145021-97-2

Upstream product

• 6576-05-2 1-(4-fluorophenyl)-2-(4-pyridyl)ethanone 
• 24424-99-5 di-tert-butyl dicarbonate 
• 40110-55-2 ethyl 2-(1-benzylpiperidine-4-ylidene)acetate 
• 451-46-7 4-fluorobenzoic acid ethyl ester 
• 108-89-4 picoline 
• 78056-59-4 ethyl 2-(1-acetyl-4-piperidyl)acetate 
• 71879-59-9 ethyl (1-benzylpiperidin-4-yl)acetate 
• 137996-01-1 4-<2-(4-fluorophenyl)-2-oxoethyl>piperidine 
• 78056-63-0 2-(1-acetyl-4-piperidinyl)-1-(4-fluorophenyl)ethanone 
• 78056-61-8 2-(1-Acetyl-4-piperidyl)acetyl chloride 
• 78056-60-7 (1-acetylpiperidin-4-yl)acetic acid 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 462-06-6 fluorobenzene 

Downstream Products

• 639468-66-9 4-[2-(4-fluorophenyl)-2-hydroxyethyl]piperidine-1-carboxylic acid tert-butyl ester 
• 137996-01-1 4-<2-(4-fluorophenyl)-2-oxoethyl>piperidine 

Relevant academic research and scientific papers

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.

Novel piperidine σ receptor ligands as potential antipsychotic drugs

σ receptor ligands represent a new class of potential antipsychotic drugs. This paper presents the structure-activity relationships leading to novel disubstituted piperidine σ ligands, which have little or no affinity for dopamine D2 receptors. Selectivity for σ sites over dopamine D2 or serotonin 5-HT2 receptors appears to be governed by the chemical nature of the piperidine nitrogen substituent, its distance from the basic nitrogen, and its orientation relative to the other piperidine substituent. Several of these compounds have good oral potency in some animal models used to evaluate potential antipsychotic drugs. The N-cyclopropylmethyl ketones and ethers (e.g. 6i (DuP 734), 6q, 18a, and 18n) have the best in vivo potency. Compounds 6i (DuP 734) and 6q did not cause catalepsy in the rat, even at very high doses. On the basis of the pharmacology profiles of these σ ligands, we propose these compounds may be effective antipsychotic drugs, which do not induce extrapyramidal side effects or tardive dyskinesia.