WO2010108074 INHIBITORS OF PI3 KINASE

Biological target:

PI3 kinase

Activity:

Inhibitor

WO2010108074.pdf
Adobe Acrobat Document 10.1 MB
Steps Conditions Reactions
a
Chloroacetone, DMSO, 1day Cyclization (Imidazopyridine formation)
b Br2, AcOH Bromination
c
Pyridine, 1day Sulfonylation
d
(PdCl2(dppf).CH2Cl2), KOAc, dioxane, 120oC, 15min then K2CO3, 100oC, 1h Suzuki cross coupling reaction
e
Pd(PPh3)4, 2M Na2CO3, dioxane, 100oC, 5h Suzuki cross coupling reaction
Steps Conditions Reactions
a
Pyridine, 1day Sulfonylation
b (PdCl2(dppf).CH2Cl2), KOAc, dioxane, sealed tube, 80oC, 2h Suzuki cross coupling reaction
c
Pd(PPh3)4, Cs2CO3, DME/H2O, 80oC, 1h Suzuki cross coupling reaction
Steps Conditions Reactions
a
K2CO3, DMF, microwave vial, 3 days N-benzylation
b Microwave vial, EtOH, 100oC, 4h Pyrimidone formation
c
Iodine, NaOAc, microwave vial, 0oC to room temperature, 1h Iodination
d (PdCl2(dppf).CH2Cl2), K2CO3, dioxane, microwaves, 80oC 10min then 100oC 10min Suzuki cross coupling reaction

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