WO2010040661 Modulators for amyloid beta

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Scaffold: triazine

Biological target:

gamma-secretase

Activity:

Inhibitor

Steps Conditions Reactions
a KOH / DMSO Tertiary amine synthesis (aromatic substitution)
b H2 / Pd-C / EtOH Primary amine synthesis (nitro reduction)
c

Pd(AcO)2 / dicyclophosphine / K2CO3 / Dioxane

Buchwald-hartwig amination
Steps Conditions Reactions
a K2CO3 / ACN Ether synthesis (nucleophilic substitution)
Steps Conditions Reactions
a dimethylzinc  / toluene / dioxane Negishi coupling
b Pd(AcO)2 / dicyclophosphine / K2CO3 / Dioxane
Buchwald-hartwig amination
Steps Conditions Reactions
a Pd2(dba)3 / CO / Et3N / AcOEt / MeOH Ester synthesis
b MeMgBr / THF Grignard reaction
Steps Conditions Reactions
a

1. Mg / Et2O

2. Cyanuric chloride / toluene

Negishi coupling
b Et3N / MeOH Secondary amine synthesis (nucleophilic substitution)

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