859538-90-2

Upstream product

• 59781-11-2 (5-(benzyloxy)pyridin-2-yl)methanol 
• 886980-65-0 5-(benzyloxy)-2-(methoxymethyl)pyridine 
• 67-56-1 methanol 
• 173913-75-2 5-(benzenesulfonyloxy)-2-(bromomethyl)pyridine 

Downstream Products

• 1034497-97-6 C₂₅H₂₅N₅O₆ 

Relevant academic research and scientific papers

THIAZOLIDINONE COMPOUNDS AND USE THEREOF

A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.

The regioselective homocoupling of meta-hydroxypyridines with hypervalent iodine(iii)

The C-H homocoupling of meta-hydroxypyridines with phenyliodine(III) diacetate (PIDA) was carried out in dichloromethane at room temperature in the presence of cesium carbonate. The coupling reaction is highly regioselective with respect to the hydroxy group at the pyridine ring. Comparative control experiments with meta-alkoxypyridine suggest that the meta-hydroxy group at the pyridine ring plays a key role during the homocoupling reaction.

OXOTETRAHYDROFURAN-2-YL-BENZIMIDAZOLE DERIVATIVE

The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a carbamoyl group; R2 represents a lower alkyl group; both of X1 and X2 represent CH, or any one of X1 and X2 represents a nitrogen atom and the other represents CH; a group of represents a group selected from the group consisting of a pyridinyl, a pyrazinyl, a pyrazolyl, a thiadiazolyl, a triazolyl, an isoxazolyl and a thiazolyl group; and k is zero or 1, or relates to pharmaceutically acceptable salts thereof.

Enantioselective Pd-catalyzed α-arylation of N-Boc-pyrrolidine: The key to an efficient and practical synthesis of a glucokinase activator

(Chemical Equation Presented) A short and practical synthesis of glucokinase activator 1 was achieved utilizing a convergent strategy involving SNAr coupling of activated aryl fluoride 11 with hydroxypyridine 9. The key to the success of the synthesis was the development of a novel method for enantioselective formation of α-arylpyrrolidines during the course of the project. In this method, (-)-sparteine-mediated enantioselective lithiation of N-Boc-pyrrolidine was followed by in situ transmetalation to zinc and Pd-catalyzed coupling with aryl bromide 3, proceeding in 92% ee. This transformation allowed the preparation of compound 1 in a 31% overall yield over six steps.

HETEROCYCLE-SUBSTITUTED BENZIMIDAZOLE DERIVATIVE

Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): (wherein X1 to X4 represent a carbon atom, etc., ring A represents a 5- or 6-membered heteroaryl having from 1 to 4 hetero atoms selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom, X5 represent an oxygen atom, etc., X represent a carbon atom, etc., Het represents a 5- or 6-membered aliphatic hetero ring, R1 represents aryl, etc., R2 represents formyl, etc., R3 represents -C1-6 alkyl, etc.), as well as their pharmaceutically acceptable salts.

PYRIDYL NON-AROMATIC NITROGENATED HETEROCYCLIC-1-CARBOXYLATE ESTER DERIVATIVE

[Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.