公开(公告)号：US06353100B1

公开(公告)日：2002-03-05

申请号：US09260143

申请日：1999-03-01

申请人： Rudolf P. M. Guit ,  Wim Buijs

发明人： Rudolf P. M. Guit ,  Wim Buijs

IPC分类号： C07D20100

CPC分类号： C07D201/08

摘要： Process for the preparation of &egr;-caprolactam, in which in a step (a) a compound with the general formula: O=CH—(CH2)4—C(O)—R  (1) in which R is —OH, —NH2 or O—R′, in which R′ is an organic group with 1 to 10 carbon atoms, is contacted with ammonia and hydrogen in a suitable solvent at elevated pressure in the presence of a hydrogenation catalyst to a mixture of primary amino compounds and &egr;-caprolactam, followed by a separate second step (b) in which the primary amino compounds are reacted to &egr;-caprolactam, wherein the solvent in step (a) is an aqueous medium, including water, the yield to &egr;-caprolactam in step (a) is more than 10%, calculated on the initial molar amount of the compound according to formula (1), that &egr;-caprolactam is separated from the aqueous mixture obtained in step (a) by extraction and that the aqueous mixture resulting from the extraction, containing the primary amino compounds, is used in step (b).

摘要翻译： 制备ε-己内酰胺的方法，其中在步骤（a）具有以下通式的化合物：其中R是-OH，-NH 2或O-R'，其中R'是有机基团，其中1至 10的碳原子在合适的溶剂中，在氢化催化剂的存在下，在氨基酸和ε-己内酰胺的混合物中，在合适的溶剂中与氨和氢接触，随后分开第二步（b），其中伯氨基 化合物与ε-己内酰胺反应，其中步骤（a）中的溶剂是水性介质，包括水，步骤（a）中ε-己内酰胺的收率大于10％，根据化合物的初始摩尔量计算 根据式（1），通过萃取将ε-己内酰胺与步骤（a）中获得的含水混合物分离，并且在步骤（b）中使用含有伯氨基化合物的萃取产生的含水混合物。

公开(公告)号：US06620945B2

公开(公告)日：2003-09-16

申请号：US10142339

申请日：2002-05-08

申请人： Toyokazu Haga ,  Akio Kayano ,  Manabu Sasyou ,  Shigeto Negi ,  Hiroyuki Naka ,  Hirofumi Noda ,  Ken-ichi Sakai

发明人： Toyokazu Haga ,  Akio Kayano ,  Manabu Sasyou ,  Shigeto Negi ,  Hiroyuki Naka ,  Hirofumi Noda ,  Ken-ichi Sakai

IPC分类号： C07D20100

CPC分类号： C07D401/04 ,  C07B2200/07 ,  C07D207/12 ,  C07D453/02 ,  C07D491/04

摘要： The present invention provides a process for producing optically active 3-hydroxy-4-methoxypyrrolidine, which is an intermediate for synthesizing a quinuclidine derivative useful as a squalene synthetase inhibitor, a salt thereof, or a hydrate thereof by subjecting a pyrrolidine derivative represented by the following formula (1-4): wherein R3a and R3b are different and each of R3a and R3b represents a hydrogen atom or a methyl group, to optical division purification by using an optically active dibenzoyltartaric acid derivative or the like.

摘要翻译： 本发明提供了一种光学活性3-羟基-4-甲氧基吡咯烷的制备方法，该方法是合成用作角鲨烯合成酶抑制剂的奎宁环衍生物，其盐或其水合物的中间体， 下式（1-4）：其中R3a和R3b不同，R3a和R3b各自表示氢原子或甲基，通过使用光学活性二苯甲酰基酒石酸衍生物等进行光学分裂纯化。