Ermili A, Mazzei M, Roma G, Cuttica A, Passerini N
Farmaco Sci. 1975 Nov;30(11):870-83.
Reaction of N,N-dialkylethoxycarbonylacetamides with substituted beta-naphthols in 3 or 6 or 7 positions with halogen, alkyl, methoxycarbonyl, methoxyl, ethoxyl in the presence of phosphorus oxychloride, led to the formation of 1-oxo-3-dialkylamino-1H-naphtho[2,1-b]pyrans bearing substituents in 5 or 8 or 9 positions, respectively. Moreover, on account of the chemical nature of such substituents, suitable chemical transformations of these compounds afforded some other 1H-naphtho[2,1-b]pyran derivatives. Pharmacological tests showed that anticonvulsant activity was improved by introduction of methoxy or ethoxy group in 9 position of several 1-oxo-3-dialkylamino-1H-naphtho[2,1-b]pyrans.
在三氯氧磷存在下，N,N - 二烷基乙氧羰基乙酰胺与在3、6或7位带有卤素、烷基、甲氧基羰基、甲氧基、乙氧基的取代β - 萘酚反应，分别生成在5、8或9位带有取代基的1 - 氧代 - 3 - 二烷基氨基 - 1H - 萘并[2,1 - b]吡喃。此外，由于这些取代基的化学性质，对这些化合物进行适当的化学转化可得到一些其他的1H - 萘并[2,1 - b]吡喃衍生物。药理试验表明，在几种1 - 氧代 - 3 - 二烷基氨基 - 1H - 萘并[2,1 - b]吡喃的9位引入甲氧基或乙氧基可提高其抗惊厥活性。
