- Merging lithium carbenoid homologation and enzymatic reduction: A combinative approach to the HIV-protease inhibitor Nelfinavir
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An effective stereocontrolled synthesis of the HIV protease inhibitor Nelfinavir is reported. Two transformations were identified crucial for achieving success: the formation of a densely functionalized α-chloroketone via the homologation of a Weinreb ami
- Castoldi, Laura,Ielo, Laura,Hoyos, Pilar,Hernáiz, María J.,De Luca, Laura,Alcántara, Andrés R.,Holzer, Wolfgang,Pace, Vittorio
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p. 2211 - 2217
(2018/03/28)
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- A new strategy for accessing (S)-1-(furan-2-yl)pent-4-en-1-ol: a key precursor of Ipomoeassin family of compounds and C1–C15 domain of halichondrins
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A highly efficient synthesis of (S)-1-(furan-2-yl)pent-4-en-1-ol, known to be an initial precursor of Ipomoeassin family of compounds and C1–C15 domain of halichondrins has been achieved via a sequence involving the use of Weinreb amide formation followed by Weinreb ketone synthesis and finally CBS (Corey–Bakshi–Shibata) reduction. Detailed study on improvement of each step is described. The title compound was converted to a potential cytotoxic agent for further pharmacological studies.
- Jammula, Subba Rao,Anna, Venkateswara Rao,Tatina, Sudhakar,Krishna, Thalishetti,Sreenivas, B. Yogi,Pal, Manojit
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supporting information
p. 3924 - 3928
(2016/08/09)
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- Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid
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A novel norstatine derivative, phenylthionorstatine [(2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid; Ptns], containing a hydroxymethylcarbonyl (HMC) isostere was designed, synthesized, and stereochemically determined. Then, Ptns was introduced into
- Ziora, Zyta,Kasai, Soko,Hidaka, Koushi,Nagamine, Ayaka,Kimura, Tooru,Hayashi, Yoshio,Kiso, Yoshiaki
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p. 1629 - 1633
(2007/10/03)
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