WO2010126895: Inhibitors of PI3 Kinase and/or mTOR

Biological target:

PI3 kinase or mTOR

Activity:

Inhibitor

WO2010126895.pdf
Adobe Acrobat Document 57.3 MB
Steps Conditions Reactions
a
NBS, (PhCO2)2, CCl4, reflux 2h Bromination
b K2CO3, DMF Nucleophilic substitution
c

1. LDA, B(OiPr)3,

2. 1M NaOH aq.

Boronic acid formation
d
Pd(PPh3)4, Na2CO3, dioxane/H2O, 80oC, overnight Suzuki cross coupling reaction
e

1. TFA, CH2Cl2, 1h

2. MeSO2Cl, Et3N, CH2Cl2

Boc-deprotection,  N-acylation
f

1. Raney-Ni, EtOH, 70oC

2. 1M LiHMDS, THF

SNAr
g

1. 1M LiHMDS, 3-amino-6-methoxypyridine, THF, -10oC

2. 2M NH3 in 2-propanol, tube sealed, 90oC overnight

SNAr

Primary amine formation

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