Methyl iodide → Methanone, [4-[(methylamino)methyl]phenyl](4-methyl-1-piperazinyl)-

Participants

Reaction Steps

A crude product of [4-(4-methyl-piperazine-1-carbonyl)-benzyl]-carbamic acid tert-butyl ester obtained in Example 1-D-293, sodium hydride and methyl iodide were treated in DMF, and further treated with TFA, to obtain (4-methylaminomethyl-phenyl)-(4-methyl-piperazin-1-yl)-methanone. Using bis-(4-methoxy-benzyl)-[5-(2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)-pyrimidin-2-yl]-amine (100 mg) and (4-methylaminomethyl-phenyl)-(4-methyl-piperazin-1-yl)-methanone (126 mg) instead of 4-(4-ethyl-piperazin-1-yl)-2,6-difluoro-phenylamine used in Step D in Example 1-D-18, in the same manner as Step D in Example 1-D-18, a crude product of 4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid methyl-[4-(4-methyl-piperazine-1-carbonyl)-benzyl]-amide was obtained, and then the PMB groups were removed according to the above Deprotection method 3, to obtain the desired compound (D-297) as a colorless powder (6 mg, 6%).

Provenance & Evidence