CAS: 1025504-45-3; Valbenazine

上下游产品

[2R-(2A,3B,11Bb)]-1,3,4,6,7,11B-六氢-9,10-二甲氧基-3-异丁基-2H-苯并[a]喹嗪-2-醇 (2R,3R,11Br)-Dihydrotetrabenazine 171598-74-6
9,10-二甲氧基-3-(2-甲基丙基)-2,3,4,6,7,11B-六氢-1H-吡啶并[2,1-A]异喹啉-2-醇 Dihydrotetrabenazine 3466-75-9
反式（2,3）-二氢四苯那嗪 S,S,S-Dhtbz 164104-49-8
(2S,3R,11Bs)-2-Hydroxy-3-Isobutyl-9,10-Dimethoxy-2,3,6,7-Tetrahydro-1H-Pyrido[2,1-A]Isoquinolin-4(11Bh)-One 1415385-79-3
丁苯那嗪 Tetrabenazine 58-46-8
(+)-丁苯那嗪 Tetrabenazine 1026016-83-0
3-异丁基-9,10-二甲氧基-1,3,4,6,7,11B-六氢-2H-吡啶并[2,1-A]异喹啉-2-酮 (3Rs,11Brs)-Tetrabenazine 718635-93-9

📜丁苯那嗪置于盐酸,4-二甲氨基吡啶,Sodium Tetrahydroborate,碳酸氢钠,溶剂黄146,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,Sodium Hydroxide体系中,用 1,4-二氧六环,甲醇,乙醇,二氯甲烷,甲基叔丁基醚,水 用作溶剂,化学反应 6.0H,反应生成缬苯那嗪
参考文献:通过开发新一代商业合成二甲苯磺酸伐苯那嗪来提高效率和可持续性
标题:通过开发新一代商业合成二甲苯磺酸伐苯那嗪来提高效率和可持续性
摘要:用于制造二甲苯磺酸伐苯那嗪(ingrezza 的 Api)的合成工艺已被证明具有高度选择性和稳健性,但通过缩短制造时间和减少总体工艺废物来简化工艺操作,实现更环保的化学性能和持续改进的机会仍然存在以及前三个最关键转型期间的环境足迹. Neurocrine 的下一代商业工艺的开发涵盖了制药绿色化学的原理( Org. Process Res. Dev. 2006,10,315−319),并采用了加速反应动力学,简化反应介质和消除不必要的后处理程序的策略,以实现更好的效果.流程效率和操作敏捷性.新的绿色工艺将制造时间缩短了 43%,材料使用量减少了 45%,同时将整体工艺产量提高了 5%,用水量减少了 32%,从而提高了效率和可持续性.
Doi:10.1021/acs.Oprd.4C00148

专利信息

专利号:US-2024239791-A1
优先权日:2021-04-26
标题 :Processes for the synthesis of valbenazine
发明人：TUCKER JOHN LLOYD
权利人:NEUROCRINE BIOSCIENCES INC
摘要:The present application relates to processes for preparing (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), which is an inhibitor of vesicular monoamine transporter 2 (VMAT2) useful in the treatment of hyperkinetic movement disorders such as tardive dyskinesia (TD).

专利号:US-2022363680-A1
优先权日:2019-09-13
标题 :Processes for the synthesis of valbenazine
发明人：TUCKER JOHN; KUCERA DAVID; HETTINGER DONALD; COCHRAN BRIAN M; BRANUM SHAWN; LE JACKIE; MCGEE KEVIN
权利人:NEUROCRINE BIOSCIENCES INC
摘要:The present application relates to processes for making (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b -hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl (S)-2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), which is an inhibitor of vesicular monoamine transporter 2 (VMAT2) useful in the treatment of hyperkinetic movement disorders such as tardive dyskinesia (TD).

专利号:US-2021087191-A1
优先权日:2020-12-04
标 题 :SUBSTITUTED 3-ISOBUTYL-9,10-DIMETHOXY-1,3,4,6,7,11B-HEXAHYDRO-2H-PYRIDO[2,1-a]ISOQUINOLIN-2-OL COMPOUNDS, THEIR SYNTHESIS, AND USE THEREOF
发明人：MILLER DAVE ALAN; ELLENBERGER DANIEL J; GUNIC ESMIR; GIRARDET JEAN-LUC; SPANGENBERG ANGELA
权利人:DISPERSOL TECHNOLOGIES LLC
摘要:The invention relates to substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds, their synthesis, pharmaceutical compositions containing them, and methods of using them in the treatment of disorders benefiting from inhibition of vesicular monoamine transporter 2 (VMAT2).

专利号:WO-2022232060-A1
优先权日:2021-04-26
标 题:Processes for the synthesis of valbenazine

专利号:EP-4330255-A1
优先权日:2021-04-26
标题 :Processes for the synthesis of valbenazine

专利号:WO-2021050977-A1
优先权日:2019-09-13
标 题 :Processes for the synthesis of valbenazine