N3-(4-methoxybenzoyl)-3,4-pyridinediamine → N4-[2-(1-tert-Butoxycarbonylpiperidin-4-yloxy)-4-tert-butylbenzoyl]-N3-(4-methoxybenzoyl)-3,4-pyridinediamine

Participants

Reaction Steps

Using methods substantially equivalent to those described in Example 101-D, 2-(N-Boc-piperidine-4-yloxy)-4-(tert-butyl)benzoic acid (1.0 g, 2.65 mmol) is converted into the acid chloride and used to acylate N3-(4-methoxybenzoyl)-3,4-pyridinediamine (600 mg, 2.47 mmol). After purification by chromatography (SiO2: 30% to 50% EtOAc in chloroform) 589 mg (40%) of the title compound is obtained.

Provenance & Evidence