75835-01-7

Upstream product

• 7433-88-7 4-methyl-2-styryl-pyridine 
• 108-47-4 2,4-lutidine 
• 100-44-7 benzyl chloride 
• 108-89-4 picoline 
• 501-52-0 3-Phenylpropionic acid 
• 100-39-0 benzyl bromide 
• 3262-89-3 triphenylboroxine 
• 865074-83-5 2-(2-methoxyethyl)-4-methylpyridine 
• 4926-28-7 2-Bromo-4-picoline 
• 536-74-3 phenylacetylene 
• 63731-33-9 4-methyl-2-phenylethynyl-pyridine 
• 100-52-7 benzaldehyde 
• 75834-96-7 2-(4-methyl(2-pyridyl))-1-phenylethan-1-ol 

Downstream Products

• 342894-91-1 1,4-dimethyl-6-phenethyl-1,2,3,6-tetrahydro-pyridine 
• 1155854-75-3 1-methyl-11-aza-tricyclo[8.3.1.0*2,7*]tetradeca-2.4,6-triene 

Relevant academic research and scientific papers

Solvent-free alkylation of N-heteroaromatic compounds by RCOOH-Pb(OAc) 4 system

The solvent-free decarboxylation of carboxylic acids by Pb(OAc)4 affords alkyl radicals, which alkylate 4-methylpyridine, quinoline, and 4-methylquinoline protonated with 2-chlorobenzoic acid. Mechanical activation is required for pyrazine alky

Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use

The present invention relates to compounds defined by Formula (I), wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

Ruthenium-catalyzed conversion of sp3 C-O bonds in ethers to C-C bonds using triarylboroxines

Catalytic conversion of unreactive sp3 C-O bonds in alkyl ethers to C-C bonds is described. Alkyl ethers bearing 2- or 4-pyridyl groups were coupled with triarylboroxines in the presence of a ruthenium catalyst. Triarylboroxines bearing a variety of functional groups including electron-withdrawing and -donating groups can be used for the reaction. No additional base was required for the coupling with the organoboron reagents, and base-sensitive groups can be tolerated. The reaction is considered to proceed via dehydroalkoxylation followed by addition of triarylboroxines to form C-C bonds.

ARYL- AND HETEROARYLCARBONYL DERIVATIVES OF BENZOMORPHANES AND RELATED SCAFFOLDS, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE

The present invention relates to compounds defined by formula (I), wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

UREA DERIVATIVES OF BENZOMORPHANES AND RELATED SCAFFOLDS, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE

The present invention relates to compounds defined by formula (I) wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

A platform for designing HIV integrase inhibitors. Part 1: 2-Hydroxy-3-heteroaryl acrylic acid derivatives as novel HIV integrase inhibitor and modeling of hydrophilic and hydrophobic pharmacophores

We present a novel series of HIV integrase inhibitors, showing IC50s ranging from 0.01 to over 370 μM in an enzymatic assay. Furthermore, pharmacophore modeling study for the inhibitors was carried out to elucidate the structure-activity relationships. Finally, we found a 3D-pharmacophore model, which is composed of a hydrophilic and a hydrophobic domain, providing valuable information for designing other novel types of integrase inhibitors.

PYRIDINES. PARTIE IX - PLURIBENZYLATION DE LA S-COLLIDINE ET DE LA LUTIDINE-2,6

A literature survey of the polymetalation of 2,6-lutidine 2 shows different results about the site(s) of deprotonation and condensation with various electrophiles.This discrepancy prompts us to examine the polylithiation (PhLi 3 equivalents, Et2O) of s-collidine 1, 2,6-lutidine 2 and more briefly of 2,4-lutidine 3.Polylithiation takes place exclusively at the methyl groups of the same position vs the ring nitrogen : 2- and/or 6-methyl of 1.The previous regioselectivity observed in the case of the monometalation in Et2O is maintained.From 1 and 2, polylithiation gives picolyl anions which lead by reaction with PhCH2Cl, simultaneously to mono-, di-symmetrical, di-non-symmetrical α-derivatives, and tri- and tetra-symmetrical α,α'-compounds; but no product is formed from a benzylic β-anion.In the same way, the deprotonation of 2-methyl-6-(2-phenylethyl) pyridine 17 leads to 2,6-bis (2-phenylethyl) pyridine 19 and 2-methyl-6-dibenzylmethyl pyridine 18, to the exclusion of the β-compound 2-methyl-6-(2,3-diphenylpropyl) pyridine 21.The latter compound is formed in low yield, besides 19 and 18, in the conditions of the Tchitchibabine reaction (NaNH2, toluene).The structure of the benzylated compounds was established mainly from the 1H-nmr data.No product was isolated which would result from the nucleophilic attack of the generated carbanions at the pyridine carbons.

Bridged-ring Nitrogen Compounds. Part 3. Synthesis of Representatives of the 1,5-Methano-4-benzazonine Ring System

Reaction of arylaldehydes with 2,4-dimethylpyridine and n-butyl-lithium gives in good yield 1-aryl-2-(4-methylpyridyl)ethanols which, after dehydration with polyphosphoric acid and catalytic hydrogenation, give 2-phenethyl-4-methylpyridines.Cyclisation of