Isopropyl chloroformate → 4-[6-(5-Methanesulfonyl-2,3-dihydro-indol-1-yl)-pyrimidin-4-yl-methylamino]-piperidine-1-carboxylic acid isopropyl ester

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Reaction Steps

7d was dissolved in DCM (1 mL) and triethylamine (0.1 mL, 14 eq) was added. Isopropyl chloroformate (0.1 mL of a 1 M solution in toluene, 2 eq) was added and the reaction mixture was stirred at room temperature for 17 h. The solution was evaporated and purified by preparative HPLC to give 7-1; LC-MS 474.0 (MH+), tR=5.21 (Method 5). EC50: 69 nM.

Provenance & Evidence