WO2010056196 New compounds 578

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Biological target:

β-Secretase: BACE

Activity:

Inhibitor

l

Steps Conditions Reactions
a Oxalyl chloride, CH2Cl2, DMF, overnight Benzoyl chloride formation
b CuCN(LiBr) in THF, -78oC
c
 		Ti(IV) ethoxide, THF, reflux, 22h
d

i). THF, 0oC

ii). HCl 2N in diethyl ether, MeOH, 2.5h

Cyclization
e
 		PdCl2(dppf), K2CO3, DMF, microwaves 150oC, 15min Suzuki cross coupling reaction