Ermili A, Balbi A, Di Braccio M, Roma G
Farmaco Sci. 1977 Oct;32(10):713-24.
Under suitable conditions the reaction of phenol and N,N-dialkylethoxycarbonylacetamides, in the presence of phosphorus oxychloride, resulted in the formation of 2-dialkylaminochromones. In a similar manner, variously substituted phenols afforded 2-dialkylaminochromones with substituents in different positions of the benzene ring. Pharmacological screening of all these compounds showed that they markedly affect the CNS, activity being mainly excitatory. Decreased activity was shown by compounds with particular substituents in the positions 6,7,8 among which two products [(V e) - K 12440, (V s) - K 12420] have weak but clear anticonvulsant effect.
在合适的条件下，苯酚与N,N - 二烷基乙氧羰基乙酰胺在三氯氧磷存在下反应，生成2 - 二烷基氨基色酮。以类似的方式，各种取代苯酚在苯环不同位置带有取代基的情况下生成2 - 二烷基氨基色酮。对所有这些化合物的药理筛选表明，它们对中枢神经系统有显著影响，活性主要为兴奋性。在6、7、8位带有特定取代基的化合物活性降低，其中两种产物[（V e）- K 12440，（V s）- K 12420]具有微弱但明显的抗惊厥作用。
