WO2010132598: Heteroaryl Compounds as PIKK Inhibitors

Biological target:

PI3 kinase or mTOR

Activity:

Inhibitor

WO2010132589.pdf
Adobe Acrobat Document 17.2 MB
Steps Conditions Reactions
a
CH3MgBr, CH2Cl2, 0oC Grignard reaction
b

1. Sodium trimethoxide, THF, 2h

2. NH2NH2, Et3N, reflux 4h

SNAr
c
iPrOH, 100oC, 15h Pyrazole formation
d
X-Phos, Pd2(dba)3, tBuOH, H2O, 100oC then Cs2CO3, 120oC, 2.5h Buchwald-Hartwig amination
e

1. m-CPBA, CH2Cl2, 0oC, 1h

2. NH4OH, iPrOH, 120oC, 40 min
S-oxidation, SNAr

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