含硫黄ピリミド[5,4-d]ピリミジン化合物の合成研究(第3報)Dipyridamoleの新合成法

概要

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Application of phosphorus pentachloride to 4,8-dihydroxy-2,6-dimercaptopyrimido-[5,4-d]pyrimidine (I) gave 4,8-dichloropyrimido[5,4-d]pyrimidine-2,6-disulfenyl dichloride (II) in a good yield, and application of piperidine to this chloride (II) afforded 4,8-dipiperidinopyrimido[5,4-d]pyrimidine-2,6-disulfenopiperidide (V). Oxidation of V with chlorine in 40%, acetic acid gave 4,8-dipiperidinopyrimido[5,4-d]pyrimidine-2,6-disulfonyl dichloride (VI) in a good yield. The reaction of this VI with diethanolamine at low temperature resulted in the formation of N, N, N', N'-tetrakis-(2-hydroxyethyl)-4,8-dipiperidinopyrimido[5,4-d]pyrimidine-2,6-disulfonamide (VIIa). Heating of VI and diethanolamine at 110 -120°for 72 hr resulted in the formation of dipyridamole (VIII) in a good yield.
公益社団法人日本薬学会の論文
1976-05-25