WO2010010133 2-thia-1,3-diazaspirocyclic substituted phenylacetamides as GLT1 mediators for neurological diseases

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Biological target:

Sodium- and chloride-dependent glycine transporter 1: GLT1

Activity:

Inhibitor

Steps Conditions Reactions
a

1. HATU / DIEA / DMF

2. HCl 4N / dioxane

Amide synthesis (HATU coupling) / Boc deprotection
b Borane-tetrahydrofuran / THF Secondary amine synthesis (amide reduction)
c

Sulfonamide / pyridine 

Cyclisation
d K2CO3  / tetrabutylammonium iodide / acetone Nucleophilic substitution

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