1,2-Ethanediamine, N1,N1,N2-trimethyl- → N-[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)-pyridin-2-yl]-N,N',N'-trimethyl-ethane-1,2-diamine

Participants

Reaction Steps

Using {5-[7-(2-chloro-pyridin-4-yl)-2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrimidin-2-yl}-bis-(4-methoxy-benzyl)-amine (100 mg, 0.154 mmol) obtained in Step A in Example 1-D-69 instead of {5-[7-(6-chloro-pyridin-3-yl)-2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrimidin-2-yl}-bis-(4-methoxy-benzyl)-amine, and N,N,N′-trimethyl ethylenediamine (30 μl, 0.23 mmol), in the same manner as Example 1-D-48, amination was carried out, to obtain a crude product of N-[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)-pyridin-2-yl]-N,N′,N′-trimethyl-ethane-1,2-diamine as a dark brown solid (55 mg), and then the PMB groups were removed according to the above Deprotection method 2, to obtain the desired compound (D-74) as a yellow powder (25 mg, 68%).

Provenance & Evidence