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1.发明授权
公开(公告)号：EP2995614B1
公开(公告)日：2018-01-31
申请号：EP15186900.5
申请日：2011-06-10
发明人： GIGUERE, Joshua, R. , MCCARTHY, Keith, E. , REISCH, Helge, A. , SANDOVAL, Sergio , STYMIEST, Jake, L.
IPC分类号： C07D265/30 , C07D489/08 , C07C209/00 , C07C269/04
CPC分类号： C07D489/08 , B01J23/42 , B01J23/44 , B01J31/1855 , B01J31/20 , B01J31/2295 , B01J31/2414 , B01J2231/40 , B01J2531/64 , B01J2531/821 , B01J2531/824 , B01J2531/828 , B01J2531/847 , C07C209/00 , C07C209/44 , C07C269/04 , C07D265/30 , C07D295/03 , C07D295/205 , Y02P20/55 , C07C211/21 , C07C271/12
摘要： The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
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2.发明公开
公开(公告)号：EP3283490A1
公开(公告)日：2018-02-21
申请号：EP16709607.2
申请日：2016-03-09
发明人： HUNTLEY, C. Frederick M. , KATAISTO, Erik Wayne , REISCH, Helge Alfred , SHARMA, Archana , STYMIEST, Jake Larry
IPC分类号： C07D489/12 , A61K31/485 , A61P25/04
CPC分类号： A61K31/485 , A61P25/04 , C07B2200/13 , C07D489/12
摘要： The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.
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3.发明公开REDUCTION OF ALPHA, BETA-UNSATURATED KETONE LEVELS IN MORPHINAN DERIVATIVE COMPOSITIONS 审中-公开吗啡喃衍生物组合物中α，β-不饱和酮水平的还原
公开(公告)号：EP3166948A1
公开(公告)日：2017-05-17
申请号：EP15744360.7
申请日：2015-07-08
IPC分类号： C07D489/08 , A61K31/485 , A61P25/00 , A61P29/00
CPC分类号： C07D489/08 , A61K31/485 , A61K45/06 , C07B2200/13
摘要： The disclosure relates to processes for reducing the amount of a compound of formula (I) or a salt or a solvate thereof present in a composition comprising compounds of formulae (I) and (II) or a salt or a solvate thereof.
摘要翻译： 本公开涉及用于减少存在于包含式（I）和（II）的化合物或其盐或溶剂化物的组合物中的式（I）化合物或其盐或溶剂化物的量的方法。
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4.发明公开TRANSITION METAL-CATALYZED PROCESSES FOR THE PREPARATION OF N-ALLYL COMPOUNDS AND USE THEREOF 有权过渡金属PROCESS FOR PRODUCING N-烯丙基化合物及其用途
公开(公告)号：EP2995614A1
公开(公告)日：2016-03-16
申请号：EP15186900.5
申请日：2011-06-10
发明人： GIGUERE, Joshua, R. , MCCARTHY, Keith, E. , REISCH, Helge, A. , SANDOVAL, Sergio , STYMIEST, Jake, L.
IPC分类号： C07D265/30 , C07D489/08 , C07C209/00 , C07C269/04
CPC分类号： C07D489/08 , B01J23/42 , B01J23/44 , B01J31/1855 , B01J31/20 , B01J31/2295 , B01J31/2414 , B01J2231/40 , B01J2531/64 , B01J2531/821 , B01J2531/824 , B01J2531/828 , B01J2531/847 , C07C209/00 , C07C209/44 , C07C269/04 , C07D265/30 , C07D295/03 , C07D295/205 , Y02P20/55 , C07C211/21 , C07C271/12
摘要： The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
摘要翻译： 本公开提供了用于第三cardamines的N-脱烷基化和使用的过渡金属催化剂的制备叔N-烯丙基胺衍生物和它们的仲胺衍生物的方法。 第三cardamines可以是生物碱，更具体地，第三cardamines可以是阿片样物质。 在具体的实施方案中，本公开提供了在使用过程中用于从东罂粟碱纳洛酮和纳曲酮的合成方法。
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