Synthesis of perhydro-N-(2,2-disubstituted-3-aminopropyl) heterocycles as potentially bioactive compounds and fragments for combinatorial chemistry

Abstract

A new method for the preparation of perhydro-­N-(2,2-disubstituted-3-aminopropyl) heterocycles that allows to obtain a large variety of corresponding derivatives with high to moderate yields using simple procedures is described.

Synthesis of 5-oxoalkane-2,2,3,3-tetracarbonitriles

“…The alkylation of CH acidic compounds is commonly carried out by treatment with alkyl halides in the presence of bases such as sodium hydroxide [12], potassium hydroxide [13], sodium methoxide [14,15], sodium hydride [16], cesium carbonate [17], and triethylamine [18]. In addition, procedures have been reported for the methylation of cyanomethylene [19] and dicyanomethylene fragment [20][21][22][23] in dimethyl sulfoxide (DMSO) in the presence of potassium carbonate or sodium hydride [24][25][26].…”