864863-72-9

Basic information

• Product Name: FPTQ
• Synonyms: FPTQ;6-[1-(2-fluoropyridin-3-yl)-5-methyltriazol-4-yl]quinoline
• CAS NO: 864863-72-9
• Molecular Formula: C17H12FN5
• Molecular Weight: 305.3090832
• Mol File: 864863-72-9.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: FPTQ(CAS DataBase Reference)
• NIST Chemistry Reference: FPTQ(864863-72-9)
• EPA Substance Registry System: FPTQ(864863-72-9)

Safety Data

• Hazardous Substances Data: 864863-72-9(Hazardous Substances Data)

Upstream product

• 5332-25-2 6-bromoquinoline 
• 864866-09-1 1-(2-fluoro-3-pyridyl)-5-methyl-4-(tri-n-butylstannyl)-1H-1,2,3-triazole 
• 372-48-5 2-fluoropyridine 
• 864866-10-4 3-azido-2-fluoropyridine 
• 173089-80-0 quinolin-6-yl triflate 
• 580-16-5 6-hydroxyquinoline 

Relevant articles and documents

Synthesis and evaluation of 6-[1-(2-[18F]fluoro-3-pyridyl)-5- methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain

The purpose of this study was to synthesize 6-[1-(2-[18F]fluoro- 3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline ([18F]FPTQ, [18F]7a) and to evaluate its potential as a positron emission tomography ligand for imaging metabotropic glutamate receptor type 1 (mGluR1) in the rat brain. Compound [18F]7a was synthesized by [ 18F]fluorination of 6-[1-(2-bromo-3-pyridyl)-5-methyl-1H-1,2,3- triazol-4-yl]quinoline (7b) with potassium [18F]fluoride. At the end of synthesis, 1280-1830 MBq (n = 8) of [18F]7a was obtained with >98% radiochemical purity and 118-237 GBq/μmol specific activity using 3300-4000 MBq of [18F]F-. In vitro autoradiography showed that [18F]7a had high specific binding with mGluR1 in the rat brain. Biodistribution study using a dissection method and small-animal PET showed that [18F]7a had high uptake in the rat brain. The uptake of radioactivity in the cerebellum was reduced by unlabeled 7a and mGluR1-selective ligand JNJ-16259685 (2), indicating that [18F]7a had in vivo specific binding with mGluR1. Because of a low amount of radiolabeled metabolite present in the brain, [18F]7a may have a limiting potential for the in vivo imaging of mGluR1 by PET.

DIARYL-SUBSTITUTED FIVE-MEMBERED HETEROCYCLE DERIVATIVE

The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X 1 represents oxygen atoms and the like, X 2 represents nitrogen atoms and the like, X 3 represents nitrogen atoms and the like, X 4 represents nitrogen atoms and the like, R 1 represents formula (II-1): wherein X 5 represents sulfur atoms and the like, A 1 represents carbon atoms and the like, A 2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being usefull for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.