secondary alkylamines with activemethylenecompounds afforded mono-sulfenylated compounds in good yields. The reactions of 2 mol of sulfenamides derived from imides with 1 mol of activemethylenecompounds in the presence of a base gave di-sulfenylated compounds. It was found that α-mono-sulfenylated ketones were prepared by the reactions of enamines with sulfenamides derived from imides. α-gem-Di-sulfenylated
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
The olefins which are vicinally substituted by amino and phenylthio groups showed the reactivity as an enamine in the reactions with heterocumulenes and in cycloadditions with a 1,3-dipole and a 2-propenimine, giving a pyrazole derivative and a pyridine derivative, respectively.
2-Alkyl-2-formyl-cyclopropane-1-carbonitriles 4, 5 and 4-formyl-2-haloalkanenitriles 3 were prepared from aliphatic enamines 1 and 2-haloacrylonitriles 2. Both stereoisomers of the cyclopropane derivatives were obtained stereoselectively using appropriate reaction conditions.
1,3-Dipolar Cycloaddition Reaction of Vinyl Azides with Enamines. Synthesis of Vinyltriazolines and Vinyltriazoles
作者:Yujiro Nomura、Yoshito Takeughi、Shuji Tomoda、Masato M. Ito
DOI:10.1246/bcsj.54.261
日期:1981.1
Reaction of α- and β-azidostyrene with enamines gave vinyltriazolines regioselectively in moderate yields. 1-Pyrrolidinyl enamines reacted with α-azidostyrene more readily than piperidino or morpholino enamines. β-Azidostyrene was as reactive as azidobenzene while α-azidostyrene was much less reactive. Vinyltriazolines formed from enamines of ketones were deaminated to yield the corresponding vinyltriazoles