1-(2-Hydroxyethyl)piperazine → HCID 67386040, compound

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)-3-fluoro-benzoic acid (70.4 mg, 0.104 mmol) obtained in Step A in Example 1-D-21 and 1-piperazineethanol (25.5 μl, 0.208 mmol) instead of 1-pyridine-3-yl-piperazine, amidation was carried out in the same manner as Step B in Example 1-D-21, 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]-phenyl}-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-methanone as a yellow solid (83.2 mg), and then the PMB groups were removed according to the above Deprotection method 3, to obtain the desired compound (D-145) as a yellow powder (24.5 mg, 43%).

Provenance & Evidence