78070-16-3Relevant articles and documents
Enantioselective Synthesis of Quaternary Δ4- and Δ5-Dehydroprolines Based on a Two-Step Formal [3+2] Cycloaddition of α-Aryl and α-Alkyl Isocyano(thio)acetates with Vinyl Ketones
Odriozola, Amaiur,Oiarbide, Mikel,Palomo, Claudio
supporting information, p. 12758 - 12762 (2017/09/25)
A divergent synthesis of optically active quaternary Δ4- and Δ5-dehydro prolines is developed based on the first catalytic enantioselective conjugate addition of α-substituted isocyano(thio)acetates to vinyl ketones that is general for both α-aryl and α-alkyl isocyano(thio)acetates. The new tetrasubstituted C?N stereocenter is formed without the need of any metal salt due to a bifunctional tertiary amine/squaramide catalyst, featuring a bulky polyaryl sidearm and an unusually short squaramide diamide H???H interatomic distance in the solid state.
Quantitative Structure Activity Relationship in 3,4-Disubstituted Pyridines and 1-(3"-Amino-4"-pyridyl)-4-arylpiperazines
Saxena, Anil K.,Arunamurthy, V.,Patnaik, G. K.,Jain, Padam C.,Anand, Nitya
, p. 873 - 878 (2007/10/02)
In a study of the SAR in 3,4-disubstituted pyridines, it has been observed that both stimulant and anticonvulsant activities are confined to 1-(3'-amino-4'-pyridyl)-4-phenylpiperazines, and further the substitution in the phenyl ring can dissociate these activities of this prototype.In order to understand the relationship of electronic (?), hydrophobic (?) and stereo (Es) parameters of the substituents with anticonvulsant activity, a multi-parameter regression analysis of twelve compounds of this group has been carried out, which suggests that hydrophobic and electronic factors are more important and anticonvulsant activity can be enhanced by compounds having log P = 2.7- 3.1 0= 2.67 (Eq. 5) and (log P)0= 3.09 (Eq. 6)> with an electron withdrawing substituent in the phenyl ring.