反应详情

4-(2-Tert-butoxycarbonylamino-ethyl)-benzoic acid was reacted with WSCI, HOBt, triethylamine and N-methylpiperazine in dichloromethane, to obtain {2-[4-(4-methyl-piperazine-1-carbonyl)-phenyl]-ethyl}-carbamic acid tert-butyl ester, and then it was reacted with sodium hydride and methyl iodide in DMF, to obtain a crude product of methyl-{2-[4-(4-methyl-piperazine-1-carbonyl)-phenyl]-ethyl}-carbamic acid tert-butyl ester. Then, this was treated with TFA, to obtain [4-(2-methylamino-ethyl)-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-(2-methylamino-ethyl)-phenyl]-(4-methyl-piperazin-1-yl)-methanone (211 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-{2-[4-(4-methyl-piperazine-1-carbonyl)-phenyl]-ethyl}-amide was obtained, and then the PMB groups were removed according to the above Deprotection method 3, to obtain the desired compound (D-295) as a colorless powder (26 mg, 24%).