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2007 Fused pyrimidine derivatives R 0515 Synthesis and Regioselective N- and O-Alkylation of 1H- or 3H-[1,2,3]Triazo- lo[4,5-d]pyrimidine-5,7(4H,6H)-diones (8-Azaxanthines) and Transformation of Their 3-Alkyl Derivatives into 1-Alkyl Isomers. — The synthesis of various title compounds is described and their behavior under various alkylating conditions is in- vestigated in detail. Highlight of the findings is a transformation of 3-alkyl derivatives such as (VII) into the corresponding 1-alkyl isomer (IX). — (ISLAM, R.; NAGAMATSU*, T.; Synthesis 2006, 24, 4167-4179; Dep. Drug Discovery Dev., Grad. Sch. Med., Dent. Pharm. Sci., Okayama Univ., Tsushima, Okayama 700, Japan; Eng.) — Mais 17- 152

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Page 1: Synthesis and Regioselective N- and O-Alkylation of 1H- or 3H-[1,2,3]Triazolo[4,5-d]pyrimidine-5,7(4H,6H)-diones (8-Azaxanthines) and Transformation of Their 3-Alkyl Derivatives into

2007

Fused pyrimidine derivativesR 0515 Synthesis and Regioselective N- and O-Alkylation of 1H- or 3H-[1,2,3]Triazo-

lo[4,5-d]pyrimidine-5,7(4H,6H)-diones (8-Azaxanthines) and Transformation of Their 3-Alkyl Derivatives into 1-Alkyl Isomers. — The synthesis of various title compounds is described and their behavior under various alkylating conditions is in-vestigated in detail. Highlight of the findings is a transformation of 3-alkyl derivatives such as (VII) into the corresponding 1-alkyl isomer (IX). — (ISLAM, R.; NAGAMATSU*, T.; Synthesis 2006, 24, 4167-4179; Dep. Drug Discovery Dev., Grad. Sch. Med., Dent. Pharm. Sci., Okayama Univ., Tsushima, Okayama 700, Japan; Eng.) — Mais

17- 152

Page 2: Synthesis and Regioselective N- and O-Alkylation of 1H- or 3H-[1,2,3]Triazolo[4,5-d]pyrimidine-5,7(4H,6H)-diones (8-Azaxanthines) and Transformation of Their 3-Alkyl Derivatives into

2007