67127-92-8

Upstream product

• 100-39-0 benzyl bromide 
• 1100844-42-5 benzyl 2-(benzyloxy)-5-methylbenzoate 
• 100-44-7 benzyl chloride 
• 22717-57-3 methyl 6-hydroxy-m-toluate 
• 424791-16-2 2-Benzyloxy-5-methyl-benzoic acid methyl ester 

Downstream Products

• 1285513-35-0 5-methyl-2-[(phenylmethyl)oxy]-N-3-pyridinylbenzamide 
• 129833-39-2 2-<2-(carboxymethyl)-4-methylphenoxy>-6-methylbenzoic acid 
• 129833-48-3 <2-(phenylmethoxy)-5-methylphenyl>acetic acid 
• 129833-50-7 2-(bromomethyl)-4-methyl-1-(phenylmethoxy)benzene 
• 67127-18-8 2-hydroxy-5-methyl-N-(1⁽²⁾H-tetrazol-5-yl)-benzamide 
• 67127-71-3 2-benzyloxy-5-methyl-N-(1⁽²⁾H-tetrazol-5-yl)-benzamide 

Relevant academic research and scientific papers

Metal-free Synthesis of Spiro-2,2′-benzo[b]furan-3,3′-ones via PhI(OAc)2-Mediated Cascade Spirocyclization

Treating the benzyl protected 3-hydroxy-1,3-bis(2-hydroxyphenyl)prop-2-en-1-ones solely with PhI(OAc)2 (PIDA) in DCE at room temperature readily furnished the seldom studied spiro-2,2′-benzo[b]furan-3,3′-ones in satisfactory to excellent yields. The hypervalent iodine reagent enables the metal-free cascade spirocyclization resulting in the dual oxidative C?O bond formation. (Figure presented.).

Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors

Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson's disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds 8e, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability.

NOVEL COMPOUNDS

The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.

Solid-phase synthesis of new saphenamycin analogues with antimicrobial activity

An array of 12 new saphenamycin analogues modified at the benzoate moiety was synthesized on solid support. Synthesis commenced with a chemoselective anchoring of saphenic acid through the carboxyl group to a 2-chlorotrityl functionalized polystyrene resin. The secondary alcohol was acylated in parallel with a series of differently substituted benzoic acid derivatives. Treatment with TFA-CH2Cl2 (5:995) released the expected saphenamycin analogues into solution. These new analogues were purified, characterized and screened for antimicrobial activity against Bacillus subtilis and Proteus mirabilis. Eight analogues exhibited MIC values against B. subtilis ranging from 0.07 to 3.93 μg/mL, comparable to the activities of previously reported saphenamycin analogues.

Benzamide derivatives

Benzamide derivatives of the formula:- STR1 wherein R1 represents a fluorine, chlorine or bromine atom, or an alkyl, alkoxy, alkylthio, alkylsulphonyl, alkanoylamino, alkylamino or alkylsulphamoyl group, each such group containing from 1 to 6 carbon atoms, a dialkylsulphamoyl, dialkylamino or dialkylcarbamoyl group (wherein the two alkyl groups may be the same or different and each contains from 1 to 4 carbon atoms), an alkanoyl, alkoxycarbonyl, alkoxycarbonylamino or alkylcarbamoyl group containing from 2 to 6 carbon atoms, or a hydroxy, formyl, nitro, trifluoromethyl, aryl, benzyloxycarbonylamino, amino, sulphamoyl, cyano, tetrazol-5-yl, carboxy, carbamoyl or aroyl group, and n represents an integer 1, 2 or 3, are new compounds possessing pharmacological properties, in particular properties of value in the treatment of respiratory disorders manifested by the interaction of tissue-fixed antibodies with specific antigens.