Synthesis of 1-[cis-2-Hydroxy-cis-3-(hydroxymethyl)-cyclobutyl]thymine,a Novel Method for the Synthesis of Cyclobutyl Nucleosides and Related Compounds |
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| Authors: | Tai-Shun Lin Mei-Zhen Luo Mao-Chin Liu |
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| Affiliation: | Department of Pharmacology and Comprehensive Cancer Center , Yale University School of Medicine , New Haven, Connecticut, 06510 |
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| Abstract: | Abstract Syntheses of 1-[cis-2-hydroxy-cis-3-(hydroxymethyl)cyclobutyl]thymine (1) and related compounds by a novel method are reported. Coupling of 3-benzyloxymethyl-l-cyclobutene (2) with silylated thymine in the presence of NIS, followed by treatment with DBU, basic hydrolysis and catalytic hydrogenation produced the target compound (1) and its isomer (12). |
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