870846-02-9

Upstream product

• 403-40-7 1-(4-fluorophenyl)ethylamine 
• 1160359-86-3 5-chloro-N-(1-(4-fluorophenyl)ethyl)pentanamide 
• 1160359-87-4 1-[1-(4-fluorophenyl)ethyl]piperidin-2-one 
• 19347-73-0 6-chlorohexanoyl chloride 
• 1119-46-6 5-chloro-valeric acid 
• 1160359-88-5 1-[1-(4-fluorophenyl)ethyl]-3-{hydroxy[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methyl}piperidin-2-one 
• 870837-18-6 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde 
• 937026-11-4 1-[(S)-1-(4-fluorophenyl)ethyl]piperidin-2-one 
• 870843-43-9 (3E)-5-chloro-2-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]valeric acid [(S)-1-(4-fluorophenyl)ethyl]amide 
• 937026-15-8 1-[(S)-1-(4-fluorophenyl)ethyl]-3-{chloro[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methyl}piperidin-2-one 
• 937026-13-6 1-[(S)-1-(4-fluorophenyl)ethyl]-3-{hydroxy[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methyl}piperidin-2-one 
• 937026-29-4 acetic acid {1-[(1S)-1-(4-fluorophenyl)ethyl]-2-oxopiperidin-3-yl}[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]methyl ester 
• 937026-24-9 1-[(S)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzoyl]piperidin-2-one 
• 937026-23-8 1-[(S)-1-(4-fluorophenyl)ethyl]-2-oxo-piperidine-3-carboxylic acid 

Relevant academic research and scientific papers

GAMMA SECRETASE MODULATORS FOR THE TREATMENT OF ALZHEIMER ' S DISEASE

This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I

SALTS OF CYNNAMIDE COMPOUND OR SOLVATES THEREOF

The invention provides crystals of dihydrochloride monohydrate of the compound of the following formula having an Aβ production inhibiting effect which crystals are characterized by exhibiting a diffraction peak at an angle of diffraction (2θ ± 0.2°) of 10.9° in powder X-ray diffractometry. Further, the invention also provides the compound in the form of various salts, crystal forms and amorphous forms which are suitable for the development of drugs.

ONE-POT METHODS FOR PREPARING CINNAMIDE DERIVATIVES

A compound represented by the following formula (1): wherein R represents a 4-fluorophenyl group and the like; Q represents —CH(CH3)— and the like; and n represents 1 and the like and a pharmaceutically acceptable salt thereof can be prepared in one-pot by reacting a compound represented by the following formula (2): wherein R1 represents a 4-fluorophenyl group and the like; and Q and n have the same meaning as described above, with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base and, if necessary, removing a protecting group.

PROCESS FOR PRODUCTION OF CINNAMAMIDE DERIVATIVE

A compound (8) represented by the formula: (8) wherein R1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2, can be produced with good efficiency by reacting a compound (3) represented by the formula: (3) wherein R1 and n are as defined above; and Q represents a single bond or -CH(Y)- where Y represents a hydrogen atom or a C1-6 alkyl group] with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base.