42122-41-8Relevant academic research and scientific papers
FUSED 1,4-DIHYDRODIOXIN DERIVATIVES AS INHIBITORS OF HEAT SHOCK TRANSCRIPTION FACTOR 1
-
Paragraph 00121, (2015/04/22)
The present invention relates to compounds of formula I wherein A1, A2 R4 and Q are as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
Platinum-Catalyzed, Terminal-Selective C(sp3)-H Oxidation of Aliphatic Amines
Lee, Melissa,Sanford, Melanie S.
supporting information, p. 12796 - 12799 (2015/10/28)
This Communication describes the terminal-selective, Pt-catalyzed C(sp3)-H oxidation of aliphatic amines without the requirement for directing groups. CuCl2 is employed as a stoichiometric oxidant, and the reactions proceed in high yield at Pt loadings as low as 1 mol%. These transformations are conducted in the presence of sulfuric acid, which reacts with the amine substrates in situ to form ammonium salts. We propose that protonation of the amine serves at least three important roles: (i) it renders the substrates soluble in the aqueous reaction medium; (ii) it limits binding of the amine nitrogen to Pt or Cu; and (iii) it electronically deactivates the C-H bonds proximal to the nitrogen center. We demonstrate that this strategy is effective for the terminal-selective C(sp3)-H oxidation of a variety of primary, secondary, and tertiary amines.
Hydrophobic amplification of noncovalent organocatalysis
Kleiner, Christian M.,Schreiner, Peter R.
, p. 4315 - 4317 (2007/10/03)
The effects of hydrogen-bonding organocatalysts and water for the acceleration of epoxide openings with a variety of nucleophiles are additive and lead to excellent yields of the catalyzed reactions in water. The Royal Society of Chemistry 2006.
Highly chemoselective addition of amines to epoxides in water
Azizi, Najmodin,Saidi, Mohammad R.
, p. 3649 - 3651 (2007/10/03)
(Chemical Equation Presented) Aminolysis of a variety of epoxides by aliphatic and aromatic amines in water, in the absence of any catalyst with high yields, is reported. β-Amino alcohols were formed under mild conditions with high selectivity and in excellent yields.
N-Alkylation d'amines en catalyse homogene. Synthese de mono- et de diamines cycliques
Bitsi, G.,Schleiffer, E.,Antoni, F.,Jenner, G.
, p. 343 - 352 (2007/10/02)
Ruthenium compounds are appropriate catalysts in the N-alkylation of amines.The synthesis of N-alkylated cyclic amines from a cyclic amine and an alcohol or via the condensation between a diol and a primary amine are described.The reaction with cyclic amines is highly selective, especially in the presence of a phosphine, making it a high yielding preparative procedure.The catalytic condensation between cyclic amines and diols yields either an aminoalcohol (A) or a bicyclic diamine (B).The temperature, the presence of phosphine, and the ratio of amine to diol are decisive in directing the reaction toward A or B.The proposed mechanism involves the dehydrogenation of the alcohol followed by attack of the amine on the aldehyde intermediate.
