WO2010056195 New compounds 575

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Biological target:

β-Secretase: BACE

Activity:

Inhibitor

l

Steps Conditions Reactions
a

i). PPh3, DIAD, THF, 0oC

ii). NaOH 3M, 50oC, 2h

Mitsunobu reaction  

Saponification

b Oxalyl chloride, CH2Cl2, DMF, 3h Benzoyl chloride formation
c

i). Rieke(R) Zinc, THF

ii). CuCN(LiBr)2 1M in THF

Zincate formation
d
 		Ti(IV) ethoxide, THF, reflux, 42h
e

i). t-BuLi, THF, -100oC, 40min

ii). HCl 1N in diethyl ether, MeOH, 3h

 

Cyclization