Novel Enantioselective Fluorinating Agents, (R)- and (S)-N-Fluoro-3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-Dioxides

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概要

• 論文の詳細を見る

• Enantioselective fluorinating agents, (R)- and (S)-N-fluoro-3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]-thiazine 1,1-dioxides (BNBT-F, 2) are readily prepared in 3 steps from racemic 3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (5) via optical resolution and fluorination. These agents make accessible both enantiomers of optically active quaternary α-fluoro carbonyl compounds in modest to high enantioselectivities. X-ray crystallographic analysis of chiral 2 reveals a unique structure wherein the nitrogen atom is highly pyramidalized and fluorine occupies an axial position.

• 公益社団法人日本薬学会の論文
• 2000-12-01

著者

• 竹内 義雄

  富山大院医薬

• Shibata Norio

  Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University

• TAKEUCHI Yoshio

  Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University

• Shibata Norio

  Faculty Of Pharmaceutical Sciences Osaka University

• LIU Zhaopeng

  Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University

• Liu Zhaopeng

  Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University

• Shibata N

  National Inst. Infectious Diseases Tokyo Jpn

• Takeuchi Yoshio

  Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University

• Takeuchi Yoshio

  Faculty Of Pharmaceutical Sciences Toyama Medical & Pharmaceutical University

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