公开(公告)号：US20160090356A1

公开(公告)日：2016-03-31

申请号：US14959416

申请日：2015-12-04

申请人： AMPAC Fine Chemicals LLC

发明人： Aslam MALIK ,  Francis HEMPENSTALL ,  Nicholas DUDA ,  Ali SULEMAN

IPC分类号： C07D211/34 ,  B01J19/24

CPC分类号： C07D211/34 ,  A61K31/4458 ,  B01J19/24 ,  B01J2219/00051 ,  B01J2219/24

摘要： Novel methods and systems for producing a substantially pure d-threo stereoisomer of methylphenidate or a salt thereof are provided. In particular, methods and systems for producing d-threo-methylphenidate hydrochloride in pure stereoisomeric form from d-threo-ritalinic acid hydrochloride using diazomethane are described. The described methods can be performed on a large scale, and thus provide d-threo methylphenidate or a salt thereof, and particularly the hydrochloride salt of d-threo-methylphenidate, in stereoisomerically pure form and in large quantities from a single batch reaction. Also described are novel compositions of d-threo methylphenidate hydrochloride.

摘要翻译： 提供了用于制备哌甲酯或其盐的基本上纯的二 - 苏式立体异构体的新方法和系统。 具体地说，描述了使用重氮甲烷从d-苏雷酸（盐酸）盐酸盐制备纯立体异构体形式的盐酸三 - 甲酯的方法和系统。 所描述的方法可以大规模进行，从而提供立体异构纯的形式的d-苏雷哌甲酯或其盐，特别是d-苏 - 哌甲酯的盐酸盐，并且大量来自单批次反应。 还描述了d-苏式哌甲酯盐酸盐的新型组合物。

公开(公告)号：US20150259289A1

公开(公告)日：2015-09-17

申请号：US14204257

申请日：2014-03-11

申请人： AMPAC Fine Chemicals LLC

发明人： Aslam MALIK ,  Francis HEMPENSTALL ,  Nicholas DUDA ,  Ali SULEMAN

IPC分类号： C07D211/34 ,  A61K31/4458

CPC分类号： C07D211/34 ,  A61K31/4458 ,  B01J19/24 ,  B01J2219/00051 ,  B01J2219/24

摘要： Novel methods and systems for producing a substantially pure d-threo stereoisomer of methylphenidate or a salt thereof are provided. In particular, methods and systems for producing d-threo-methylphenidate hydrochloride in pure stereoisomeric form from d-threo-ritalinic acid hydrochloride using diazomethane are described. The described methods can be performed on a large scale, and thus provide d-threo methylphenidate or a salt thereof, and particularly the hydrochloride salt of d-threo-methylphenidate, in stereoisomerically pure form and in large quantities from a single batch reaction. Also described are novel compositions of d-threo methylphenidate hydrochloride.

摘要翻译： 提供了用于制备哌甲酯或其盐的基本上纯的二 - 苏式立体异构体的新方法和系统。 具体地说，描述了使用重氮甲烷从d-苏雷酸（盐酸）盐酸盐制备纯立体异构体形式的盐酸三 - 甲酯的方法和系统。 所描述的方法可以大规模进行，从而提供立体异构纯的形式的d-苏雷哌甲酯或其盐，特别是d-苏 - 哌甲酯的盐酸盐，并且大量来自单批次反应。 还描述了d-苏式哌甲酯盐酸盐的新型组合物。

公开(公告)号：US20140350283A1

公开(公告)日：2014-11-27

申请号：US13902296

申请日：2013-05-24

申请人： AMPAC Fine Chemicals LLC

发明人： Brian MORGAN ,  Olivier DAPREMONT ,  Patrick BERGET ,  Ali SULEMAN ,  William DUBAY ,  Jeffrey D. BUTLER

IPC分类号： C07C253/30 ,  C07C215/54 ,  C07C213/02 ,  C07C255/36 ,  C07C255/37

CPC分类号： C07C253/30 ,  C07B2200/07 ,  C07B2200/09 ,  C07C213/02 ,  C07C215/54 ,  C07C255/36 ,  C07C255/37

摘要： Compounds and methods for preparing substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds from an isomerically pure starting material are described. In particular, methods of preparing a 3-(1-(dimethylamino)-2-methylpentane-3-yl)phenol as a substantially optically pure (R,R) stereoisomer are described. Using a method of the present invention, only the (R,R) and (S,S) stereoisomers of the target compound are produced, increasing the yield and stereoselectivity of the desired (R,R) stereoisomer.

摘要翻译： 描述了由异构纯的起始原料制备取代的3-（1-氨基-2-甲基戊烷-3-基）苯基化合物的化合物和方法。 特别地，描述了制备作为基本上光学纯的（R，R）立体异构体的3-（1-（二甲基氨基）-2-甲基戊烷-3-基）苯酚的方法。 使用本发明的方法，仅产生目标化合物的（R，R）和（S，S）立体异构体，从而提高所需（R，R）立体异构体的产率和立体选择性。