Methyl(2-(morpholin-4-yl)ethyl)amine → 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-methyl-N-(2-morpholin-4-yl-ethyl)-benzamide

関与物質

反応手順

Using methyl-(2-morpholin-4-yl-ethyl)-amine (29.8 mg, 0.206 mmol) obtained in Step A instead of 3-(aminomethyl)pyridine, and 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 (68.1 mg, 0.103 mmol) obtained in Step A in Example 1-D-19, in the same manner as Step B in Example 1-D-19, amidation was carried out, 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-methyl-N-(2-morpholin-4-yl-ethyl)-benzamide as a yellow solid (70.2 mg), and then the PMB groups were removed according to the above Deprotection method 3, to obtain the desired compound (D-139) as a yellow powder (42.0 mg, 75%).

情報源と証拠