WO2010034656 Isoxazolo[4,5]pyridin-3-yl-piperazin derivatives useful as modulators of dopamine D3 receptors

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Scaffold: piperazine

Biological target:

Dopamine receptor: D3

Activity:

Agonist

Steps Conditions Reactions
a NH2-OH / EtOH / H2O Imine synthesis
b

1. NCS / ACN

2. tert-Butyl 1-piperazinecarboxylate / Et3N / DCM

Chlorination / Tertiary amine synthesis (nucleophilic substitution)
c KOH aq / Dioxane  Cyclisation
d HCl 4N / Dioxane / DCM Boc deprotection
e Na(AcO)3BH / Et3N / DCM Tertiary amine synthesis (Reductive amination)
f HCl 4N / Dioxane / DCM Boc deprotection
g AcOH / TBTU / DIEA / Dioxane Amide synthesis (TBTU coupling)

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