WO2010033074 Use of a TLR7 agonist for the treatment of cancer

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Biological target:

Toll-like receptor 7: TLR7

Activity:

Agonist

Steps Conditions Reactions
a

1. Butylamine / DIEA

2. TFA / MeOH  

Secondary amine deprotection (nucleophilic substitution) / THP deprotection
b 2-chloro-5-chloromethylpyridine / K2CO3  / DMF Nucleophilic substitution
c

1. Br2 / CHCl3:MeOH 100:1 

2. HCl 12N 

Oxidation
d Dimethylaminoethanol / NaH / dioxane Ether synthesis (nucleophilic substitution)