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. 
Manufacture of the PI3K β-Sparing Inhibitor Taselisib. Part 1: Early-Stage Development Routes to the Bromobenzoxazepine Core. 
Synthesis of PI3K inhibitor GDC-0077 via a stereocontrolled N-arylation of α-amino acids. 
 R.Hong, et al, Cancer Res., 2018, 78(4), DOI: 10.1158/1538-7445.
 T.Remarchuk, et al, Org. Process Res. Dev., 2019, 23(5), pp 775-782.
 C.Han, et al, Tetrahedron, 2019, 75(32), pp 4351-4352.
NONH for all modes of transport
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