863719-46-4

Upstream product

• 100-61-8 N-methylaniline 
• 7693-52-9 4-bromo-2-nitrophenol 
• 40925-68-6 2-amino-4-bromo-phenol 
• 863724-27-0 tert-butyl (5-bromo-2-oxo-1,3-benzoxazol-3(2H)-yl)acetate 
• 14733-73-4 5-bromo-1,3-benzoxazol-2(3H)-one 

Downstream Products

• 1396795-88-2 N-methyl-2-{2-oxo-5-[4-(trifluoromethyl)phenyl]-1,3-benzoxazol-3(2H)-yl}-N-phenylacetamide 
• 863724-60-1 N-methyl-2-[2-oxo-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1,3-benzoxazol-3(2H)-yl]-N-phenylacetamide 
• 1534370-72-3 2-[5-{2-[(dimethylamino)methyl]phenyl}-2-oxo-1,3-benzoxazol-3(2H)-yl]-N-methyl-N-phenylacetamide 
• 1534370-73-4 2-[5-{4-[(dimethylamino)methyl]phenyl}-2-oxo-1,3-benzoxazol-3(2H)-yl]-N-methyl-N-phenylacetamide 
• 1534370-74-5 N-methyl-2-[5-(2-methylpyridin-3-yl)-2-oxo-1,3-benzoxazol-3(2H)-yl]-N-phenylacetamide 

Relevant academic research and scientific papers

Development of a18F-Labeled Radiotracer with Improved Brain Kinetics for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Ischemic Brain and Glioma

We designed four novel acetamidobenzoxazolone compounds 7a-d as candidates for positron emission tomography (PET) radiotracers for imaging the translocator protein (18 kDa, TSPO) in ischemic brain and glioma. Among these compounds, 2-(5-(6-fluoropyridin-3-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-N-methyl-N-phenylacetamide (7d) exhibited high binding affinity (Ki = 13.4 nM) with the TSPO and moderate lipophilicity (log D = 1.92). [18F]7d was radiosynthesized by [18F]fluorination of the bromopyridine precursor 7h with [18F]F- in 12 ± 5% radiochemical yield (n = 6, decay-corrected). In vitro autoradiography and PET studies of ischemic rat brain revealed higher binding of [18F]7d with TSPO on the ipsilateral side, as compared to the contralateral side, and improved brain kinetics compared with our previously developed radiotracers. Metabolite study of [18F]7d showed 93% of unchanged form in the ischemic brain at 30 min after injection. Moreover, PET study with [18F]7d provided a clear tumor image in a glioma-bearing rat model. We demonstrated that [18F]7d is a useful PET radiotracer for visualizing not only neuroinflammation but also glioma and will translate this radiotracer to a “first-in-human” study in our facility.

Convenient synthesis of benzoxazolone derivatives by cross-coupling of benzoxazolone boronates with aryl halides

Benzoxazolone derivatives with various substituents at the C-5 position were synthesized efficiently via benzoxazolone boronates as the key intermediate. The target compounds were also synthesized from (het)aryl halides in a one-pot process. These methods permitted efficient exploratory syntheses of a series of benzoxazolone derivatives. Georg Thieme Verlag Stuttgart New York.

Design, synthesis and structure-activity relationships of novel benzoxazolone derivatives as 18 kDa translocator protein (TSPO) ligands

Selective 18 kDa translocator protein (TSPO) ligands are expected to be therapeutic agents with a wide spectrum of action on psychiatric disorders and fewer side effects. We designed novel benzoxazolone derivatives and examined the structure-activity rela

NOVEL HETEROCYCLIC COMPOUND

A drug having a high affinity for benzodiazepine ω3 receptors and showing curative and preventive effects for anxiety and depression, which comprises as the active ingredient, for example, a compound of the formula (1): wherein R1 an