1266786-47-3

Upstream product

• 2142-63-4 1-(3-Bromophenyl)ethanone 
• 953741-63-4 rac-2-amino-2-(3-bromo-phenyl)-propionitrile 
• 1394137-79-1 (S)-N-((R)-2-(3-bromophenyl)-1-(tert-butyldiphenylsilyloxy)propan-2-yl)-2-methylpropane-2-sulfinamide 
• 1394137-71-3 (R)-5-[3-(benzhydrylideneamino)phenyl]-5-methyl-2,6-dihydro-2H-1,4-oxazin-3-amine 
• 1266784-04-6 (R)-(+)-N-[1-(3-bromo-phenyl)-2-hydroxy-1-methyl-ethyl]-2-chloro-acetamide 
• 7399-36-2 rac-2-amino-2-(3-bromophenyl)-propionic acid 
• 1352419-24-9 (R)-5-(3-bromophenyl)-5-methyl-5,6-dihydro-2H-1,4-oxazin-3-amine 
• 1352419-23-8 (5R)-5-(3-bromophenyl)-5-methylmorpholine-3-thione 
• 1213181-85-1 (2R)-2-amino-2-(3-bromophenyl)-propan-1-ol 
• 1266785-37-8 (5R)-5-(3-bromophenyl)-5-methyl-morpholin-3-one 
• 1183581-39-6 (RS)-2-amino-2-(3-bromo-phenyl)-propionic acid methyl ester 
• 1183013-69-5 (RS)-2-amino-2-(3-bromo-phenyl)-propan-1-ol 
• 86873-60-1 5-chloropicolinic acid 
• 1352419-25-0 (5R)-5-(3-aminophenyl)-5-methyl-5,6-dihydro-2H-1,4-oxazin-3-amine 

Relevant academic research and scientific papers

1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads

1,4-Oxazines are presented, which show good in vitro inhibition in enzymatic and cellular BACE1 assays. We describe lead optimization focused on reducing the amidine pKa while optimizing interactions in the BACE1 active site. Our strategy permi

A practical entry to β-aryl-β-alkyl amino alcohols: Application to the synthesis of a potent BACE1 inhibitor

The 1,2-addition of alkyl Grignard reagents to readily available N-tert-butanesulfinyl ketimines, bearing an α-silyloxy substituent, proceeds in high yields and excellent diastereocontrol. The utility of the present method was demonstrated by the synthesi

5,6-DIHYDRO-2H-[1,4]OXAZIN-3-YL-AMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta- amyloid.

3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINES

The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. T

3-AMINO-5-PHENYL-5,6-DIHYDRO-2H-[1,4]OXAZINE DERIVATIVES

The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[l,4]oxazine derivatives of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active