Asymmetric Iodolactamization Induced by Chiral Oxazolidine Auxiliary
摘要:
Asymmetric iodolactamization reactions of unsaturated amides with oxazolidines as the chiral auxiliaries were investigated. With (4S)-4-((2R)-2-butyl)-2,2-dimethyloxazolidine as the auxiliary and LiH as the base, a number of unsaturated amides underwent iodolactamization smoothly to afford the corresponding gamma- and delta-lactams in 30-98% yield with de values up to 97%.
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
Copper(II) Carboxylate-Promoted Intramolecular Carboamination of Alkenes for the Synthesis of Polycyclic Lactams
作者:Peter H. Fuller、Sherry R. Chemler
DOI:10.1021/ol702401w
日期:2007.12.1
intramolecular carboamination reactions of variously substituted gamma-alkenyl amides have been investigated. These oxidative cyclization reactions efficiently provide polycyclic lactams, useful intermediates in nitrogen heterocycle synthesis, in good to excellent yields. The efficiency of the carboamination process is dependent upon the structure of the amide backbone as well as the nitrogen substituent.
已经研究了羧酸铜 (II) 促进的各种取代 γ-烯基酰胺的分子内碳胺化反应。这些氧化环化反应有效地提供了多环内酰胺,它是氮杂环合成中有用的中间体,产率很高。碳胺化过程的效率取决于酰胺主链的结构以及氮取代基。
Sulfamides as gamma-secretase inhibitors
申请人:——
公开号:US20040049038A1
公开(公告)日:2004-03-11
Novel sulfamides of formula (1) are disclosed. The compounds exert an inhibitory action on the processing of APP by gamma-secretase, and are therefore useful in the treatment or prevention of Alzheimer's disease.