1391001-77-6

Basic information

• Product Name: N-(3-((4aS,5S,7aS)-2-amino-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide
• Synonyms: N-(3-((4aS,5S,7aS)-2-amino-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide
• CAS NO: 1391001-77-6
• Molecular Weight: 435.454
• Mol File: 1391001-77-6.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: N-(3-((4aS,5S,7aS)-2-amino-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(3-((4aS,5S,7aS)-2-amino-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide(1391001-77-6)
• EPA Substance Registry System: N-(3-((4aS,5S,7aS)-2-amino-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide(1391001-77-6)

Safety Data

• Hazardous Substances Data: 1391001-77-6(Hazardous Substances Data)

Upstream product

• 1391001-95-8 tert-butyl ((4aS,5S,7aS)-7a-(2-fluoro-5-(5-methoxypyrazine-2-carboxamido)phenyl)-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-2-yl)carbamate 
• 1391001-93-6 N-(((3S,4R,5S)-5-(fluoromethyl)-3-(2-fluorophenyl)-4-(hydroxymethyl)tetrahydrofuran-3-yl)carbamothioyl)benzamide 
• 1391001-92-5 ((2S,3R,4S)-4-amino-2-(fluoromethyl)-4-(2-fluorophenyl)tetrahydrofuran-3-yl)methanol 
• 1391001-91-4 (3aR,4S,6aS)-4-(fluoromethyl)-6a-(2-fluorophenyl)hexahydrofuro[3,4-c]isoxazole 
• 1391001-89-0 (S)-2-((1-fluorobut-3-en-2-yl)oxy)-1-(2-fluorophenyl)ethanone 
• 1391001-88-9 (S)-2-((1-fluorobut-3-en-2-yl)oxy)-N-methoxy-N-methylacetamide 
• 1391001-87-8 tert-butyl (S)-2-((1-fluorobut-3-en-2-yl)oxy)acetate 
• 1174321-90-4 tert-butyl ((4aS,5S,7aS)-7a-(5-amino-2-fluorophenyl)-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-2-yl)carbamate 
• 40155-42-8 5-methoxy-pyrazine-2-carboxylic acid 
• 36070-80-1 5-chloropyrazinoic acid 

Relevant articles and documents

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Alzheimer's disease (AD) is characterized by accumulation of β-amyloid (Aβ) plaques and neurofibrillary tau tangles in the brain. β-Site amyloid precursor protein cleaving enzyme 1 (BACE1) plays a key role in the generation of Aβ fragments via extracellular cleavage of the amyloid precursor protein (APP). We became interested in developing a BACE1 PET ligand to facilitate clinical assessment of BACE1 inhibitors and explore its potential in the profiling and selection of patients for AD trials. Using a set of PET ligand design parameters, compound 3 (PF-06684511) was rapidly identified as a lead with favorable in vitro attributes and structural handles for PET radiolabeling. Further evaluation in an LC-MS/MS cold tracer study in rodents revealed high specific binding to BACE1 in brain. Upon radiolabeling, [18F]3 demonstrated favorable brain uptake and high in vivo specificity in nonhuman primate (NHP), suggesting its potential for imaging BACE1 in humans.

FUSED AMINODIHYDROTHIAZINE DERIVATIVES

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