抗腫瘍剤関連化合物の合成研究(第1報)Oxazolo[4,5-d]pyrimidine類ならびにPyrimido[5,4-b][1,4]oxazine類の合成研究
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概要
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The present work was undertaken in order to synthesize oxazolo[4,5-d]pyrimidines which are of interest as antimetabolites. The Schotten-Baumann reaction of 2,4-diamino-5-hydroxy-6-methylpyrimidine (III) with ethyl chlorocarbonate gave 2,4-diamino-5-ethoxycarbonyloxy-6-methylpyrimidine (XII). XII was refluxed in pyridine to give 5-amino-7-methyloxazolo[4,5-d]pyrimidin-2(3H)-one (XIII), which was alkylated with alkyl halide to give 3-alkyloxazolo[4,5-d]pyrimidine derivatives (XIVa-d). Also the Schotten-Baumann reaction of III with ethyl bromoacetate and ethyl α-bromopropionate gave pyrimido[5,4-b][1,4]oxazine derivatives (XV) and (XVII), respectively.
- 公益社団法人日本薬学会の論文
- 1973-06-25
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