110137-64-9

Upstream product

• 1571-08-0 methyl 4-formylbenzoate 
• 62-53-3 aniline 
• 39126-16-4 methyl 4-[(phenylamino)methyl]benzoate 
• 619-66-9 4-Carboxybenzaldehyde 
• 3939-34-2 4-[(phenylimino)methyl]benzoic acid 

Relevant academic research and scientific papers

Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages

Histone deacetylases (HDACs) play an important role in cancer, degenerative diseases and inflammation. The currently applied HDAC inhibitors in the clinic lack selectivity among HDAC isoforms, which limits their application for novel indications such as i

BF3·Et2O as a metal-free catalyst for direct reductive amination of aldehydes with amines using formic acid as a reductant

A versatile metal- and base-free direct reductive amination of aldehydes with amines using formic acid as a reductant under the catalysis of inexpensive BF3·Et2O has been developed. A wide range of primary and secondary amines and diversely substituted aldehydes are compatible with this transformation, allowing facile access to various secondary and tertiary amines in high yields with wide functional group tolerance. Moreover, the method is convenient for the late-stage functionalization of bioactive compounds and preparation of commercialized drug molecules and biologically relevant N-heterocycles. The procedure has the advantages of simple operation and workup and easy scale-up, and does not require dry conditions, an inert atmosphere or a water scavenger. Mechanistic studies reveal the involvement of imine activation by BF3and hydride transfer from formic acid.

Main-Group-Catalyzed Reductive Alkylation of Multiply Substituted Amines with Aldehydes Using H2

Given the growing demand for green and sustainable chemical processes, the catalytic reductive alkylation of amines with main-group catalysts of low toxicity and molecular hydrogen as the reductant would be an ideal method to functionalize amines. However, such a process remains challenging. Herein, a novel reductive alkylation system using H2 is presented, which proceeds via a tandem reaction that involves the B(2,6-Cl2C6H3)(p-HC6F4)2-catalyzed formation of an imine and the subsequent hydrogenation of this imine catalyzed by a frustrated Lewis pair (FLP). This reductive alkylation reaction generates H2O as the sole byproduct and directly functionalizes amines that bear a remarkably wide range of substituents including carboxyl, hydroxyl, additional amino, primary amide, and primary sulfonamide groups. The synthesis of isoindolinones and aminophthalic anhydrides has also been achieved by a one-pot process that consists of a combination of the present reductive alkylation with an intramolecular amidation and intramolecular dehydration reactions, respectively. The reaction showed a zeroth-order and a first-order dependence on the concentration of an imine intermediate and B(2,6-Cl2C6H3)(p-HC6F4)2, respectively. In addition, the reaction progress was significantly affected by the concentration of H2. These results suggest a possible mechanism in which the heterolysis of H2 is facilitated by the FLP comprising THF and B(2,6-Cl2C6H3)(p-HC6F4)2.

Modulators of methyl modifying enzymes, compositions and uses thereof

Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF

Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein

Direct and indirect reductive amination of aldehydes and ketones with solid acid-activated sodium borohydride under solvent-free conditions

A simple and convenient procedure for reductive amination of aldehydes and ketones using sodium borohydride activated by boric acid, p-toluenesulfonic acid monohydrate or benzoic acid as reducing agent under solvent-free conditions is described.

Clean and Simple Chemoselective Reduction of Imines to Amines Using Boric Acid-Activated Sodium Borohydride under Solvent-Free Conditions

The first clean and highly effective solvent-free chemoselective reduction of functionalized aldimines and ketimines bearing easily reducible functional groups, such as ketone, carboxylic acid, ester, nitrile, amide, nitro, furyl and alkenyl groups, to th

Selective Reduction of Imines with the Diborane-Methanol System

The selective reduction of imines with diborane-methanol system was investigated.This system reduced imines quatitatively, and other functional groups tested were unaffected.Keywords-imine; diborane; selective reduction; diborane-methanol system; secondary amine; dimethoxyborane