2 - Amino - 6 - Alkoxy Purine Synthesis

2-amino-6-alkoxy-purine is an important intermediate of nucleotide.Guanine was acetylated as the origination raw material to synthesize the N²,9-diacetyl -guanine, the yield is 95.2%. Then from chlorized, hydrolysed to give 2-amino-6-chloropurine, the yield is 84.2%. From alkoxy reaction to synthesize 2-amino-6-methoxyl-purine, 2-amino-6-ethoxyl-purine ,2-amino-6-iso-propyloxyl-purine and 2-amino-6-tri-flouethoxyl-purine. we study each compound's synthesis craftwork route, the optimized factors of 2-amino-6-methoxyl-purine were: n(2-amino-6- chloride):n(NaOCH3)=1:5, solvent is CH3OH , refluxing for 10h, the yield is 89.1%; the optimized factors of 2-amino-6-ethoxyl-purine were n(2-amino -6- chloride):n(NaOCH₃):=1:3, solvent is CH-3CH₂OH , refluxing for 12h, the yield is 68.5%; the optimized factors of 2-amino-6-iso-propy-loxyl-purine were n(2-amino-6-chloride):n(NaOCH(CH3)2)-1:4, solvent is DMF, refluxing for 13h, the yield is 54%; the optimized factors of 2-amino-6- tri-flouethoxyl -purine were: in the condition of absolutely anhydrous ,solvent is dimethy suloxide (DMSO), catalyst is CuI, reaction temperature is 160°C , n(2-amino-6-chlorid e):n(NaOCH₂CF-3)=1 :5, m(DMSO):m(2-amino-6-chloride)= 1:13, n(CuI): n(2-amino-6-chloride)= 1:2, the ratio of yield is 83.2 %.