题 :Biocatalysts and methods for the synthesis of Ubujipan intermediates

专利号:CN-119020312-A
优先权日:2024-09-09
标题 :Novel aminotransferase and application thereof in synthesis of zimetapam

专利号:CN-118834160-A
优先权日:2023-04-23
标 题:Asymmetric synthesis of key chiral lactam intermediates and their derivatives of Ubrelvy

专利号:EP-4490281-A1
优先权日:2022-03-10
标 题:Biocatalyst and method for the synthesis of ubrogepant intermediates