Diisopropylethylamine → N-{3-[(2,5-dichloro-pyrimidin-4-ylamino)-methyl]-pyridin-2-yl}-N-methyl-methanesulphonamide

関与物質

反応条件

反応手順

2,4,5-trichloropyrimidine (1.0 g, 5.45 mmol) is suspended in 20 mL DCM and the reaction mixture is cooled to 0° C. Then a solution of N-(3-aminomethyl-pyridin-2-yl)-N-methyl-methanesulphonamide (1.17 g, 5.45 mmol) and DIPEA (1.95 mL, 10.9 mmol) in 10 mL DCM is added and the mixture is stirred overnight. The reaction mixture is diluted with DCM and washed 3× with 1 N NH4Cl solution. The organic phase is dried on magnesium sulphate and evaporated down in vacuo. The crude product A-2b (HPLC-MS: tRet.=2.00 min; MS (M+H)+=362) is used in successive reactions without further purification.

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