126400-95-1Relevant articles and documents
Mimicking enzymatic transaminations: Attempts to understand and develop a catalytic asymmetric approach to chiral α-amino acids
Bachmann, Stephan,Knudsen, Kristian Rahbek,Jorgensen, Karl Anker
, p. 2044 - 2049 (2004)
Attempts are made to build a bridge between asymmetric catalysis and enzymatic reactions by mechanistic investigations and the development of a catalytic and enantioselective approach to amination of α-keto esters by primary amines catalyzed by chiral Lewis acids as a model for transamination enzymes. Different Lewis acids can catalyze the half-transamination of α-keto esters using primary amine nitrogen sources such as pyridoxamine and 4-picolylamine. The mechanistic studies of the Lewis-acid catalyzed half-transamination using deuterium-labelled compounds show the incorporation of deuterium atoms in several positions of the α-amino acid derivative, indicating that the enol of the α-keto ester plays an important role along the reaction path. The catalytic enantioselective reactions are dependent on the pKa-value of the solvent since enantioselectivities were only obtained in solvents with high pKa-values relative to methanol. However, stronger acidic conditions generally gave better yields, but poor enantioselectivities. A series of chiral Lewis acids were screened as catalysts for the enantioselective half-transamination reactions and moderate yields and enantioselectivities of up to 46% ee were obtained.
Development of triazine-based esterifying reagents containing pyridines as a nucleophilic catalyst
Yamada, Kohei,Liu, Jie,Kunishima, Munetaka
supporting information, p. 6569 - 6575 (2018/09/25)
We have developed new triazine-based esterifying reagents comprising pyridines that can act as a nucleophilic catalyst. 1-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-3,5-lutidinium chloride (DMT-3,5-LUT) was found to exhibit a superior reactivity for the dehydrating condensation reaction between carboxylic acids and alcohols. The reaction of DMT-3,5-LUT with carboxylic acids produces intermediacy of acyloxytriazines, which is known to exhibit moderate reactivity toward alcohols, with concomitant liberation of 3,5-lutidine. The subsequent chemical transformation of the acyloxytriazines and alcohols into esters can be accelerated by the action of 3,5-lutidine as a nucleophilic catalyst. The detailed reaction mechanism revealed by a time-course analysis of the reactions is also discussed.
NS5B polymerase inhibitor
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Paragraph 0017, (2017/08/19)
The invention discloses a compound represented by a formula shown in the description, or medicinal salts thereof. The compound has a better hepatitis C treatment effect than sofosbuvir, has similar toxic and side effects with the sofosbuvir, and does not have obvious untoward effects.
