The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising compounds of formu
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(2020/12/29)
Catalytic N-Dealkylation of Tertiary Amines--A Biomimetic Oxygenation Reaction
A heterogeneous catalyst system is described for N-dealkylation of tertiary amines.A large number of tertiary amines including some important synthetic drugs were N-dealkylated to give the corresponding secondary amines in 50-65percent yields.The reaction was carried out at room temperature by stirring a solution of a tertiary amine in methanol containing 10percent palladium-on-charcoal catalyst.The reaction had absolute requirement for molecular oxygen like the enzymatic dealkylation reaction.It also needed methanol to act as the reductant of molecular oxygen like the NADPH in the enzymatic reaction.A catalytic cycle similar to cytochrome P-450-catalysed oxygenation cycle is proposed for activation and transfer of oxygen to the α-carbon of tertiary amines to give unstable carbinolamines which on dissociation yield secondary amines.