Longobardi M, Bondavalli F, Ranise A, Schenone P
Farmaco Sci. 1979 Nov;34(11):952-9.
By reaction of secondary amines with 3-hydroxymethylene-exo-5,6-trimethylenenorbornan-2-one, synthesized from exo-5,6-trimethylenenorbornan-2-one and sodium/ethyl formate, a series of N,N-disubstituted 3-aminomethylene-exo-5,6-trimethylenenorbornan-2-ones has been obtained. These compounds gave N,N-disubstituted 3-aminomethyl-exo-5,6-trimethylenenorbornan-2-ones by LiAlH4 or catalytic reduction. Starting from the same alpha-hydroxymethyleneketone, pyrazole derivatives (V) and (VI) have been also synthesized; the former showed anticonvulsant activity in mice.
通过仲胺与由外向-5,6-亚甲基降冰片烷-2-酮和甲酸钠合成的3-羟基亚甲基外向-5,6-亚甲基降冰片烷-2-酮反应，得到了一系列N,N-二取代的3-氨基亚甲基外向-5,6-亚甲基降冰片烷-2-酮。这些化合物通过LiAlH4或催化还原得到N,N-二取代的3-氨基甲基外向-5,6-亚甲基降冰片烷-2-酮。从相同的α-羟基亚甲基酮出发，还合成了吡唑衍生物(V)和(VI)；前者在小鼠中显示出抗惊厥活性。
