861369-89-3

Upstream product

• 50-00-0 formaldehyd 
• 98-86-2 acetophenone 
• 91-21-4 1,2,3,4-tetrahydroisoquinoline 
• 936-59-4 3-chloropropiophenone 
• 3623-15-2 phenyl propargyl ketone 
• 4187-87-5 1-Phenyl-2-propyn-1-ol 
• 100-52-7 benzaldehyde 

Downstream Products

• 639467-80-4 2-(3-chloro-3-phenylpropyl)-1,2,3,4-tetrahydroisoquinoline 
• 16576-50-4 3-[3,4-dihydroisoquinolin-2(1H)-yl]-1-phenylpropan-1-ol 

Relevant academic research and scientific papers

Metal-free synthesis of β-aminoketones by the reductive hydroamination of ynones

This study describes a cascade method for the synthesis of β-aminoketones through the reductive hydroamination of alkynes under very mild metal-free conditions. It allows for the rapid conversion of ynones and amines into corresponding β-aminoketones with a broad substrate scope and diverse functionalities. This straightforward and easy-to-handle reaction process can be successfully applied for the synthesis of Proroxan and Propipocaine, offering a potential option for the synthesis of drug molecules with the β-aminoketone skeleton.

Syntheses and Binding Studies of New [(Aryl)(aryloxy)methyl]piperidine Derivatives and Related Compounds as Potential Antidepressant Drugs with High Affinity for Serotonin (5-HT) and Norepinephrine (NE) Transporters

In a wide search program toward new, efficient, and fast-acting antidepressant drugs, we have prepared series of new compounds having an (aryl)(aryloxy)methyl moiety linked directly or through a methylene chain to different substituted and unsubstituted cycles (isoquinoline, piperazine, piperidine, tetrahydropyran, or cyclopentane). These compounds have been evaluated for their affinities for serotonin (5-HT) transporter (SERT) and 5-HT1A and 5-HT2A receptors. Racemic mixtures of 4-[(aryl)(aryloxy)methyl]piperidine derivatives showed much higher affinity values for SERT than fluoxetine and resulted in lack of affinity for 5-HT 1A and 5-HT2A receptors. Some of these racemic mixtures were resolved to their enantiomers and tested for binding to norepinephrine (NE) transporter (NET), dopamine (DA) transporter (DAT), and α2 receptor. Several of these enantiomers [(-)-15b, (-)-15j, (-)-15t, (+)-15u] displayed a dual binding profile with affinities for SERT and NET with K i i = 1.9 and 13.5 nM, respectively), and further pharmacological characterization is in progress for its evaluation as a antidepressant.