Synthetic Versatility of<i>N</i>-(Silylmethyl)imines: Water-Induced Generation of<i>N</i>-Protonated Azomethine Ylides of Nonstabilized Type and Fluoride-Induced Generation of 2-Azaallyl Anions
N-(Silylmethyl)imines generateN-protonatedazomethineylides of nonstabilized type when treated with water in HMPA, which undergo stereospecific and regioselectivecycloadditions with electron-poo...
Transmetallation of n-(trialkylstannyl)methylimines. A new method for the generation and cycloaddition of 2-azaallyl anions.
作者:William H. Pearson、Daniel P. Szura、William G. Harter
DOI:10.1016/s0040-4039(00)80203-8
日期:1988.1
Transmetallation of imines 1 at −78° with RLi provided 2-azaallylanions 2, which readily undergo cycloaddition with olefinic anionophiles, providing pyrrolidines. Of particular note is the generation of unstabilized 2-azaallylanions for the first time (Table 1, entries 1–3).
The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.