9-Bromo-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
9-Bromo-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine
Nonfluorochemicals, API&Intermediates
KUMI0F299
1282516-67-9
MFCD22372760

Rea
58204906

Reax
21256804
image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
9-Bromo-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine
C11H9BrN2O
265.11
98%
Light Yellow to Yellow Solid
121°C
5g,10g,25g,50g,100g,250g,500g,1kg and 25kg
Store at room temperture
9-Bromo-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine is a useful intermediate that typcially used in the preparation of GDC-0077 as a potent and selective PI3K inhibitor with potential antineoplastic activity for the treatment of breast cancer, and GDC-0032 as a PI3K β-Sparing Inhibitor for the treatment of metastatic breast cancer and non-small cell lung cancer.
GDC-0077 is a selective PI3K alpha inhibitor that demonstrates robust efficacy in PIK3CAmutant breast cancer models as a single agent and in combination with standard of care therapies. [1]
Manufacture of the PI3K β-Sparing Inhibitor Taselisib. Part 1: Early-Stage Development Routes to the Bromobenzoxazepine Core. [2]
Synthesis of PI3K inhibitor GDC-0077 via a stereocontrolled N-arylation of α-amino acids. [3]
References:
[1] R.Hong, et al, Cancer Res., 2018, 78(4), .
[2] T.Remarchuk, et al, Org. Process Res. Dev., 2019, 23(5), pp 775-782.
[3] C.Han, et al, Tetrahedron, 2019, 75(32), pp 4351-4352.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Warning
H315,H319,H335
P261,P305+P351+P338
2934990300
NONH for all modes of transport

1. Product Specification
2. Safety Data Sheet
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