139290-69-0

Usage

Chemical Properties

Colourless to yellowish solid

Upstream product

• 332-42-3 (2-bromoethyl)-4-fluorobenzene 
• 140235-25-2 (+/-)-α-(2,3-dimethoxyphenyl)-4-piperidinemethanol 
• 243640-29-1 4-[1-oxo-1-(2,3-dimethoxyphenyl)methyl]-N-2-(4-fluorophen-1-oxo-ethyl)piperidine 
• 243640-20-2 (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, (2S,3S)-(+)-di-(p-anisoyl)-tartaric acid salt 
• 869749-06-4 (S)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, (2S,3S)-(+)-di-(p-anisoyl)-tartaric acid salt 
• 243640-37-1 4-[1-hydroxy-1-(2,3-dimethoxyphenyl)methyl]-N-2-(4-fluorophen-1-oxo-ethyl)piperidine 
• 91-16-7 1,2-dimethoxybenzene 
• 139290-66-7 1-[2-(4-fluorophenyl)-ethyl]-4-piperidinecarboxamide 
• 175673-57-1 (-)-MDL 100907 
• 1126-09-6 4-carbethoxypiperidine 
• 175553-32-9 1-[2-(4-fluorophenyl)ethyl]-4-piperidinecarboxylic acid N-methoxy N-methyl amide 
• 175553-31-8 1-[2-(4-fluorophenyl)-ethyl]-piperidine-4-carboxylic acid ethyl ester 
• 7589-27-7 2-(4-Fluorophenyl)ethanol 
• 252364-39-9 4-[1-oxo-1-(2,3-dimethoxyphenyl)methyl]-N-2-(4-fluorophenylethyl)piperidine 

Downstream Products

• 139290-76-9 (S,S)-(+)-α-[(2,3-dimethoxyphenyl)-[1-[2-(4-fluorophenyl)ethyl]-4-piperidinyl]methyl]-α-methoxybenzene acetate 
• 243640-20-2 (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, (2S,3S)-(+)-di-(p-anisoyl)-tartaric acid salt 
• 869749-06-4 (S)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, (2S,3S)-(+)-di-(p-anisoyl)-tartaric acid salt 
• 243640-24-6 (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, butyrate ester 
• 243640-22-4 α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, butyrate ester 
• 175673-57-1 (-)-MDL 100907 
• 175553-30-7 (S)-(-)-α-(2-hydroxy-3-methoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanone 
• 175553-29-4 (R)-(+)-α-(2-hydroxy-3-methoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanone 
• 139290-65-6 R-(+)-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol 

Relevant academic research and scientific papers

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET

Radiolabelled piperidine derivatives such as [11C]MDL 100907 and [18F]altanserin have played an important role in diagnosing malfunction in the serotonergic neurotransmission. A variety of novel piperidine MDL 100907 derivatives, possible to label with 18F-fluorine, were synthesized to improve molecular imaging properties of [11C]MDL 100907. Their in vitro affinities to a broad spectrum of neuroreceptors and their lipophilicities were determined and compared to the clinically used reference compounds MDL 100907 and altanserin. The novel compounds MA-1 (53) and (R)-MH.MZ (56) show Ki-values in the nanomolar range towards the 5-HT2A receptor and insignificant binding to other 5-HT receptor subtypes or receptors. Interestingly, compounds MA-1 (53), MH.MZ (55) and (R)-MH.MZ (56) provide a receptor selectivity profile similar to MDL 100907. These compounds could possibly be preferable antagonistic 18F-tracers for visualization of the 5-HT2A receptor status. Medium affine compounds (VK-1 (32), (51), (52), (54)) were synthesized and have Ki values between 30 and 120 nM. All promising compounds show log P values between 2 and 3, that is, within the range of those for the established radiotracers altanserin and MDL 100907. The novel compounds MA-1 (53) and (R)-MH.MZ (56) thus appear to be promising high affine and selective tracers of 18F-labelled analogues for 5-HT2A imaging with PET.

COMBINATION OF A HYPNOTIC AGENT AND R (+)-ALPHA-(2,3-DIMETHOXY-PHENYL)-1-[2-(4-FLUOROPHENYL)ETHYL]-4-PIPERIDINEMETHANOL AND THERAPEUTIC APPLICATION THEREOF

The invention concerns the combination of a short-acting hypnotic agent and R-(+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol (Compound A) or its prodrug having the Formula II: wherein R is C1-C20 alkyl o

Processes for the preparation of (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol"

The present invention provides various processes for the preparation of (R)-±-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:

Use of MDL-100,907 for treatment of allergic and eosinophil mediated diseases

Methods of modulating eosinophil migration, chemotaxis or generation, in vitro, ex vivo, and in vivo are provided. Methods include contacting eosinophils with an amount of 5-HT2A receptor agonist or antagonist sufficient to modulate eosinophil migration, chemotaxis or generation.

The "reverse-tethered" ruthenium (II) catalyst for asymmetric transfer hydrogenation: Further applications

The attachment of a tethering group from the basic nitrogen atom to the arene ligand of a ruthenium(II) catalyst greatly improves its ability to catalyze asymmetric transfer hydrogenation (ATH) reactions. In this paper, we describe further applications of this versatile system to an extended substrate range.

Novel processes for the preparation of (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol

The present invention provides various processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:

Novel processes for the preparation or (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol

The present invention provides various processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:

Use of (+)-a-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol or its prodrug in the treatment of symptoms of dementia and dopamine induced psychosis

The present invention is directed to use of (+)-α-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol or its prodrug (Formula II) in treating patients for symptoms of dementia and dopamine induced psychosis.

USE OF R-(+)-alpha-(2,3-DIMETHOXYPHENYL-1-[2-(4-FLUOROPHENYL) ETHYLl-4-PIPERIDINEMETHANOL FOR THE TREATMENT OF SLEEP DISORDERS

A method of treating a patient for a Sleep Disorder comprising administering an effective amount of R-(+)-α-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol or a pharmaceutically acceptable salt thereof to a patient in need of such treatment.