Kinetic Resolution of Cyclic Secondary Azides, Using an Enantioselective Copper-Catalyzed Azide-Alkyne Cycloaddition
An enantioselective copper-catalyzed azide-alkyne cycloaddition (E-CuAAC) is reported by kinetic resolution. Chiral triazoles were isolated in high yield with limiting alkyne (up to 97:3 enantiomeric ratio (er)). A range of substrates were tolerated (>30 examples), and the reaction was scaled to >1 g. The er of a triazole product could be enhanced by recrystallization and the recovered scalemic azide could be racemized and recycled. Recycling the azide allows efficient use of the undesired azide enantiomer.
Alexander, Juliana R.,Ott, Amy A.,Liu, En-Chih,Topczewski, Joseph J.
There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.
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Page/Page column 58
(2012/11/13)
Baker's yeast catalysed enantioselective reduction of chroman-4-ones
Substituted chroman-4-ones 1a-10a on catalytic reduction with Baker's Yeast give (S)-chroman-4-ols 1c-11c with high enantioselectivity. The absolute configuration has been determined by specific rotation and CD spectra.
Ramadas,David Krupadanam
p. 1119 - 1122
(2007/10/03)
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