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The invention provides a synthetic method of (purin-6-yl)amino acids which a re useful as medicaments of anticancer, anti-virus agents and so on or their intermediates. Methyl (R, S)-3-[4-(9-benzylpurin-6-yl) phenyl]-2-[ (t- butoxycarbonyl) amino] propanoate is produced by making 9-benzyl-6-iodopurin e react with methyl (R, S)-2-[ (t-butoxycarbonyl) amino]-3-[4- (trimethylstananyl) phenyl] propionate in the presence of Pd2dba3, triphenylarsine and copper iodide.