(purin-6-yl) amino acid and production method thereof

C - Chemistry – Metallurgy – 07 – D

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C07D 473/32 (2006.01) A61K 31/52 (2006.01) C07D 473/00 (2006.01)

Patent

CA 2507893

The invention provides a synthetic method of (purin-6-yl)amino acids which are 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-iodopurine react with methyl (R, S)-2-[ (t-butoxycarbonyl) amino]-3-[4- (trimethylstananyl) phenyl] propionate in the presence of Pd2dba3, triphenylarsine and copper iodide.

L'invention concerne un procédé de synthèse d'acides (purin-6-yl) aminés servant de médicaments dans le traitement du cancer, d'agents antiviraux etc., ainsi que leurs intermédiaires. Selon l'invention, du propanoate de méthyl (R, S)-3-[4-(9-benzylpurin-6-yl) phényl]-2-[(t-butoxycarbonyl) amino] est produit par réaction de 9-benzyl-6-iodopurine avec du propionate de méthyl (R, S)-2-[(t-butoxycarbonyl) amino]-3-[4-(triméthylstananyl) phényl] en présence de Pd¿2?dba¿3?, de triphénylarsine et d'iodure de cuivre.

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