Balbi A, Roma G, Di Braccio M, Ermili A
Farmaco Sci. 1978 Nov;33(11):807-21.
When reaction of N,N-dialkyl-alpha-ethoxycarbonyl-alpha-alkylacetamides with beta-naphthol in the presence of phosphorus oxychloride was carried out in chlorobenzene at reflux, formation of 1-oxo-2-alkyl-3-dialkyl-amino-1H-naphtho[2,1-b]pyrans was achieved together with some other products whose structure was defined. Moreover, substitution of the 2 position of 1-oxo-3-dialkylamino-1H"naphtho[2,1-b]pyrans with chlorine or cyano group as well as the preparation of 1-thio-3-dialkylamino-1H-naphtho[2,1-b]pyrans was obtained by suitable chemical methods. Pharmacological screening of these compounds showed the lack of psychotropic activity of the corresponding 1-oxo-3-dialkylamino-1H-naphtho[2,1-b]pyrans.
当在氯苯中回流条件下，使N,N - 二烷基 -α- 乙氧羰基 -α- 烷基乙酰胺与β-萘酚在三氯氧磷存在下发生反应时，除了确定结构的其他一些产物外，还生成了1 - 氧代 - 2 - 烷基 - 3 - 二烷基氨基 - 1H - 萘并[2,1 - b]吡喃。此外，通过适当的化学方法实现了用氯或氰基取代1 - 氧代 - 3 - 二烷基氨基 - 1H - 萘并[2,1 - b]吡喃的2位，以及制备1 - 硫代 - 3 - 二烷基氨基 - 1H - 萘并[2,1 - b]吡喃。对这些化合物的药理筛选表明，相应的1 - 氧代 - 3 - 二烷基氨基 - 1H - 萘并[2,1 - b]吡喃缺乏精神活性。
