N-(3-Aminopropyl)morpholine → 4-[4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl]-N-(3-morpholin-4-yl-propyl)-benzamide

Participants

Reaction Steps

Using 4-(4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl)-benzoic acid (50.0 mg, 0.0758 mmol) obtained in Step A in Example 1-D-19 and N-(3-aminopropyl)morpholine (22.1 μl, 0.152 mmol) instead of 3-(aminomethyl)pyridine, amidation was conducted in the same manner as Step B in Example 1-D-19, to obtain a crude product of 4-[4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl]-N-(3-morpholin-4-yl-propyl)-benzamide as a yellow solid (44.8 mg), and then the PMB groups were removed according to the above Deprotection method 2, to obtain the desired compound (D-93) as a yellow powder (29.3 mg, 71%).

Provenance & Evidence