1-[(Pyridin-3-yl)methyl]piperazine → [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-phenyl]-(4-pyridin-3-ylmethyl-piperazin-1-yl)-methanone

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 (54 mg) and 1-pyridin-3-ylmethyl-piperazine (22 mg) obtained in Step A in Example 1-D-315 instead of 3-(aminomethyl)pyridine used in Step B in Example 1-D-19, treatment was carried out 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)-3-fluoro-phenyl]-(4-pyridin-3-ylmethyl-piperazin-1-yl)-methanone, and then the PMB groups were removed according to the above Deprotection method 3, to obtain the desired compound (D-315) as a yellow powder (32.0 mg, 83%).

Provenance & Evidence