Azaquinolizine類の合成研究(第2報) : 1,3,4,6,7,8,9,9a-Octahydro-2H-pyrido[1,2-a]pyrazineの新合成法

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Ethyl 2-piperidinecarboxylate was converted to the corresponding 1-cyanomethyl compound (I) by the strecker synthesis. I was reduced over Raney nickel catalyst at 130° at high pressure to 1,3,4,6,7,8,9,9a-octahydro-2H-pyrido [1,2-a] pyrazin-1 (9aH)-one (II). II was reduced to 1,3,4,6,7,8,9,9a-octahydro-2H-pyrido [1,2-a] pyrazine (III) with lithium aluminum hydride. The compound III was also prepared by another method according to the following process. 2-(Aminomethyl) pyridine was reacted with chloroacetyl chloride to give 2-(chloroacetamidomethyl) pyridine which was cyclized to the corresponding pyridinium salt (VI) by heating in alcoholic solution for 3 hr. The salt (VI) was then reduced over platinum oxide catalyst to 1,3,4,6,7,8,9,9a, -octahydro-2H-pyrido [1,2-a] pyrazin-3 (4H)-one (VII), which was reduced with lithium aluminium hydride to III.
公益社団法人日本薬学会の論文
1967-06-25