Necleosides. CXLIX. Novel and Practical Synthesis of α-Monofluoro- and α, α-Difluorothymidine (F-TDR and F_2-TDR)

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概要

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• Di-O-tert-butyldiphenylsilyl (BDPS)-thymidine (2) was converted to α-bromo-3', 5'-di-O-BDPS-thymidine (3) by photobromination. Crude 3 was hydrolyzed to the α-hydroxythymidine derivative 4 which was oxidized with MnO_2 to the 5-formyluracil nucleoside 5. Fluorination of 4 with diethylamino-sulfur trifluoride afforded the protected α-fluorothymidine 6. Similarly, 5 was converted into the α, α-difluorothymine nucleoside 7. These protected fluorothymidines (6 and 7) were deblocked by treatment with tetra-n-butylammonium fluoride to give α-fluorothymidine(8,F-TDR) and α, α-difluorothymidine (9,F_2-TDR).

• 公益社団法人日本薬学会の論文
• 1988-04-25

著者

• Watanabe Kyoichi

  Laboratory Of Organic Chemistry Sloan-kettering Institute For Cancer Research Memorial Sloan-ketteri

関連論文

• Necleosides. CXLIX. Novel and Practical Synthesis of α-Monofluoro- and α, α-Difluorothymidine (F-TDR and F_2-TDR)

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