134272-15-4

Upstream product

• 609-14-3 2-acetylpropanoic acid ethyl ester 
• 100-46-9 benzylamine 

Downstream Products

• 134272-17-6 ethyl 3-(N-benzyl)methoxyacetamido-2-methylcrotonate 
• 134272-20-1 ethyl 3-(N-benzyl)ethoxyacetamido-2-methylcrotonate 
• 134272-24-5 N-benzyl-5,6-dimethyl-3-ethoxy-4-hydroxy-2-pyridone 
• 134272-21-2 N-benzyl-4-hydroxy-3-methoxy-5,6-dimethylpyridin-2(1H)-one 

Relevant academic research and scientific papers

Redox Property of Enamines

Enamines are electron-rich compounds bearing intriguing redox properties. Herein, a series of secondary enamines condensed from primary amine and β-ketocarbonyls were synthesized and their electrochemical oxidation properties were systematically studied by cyclic voltammetry. Furthermore, theoretical calculation of oxidation potentials of enamines, particularly those catalytic intermediates, was also conducted to further broaden the scope investigated. Possible structural factors on oxidation and the nature of the resulted radical cation intermediates were revealed and discussed. Correlation of redox potentials with molecular properties such as highest occupied molecular orbital energies and natural population analysis charge were explored, and there appears no simple linear correlation. On the other hand, a good correlation with Mayr's nucleophilicity parameter N was noted among a range of catalytically relevant enamines. Spin population analysis disclosed that enamine radical cations mainly exhibit the carbon-center free radical feature. Taking experimental and computation data together, a comprehensive picture about the redox property of enamines is presented, which would provide guidance in the development of oxidative enamine catalysis and transformations.

Expanding dynamic kinetic protocols: Transaminase-catalyzed synthesis of α-substituted β-amino ester derivatives

Several α-alkylated β-amino esters have been obtained via DKR processes employing a kit of transaminases and isopropylamine as an amino donor in aqueous medium under mild conditions. Thus, while acyclic α-alkyl-β-keto esters afforded excellent conversions and enantioselectivities, although usually low diastereoselectivities, using more constrained cyclic β-keto esters high to excellent inductions were obtained.

ANTIPRURITICS

It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having an agonistic activity to the cannabinoid receptor shows an antipruritics effect.

PYRIDONE DERIVATIVE HAVING AFFINITY FOR CANNABINOID 2-TYPE RECEPTOR

It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R' is a group represented by the formula: -Y1-Y2-Y3Ra wherein Y1 is single bond or the like; Y2 is -C(=O)-NH- or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.

A FACILE SYNTHESIS OF SUBSTITUTED 4-HYDROXY-2-PYRIDONES

Substituted 4-hydroxy-2-pyridones (1a-1d) were easily synthesized from ethyl acetoacetate in good yields via C-alkylation, enamine formation, N-acylation, intramolecular cyclization, and debenzylation.