Pyrimido-1,4-diazepine誘導体の合成(第2報)5,6-Diamino-1,3-dimethyluracilとβ-ジカルボニル化合物との反応

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Four new pyrimido-1,4-diazepine derivatives, 2,4,6,8-tetramethyl-3H-pyrimido[4,5-b]-[1,4]diazepine-7,9(6H, 8H)-dione (IV), 2,4-diphenyl-6,8-dimethyl-3H-pyrimido[4,5-b][1,4]-diazepine-7,9(6H, 8H)-dione(VII), 4-phenyl-2,6,8-trimethyl-3H- pyrimido[4,5-b][1,4]-diazepine-7,9(6H, 8H)-dione(X), and 2-phenyl-4,6,8-trimethyl-3H-pyrimido[4,5-b][1,4]-diazepine-7,9(6H, 8H)-dione(XI), were synthesized. When 5,6-diamino-1,3-dimethyluracil(I) was heated in butanol with acetylacetone, dibenzoylmethane, or benzoylacetone, 4-(6-amino-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5-pyrimidylamino)-3-penten-2-one (III), 1,3-diphenyl-3-(6-amino-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5-pyrimidylamino)-2-propen-1-one(V), or 1-phenyl-3-(6-amino-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5-pyrimidylamino)-2-buten-1-one (IX) were obtained, respectively, under elimination of water. Heating of I with acetylacetone, dibenzoylmethane or benzoylacetone in polyphosphoric acid afforded IV, VII, or X, were and in the case of heating I with benzoylacetone, XI was obtained in a poor yield besides X. IV, VII, and X were also obtained by heating III, V, and IX in polyphosphoric acid.
公益社団法人日本薬学会の論文
1977-01-25