69293-74-9

Upstream product

• 109-89-7 diethylamine 
• 17201-43-3 4-cyanobenzyl bromide 
• 70135-28-3 (4-cyanophenyl)diazomethane 
• 105-07-7 4-cyanobenzaldehyde 
• 13686-66-3 N,N-diethylaminodimethylsilane 
• 874-86-2 4-cyanobenzyl chloride 
• 616-39-7 N,N-diethylnmethylamine 
• 623-00-7 4-bromobenzenecarbonitrile 

Downstream Products

• 84227-70-3 p-(diethylaminomethyl)benzylamine 
• 62642-59-5 4-diethylaminomethyl-benzoic acid 
• 125743-63-7 4-[(4-methyl-1-piperazinyl)methyl]benzonitrile 
• 91271-57-7 (4-((diethylamino)methyl)phenyl)methanol 
• 78329-96-1 4-diethylaminomethyl-benzoic acid-(3-dibutylamino-propyl ester) 

Relevant academic research and scientific papers

Simple Metal-Free Direct Reductive Amination Using Hydrosilatrane to Form Secondary and Tertiary Amines

This work describes the use of cheap, safe, and easy-to-handle hydrosilatrane as the reductant in direct reductive amination reactions. This efficient method enables a facile, metal-free access to secondary and tertiary amines from a wide range of aldehydes and ketones, with the synthesis of tertiary amines requiring no additives at all. This reaction demonstrates excellent functional group tolerance, chemoselectivity, and scalability. (Figure presented.).

tert-Butoxy-Radical-Promoted α-Arylation of Alkylamines with Aryl Halides

In the presence of a tert-butoxy radical precursor, the reaction of alkylamines with aryl halides was found to give α-arylated alkylamines through homolytic aromatic substitution of the halogen atoms.

Synthesis of new 4-Aminoquinolines and evaluation of their in vitro activity against chloroquine-sensitive and chloroquine-resistant plasmodium falciparum

The efficacy of chloroquine, once the drug of choice in the fight against Plasmodium falciparum, is now severely limited due to widespread resistance. Amodiaquine is one of the most potent antimalarial 4-Aminoquinolines known and remains effective against chloroquineresistant parasites, but toxicity issues linked to a quinone-imine metabolite limit its clinical use. In search of new compounds able to retain the antimalarial activity of amodiaquine while circumventing quinone-imine metabolite toxicity, we have synthesized five 4-Aminoquinolines that feature rings lacking hydroxyl groups in the side chain of the molecules and are thus incapable of generating toxic quinone-imines. The new compounds displayed high in vitro potency (low nanomolar IC50), markedly superior to chloroquine and comparable to amodiaquine, against chloroquine-sensitive and chloroquine-resistant strains of P. falciparum, accompanied by low toxicity to L6 rat fibroblasts and MRC5 human lung cells, and metabolic stability comparable or higher than that of amodiaquine. Computational studies indicate a unique mode of binding of compound 4 to heme through the HOMO located on a biphenyl moeity, which may partly explain the high antiplasmodial activity observed for this compound.

CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and 15 the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a' and I-A.a'' in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

Carboxamide compounds and their use as calpain inhibitors

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of

Lewis acid-catalyzed reductive amination of carbonyl compounds with aminohydrosilanes

The TiCl4-catalyzed reaction of aromatic carbonyl compounds with (dialkylamino)dimethylsilanes gave tertiary amines in moderate to high yields. The reductive amination of aliphatic aldehydes was effectively catalyzed by ZnI2. Methyl

Electron Transfer in Competition with Loss of Nitrogen in Photochemical Reactions of Aryldiazomethane with Diethylamine

The photolysis of aryldiazomethanes was studied as a function of aryl substituents and the p-nitro group was found to exert a special effect of product distribution.