Concise Synthesis of the Anti-HIV Nucleoside EFdA
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概要
- 論文の詳細を見る
EFdA (4'-ethynyl-2-fluoro-2'-deoxyadenosine), a nucleoside reverse transcriptase inhibitor with extremely potent anti-HIV activity, was concisely synthesized from (R)-glyceraldehyde acetonide in an 18% overall yield by a 12-step sequence involving highly diastereoselective ethynylation of an α-alkoxy ketone intermediate. The present synthesis is superior, both in overall yield and in the number of steps, to the previous one which required 18 steps from an expensive starting material and resulted in a modest overall yield of 2.5%.
- 2012-06-23
著者
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Kuwahara Shigefumi
Laboratory Of Agricultural Chemicals Faculty Of Agriculture Ibaraki University
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Yoshida Mayumi
Laboratory Of Animal Biotechnology Interdisciplinary Graduate School Of Science And Technology Shins
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Ohrui Hiroshi
Yokohama Coll. Of Pharmacy
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Miyagi Takuho
Laboratory Of Applied Bioorganic Chemistry Graduate School Of Agricultural Science Tohoku University
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Nagasawa Tomohiro
Laboratory Of Applied Bioorganic Chemistry Graduate School Of Agricultural Science Tohoku University
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Kageyama Masayuki
Laboratory Of Applied Bioorganic Chemistry Graduate School Of Agricultural Science Tohoku University
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Yoshida Mayumi
Laboratory Of Applied Bioorganic Chemistry Graduate School Of Agricultural Science Tohoku University
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