- Practical and efficient route to (S)-γ-fluoroleucine
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A practical and efficient route to (S)-γ-fluoroleucine was developed via compound 9. Introduction of the fluorine was achieved using N,N-diethylaminosulfur trifluoride (DAST) treatment on a tertiary alcohol 8.
- Truong, Vouy Linh,Gauthier, Jacques Yves,Boyd, Michael,Roy, Bruno,Scheigetz, John
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p. 1279 - 1280
(2007/10/03)
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- A new entry to polyfunctionalized 4,5-trans disubstituted oxazolidin-2-ones from L-aspartic acid
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A straightforward synthesis of enantiomerically pure (4R,5S)-5-oxazolidinecarboxylic acid, 2-oxo-4-[(t-butyldimethyl-silyloxy)methyl]-, benzyl ester and of (4S,5S)-4-oxazolidinecarboxylic acid, 2-oxo-5-[(t-butyldimethylsilyloxy)methyl]-, benzyl ester was envisaged starting from readily available L-aspartic acid. The key step is the diastereoselective addition of iodine with the introduction of a new stereogenic centre.
- Luppi, Gianluigi,Tomasini, Claudia
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p. 797 - 800
(2007/10/03)
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- Peptide based interleukin-1β converting enzyme (ICE) inhibitors: Synthesis, structure activity relationships and crystallographic study of the ICE-inhibitor complex
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Based on the X-ray structure of the complex of Ac-Tyr-Val-Ala-Asp-H (L- 709049) and interleukin-1β converting enzyme (ICE), we synthesized compounds which were derived from 2-NapCO-Val-Pro-Asp-CH2OPh (1) to obtain a potent inhibitor in the cell
- Okamoto, Yoshinori,Anan, Hideki,Nakai, Eiichi,Morihira, Koichiro,Yonetoku, Yasuhiro,Kurihara, Hiroyuki,Sakashita, Hitoshi,Terai, Yoshiya,Takeuchi, Makoto,Shibanuma, Tadao,Isomura, Yasuo
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