申请人:Fine Organics Limited
公开号:US05371247A1
公开(公告)日:1994-12-06
A potassium salt useful in the production of certain N-substituted alkyl or arylalkyl thionitroethenamines is produced by the reaction of the dipotassium salt of a 2-nitrodithio aliphatic acid such as 2-nitrodithio acetic acid with branched chain primary alkylamines, secondary alkylamines, arylalkylamines or heterocyclic alkylamines such as dimethylamine, pinacolylamine, benzylamine or piperonylamine, thereby converting one only of the KS-groups to an alkylamine group. The resulting monopotassium salt may be alkylated or arylalkylated to produce an N-substituted alkyl or arylalkyl thionitroethenamine. This compound may be reacted with a suitable amine to produce compounds containing the pharmaceutically active grouping --NHC(.dbd.CHNO.sub.2)NHX, wherein X represents an alkyl, arylalkyl or heterocyclic alkyl group.
通过将2-硝基二硫代醋酸的二钾盐与支链初级烷胺、次级烷胺、芳基烷胺或杂环烷胺(例如二甲胺、皮纳科利胺、苄胺或吡哆酰胺)反应,可以生产一种在生产某些N-取代烷基或芳基烷基硫代亚硝基乙烯胺时有用的钾盐,从而将KS基团之一转化为烷基胺基团。所得的单钾盐可以烷基化或芳基烷基化,以产生N-取代烷基或芳基烷基硫代亚硝基乙烯胺。此化合物可以与适当的胺反应,以产生含有药用活性基团--NHC(.dbd.CHNO.sub.2)NHX的化合物,其中X代表烷基、芳基烷基或杂环烷基。