New Positive allosteric modulators of nicotinic acetylcholine receptor
申请人:Eskildsen Jørgen
公开号:US20130012530A1
公开(公告)日:2013-01-10
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.
Highly Enantioselective Borane Reduction of Heteroaryl and Heterocyclic Ketoxime Ethers Catalyzed by Novel Spiroborate Ester Derived from Diphenylvalinol: Application to the Synthesis of Nicotine Analogues
作者:Kun Huang、Francisco G. Merced、Margarita Ortiz-Marciales、Héctor J. Meléndez、Wildeliz Correa、Melvin De Jesús
DOI:10.1021/jo800204n
日期:2008.6.1
An asymmetric synthesis for the preparation of nonracemic amines bearing heterocyclic and heteroaromatic rings is described. A variety of important enantiopure thionyl and arylalkyl primary amines were afforded by the borane-mediated enantioselective reduction of O-benzyl ketoximes using 10% of catalyst 10 derived from (S)-diphenylvalinol and ethylene glycol with excellent enantioselectivity, in up
描述了制备带有杂环和杂芳环的非外消旋胺的不对称合成。使用 10%衍生自 ( S )-二苯基缬氨醇和乙二醇的催化剂10 ,通过硼烷介导的对映选择性还原O-苄基酮肟,得到各种重要的对映纯亚硫酰基和芳烷基伯胺,具有优异的对映选择性,高达 99% ee 。首次不对称还原 3- 和 4-吡啶基衍生的O-苄基酮肟醚的最佳条件是在 10 °C 下在二恶烷中使用 30% 的催化负载量实现的。( S ) -N-乙基降烟碱 ( 3 ) 也由 TIPS 保护的 ( S )-2-氨基-2-吡啶乙醇在 97% ee 中成功合成。
NEW POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTOR
申请人:H. Lundbeck A/S
公开号:US20140044806A1
公开(公告)日:2014-02-13
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.
Positive allosteric modulators of nicotinic acetylcholine receptor
申请人:H. Lundbeck A/S
公开号:US09050327B2
公开(公告)日:2015-06-09
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.