175673-57-1

Upstream product

• 332-42-3 (2-bromoethyl)-4-fluorobenzene 
• 311348-76-2 (S)-(-)-α-(2,3-dimethoxyphenyl)-4-piperidinemethanol 
• 252364-39-9 4-[1-oxo-1-(2,3-dimethoxyphenyl)methyl]-N-2-(4-fluorophenylethyl)piperidine 
• 175553-31-8 1-[2-(4-fluorophenyl)-ethyl]-piperidine-4-carboxylic acid ethyl ester 
• 175553-32-9 1-[2-(4-fluorophenyl)ethyl]-4-piperidinecarboxylic acid N-methoxy N-methyl amide 
• 869749-06-4 (S)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, (2S,3S)-(+)-di-(p-anisoyl)-tartaric acid salt 
• 139290-69-0 (2,3-dimethoxy-phenyl)-{1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-methanol 
• 139290-71-4 4-(2,3-Dimethoxybenzoyl)-1-piperidinecarboxylic acid 1,1-dimethylethyl ester 
• 139290-72-5 (2,3-dimethoxyphenyl)(piperidin-4-yl)methanone 
• 140235-25-2 (+/-)-α-(2,3-dimethoxyphenyl)-4-piperidinemethanol 
• 7589-27-7 2-(4-Fluorophenyl)ethanol 
• 139290-76-9 (S,S)-(+)-α-[(2,3-dimethoxyphenyl)-[1-[2-(4-fluorophenyl)ethyl]-4-piperidinyl]methyl]-α-methoxybenzene acetate 
• 175553-30-7 (S)-(-)-α-(2-hydroxy-3-methoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanone 
• 74-88-4 methyl iodide 

Downstream Products

• 175553-30-7 (S)-(-)-α-(2-hydroxy-3-methoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanone 
• 139290-69-0 (2,3-dimethoxy-phenyl)-{1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-methanol 

Relevant academic research and scientific papers

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.

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:

A practical synthesis of the serotonin 5-HT(2a) receptor antagonist MDL 100907, its enantiomer and their 3-phenolic derivatives as precursors for [11C ]labeled PET ligands

A practical synthesis of the 3-phenolic precursor of MDL 100907, a selective 5-HT(2A) receptor antagonist, is described. The route was also applied to the enantiomeric series, thus affording the direct precursors of both 3-[11C]MDL 100907 and its enantiomer as ligands for positron emission tomography. Similar methodology was developed for the direct synthesis of MDL 100907 and its enantiomer, MDL 100009. The routes utilized classical optical resolution of the N-nor intermediates in at least 98% enantiomeric excess and easily afforded multigram amounts of the chiral precursors of a variety of N- and 3-O-substituted enantiomers. Copyright (C) 2000 Elsevier Science Ltd.

An efficient synthesis of the precursors of [11C]MDL 100907 labeled in two specific positions

An efficient, integrated route for the synthesis of two precursors of [11C]MDL 100907 labeled in the 2'- or 3'-methoxy position is reported. The synthesis involved a one-pot, two-step process to transform the intermediate esters to ketones and subsequent resolution of the racemic alcohols to their respective enantiomers. The resolved, enantiomerically pure phenol precursors were reacted with high specific activity [11C]methyl iodide to produce [11C]MDL 100907 labeled in two specific positions.

Synthesis and preliminary in vivo evaluation of [11C]MDL 100907: A potent and selective radioligand for the 5-HT2A receptor system

11C-Labeled MDL 100907 and MDL 100009 were prepared by the reaction of [11C]CH3I with the corresponding phenol precursors. In vivo studies conducted in rats and a baboon demonstrated that intravenously injected [2-O[11C]CH3]MDL 100907 was regionally distributed in the brain in a manner consistent with the known distribution of 5-HT2A receptors. Injection of [2-O[11C]CH3]MDL 100009 resulted in a uniform brain distribution of radioactivity without regional localization consistent with the lower affinity of MDL 100009 for 5-HT2A receptors.