Enantioselective Claisen Rearrangements: Development of a First Generation Asymmetric Acyl-Claisen Reaction
作者:Tehshik P. Yoon、David W. C. MacMillan
DOI:10.1021/ja015612d
日期:2001.3.1
The development of an enantioselective catalytic Claisenrearrangement remains an important yet elusive goal in chemical synthesis. With this objective in mind, we recently reported the acyl-Claisen rearrangement, a Lewis acid-catalyzed variant of the Bellus reaction that utilizes acid chlorides and allylic amines in the stereoselective synthesis of ɑ,β-disubstituted-y,δ-unsaturated carbonyls (eq 1)
Palladium-catalyzed coupling of organic halides and tertiary allylic amines
作者:Lucio Filippini、Marilena Gusmeroli、Raul Riva
DOI:10.1016/0040-4039(93)85030-z
日期:1993.3
The palladium-catalyzed reaction between aryl or perfluoro-alkyl iodides and tertiary allylicamines provides a practical route to 3-aryl- or 3-perfluoroalkyl-allylic amines. The outcome of the arylation of tertiary allylicamines can be affected by a change of solvent.
SUBSTITUTED INTERNAL VINYL-BORONIC ACIDS AND BORONIC ACID DERIVATIVES
申请人:Math Shivanand K.
公开号:US20120041193A1
公开(公告)日:2012-02-16
Disclosed herein are vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives useful as synthetic intermediates for the preparation of therapeutic agents. Also disclosed are methods of synthesis of vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives.
Pyrimido [4,5-D] Azepine Derivatives As 5-HT2C Agonists
申请人:Andrews Mark
公开号:US20100113422A1
公开(公告)日:2010-05-06
The present invention provides a compound of formula (I):
or a pharmaceutically acceptable salt thereof wherein the variables R
1
, R
2
, R
3a
, R
3b
, R
3b
, R
3d
, and R
100
are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a 5-HT
2c
receptor-mediated disorders with a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).
amination of olefins with secondary alkyl amines to afford allylic amines, eliminating the need for oxidants. This method is compatible with a broad scope of olefins and can be extended to achieve a site- and diastereoselective amination of terpenes. Mechanistic studies disclose that the reaction proceeds via a cobaloxime-promoted hydrogen atom transfer pathway to afford the product that results from cleavage