含硫黄ピリミド[5,4-d]ピリミジン化合物の合成研究(第2報)2-メチルスルホニルピリミド[5,4-d]ピリミジン-6-スルホンアミド誘導体の合成と転位反応

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In order to examine the relation between the structure and the activity of coronary vasodilation and inhibition of platelet aggregation, 9 kinds of 2-methylsulfonylpyrimido-[5,4-d]pyrimidine derivatives possessing a sulfonamide group at 6-position were synthesized. Reaction of N, N-bis(2-hydroxyethyl)-2-methylsulfonyl-4,8-dipiperidinopyrimido-[5,4-d]pyrimidine-6-sulfonamide (Va) with an excess of sodium hydroxide solution or an excess of diethanolamine at low temperature gave 6-[2-(2-hydroxyethylamino)ethoxy]-2-methylsulfonyl-4,8-dipiperidinopyrimido[5,4-d]pyrimidine (VIIa) in a quantitative yield. When a mixture of Va and triethylamine was refluxed in butanol, 6-[bis(2-hydroxyethyl)-amino]-2-methylsulfonyl-4,8-dipiperidinopyrimido[5,4-d]pyrimidine (IXa) was obtained in a good yield, and IXa was obtained by heating VIIa in butanol. Analogous sulfonamide derivatives (Vb, c, j) also underwent a similar reaction.
公益社団法人日本薬学会の論文
1976-05-25