Trimethylsilyl iodide → N-(((R)-1-(4-aminobutanoyl)pyrrolidin-2-yl)methyl)-6-(2-cyanophenyl)-2-(2-(tetrahydro-2H-pyran-2-yl)ethylamino)nicotinamide

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Reaction Steps

To a solution of benzyl 4-((R)-2-((6-(2-cyanophenyl)-2-(2-(tetrahydro-2H-pyran-2-yl)ethylamino)nicotinamido)methyl)pyrrolidin-1-yl)-4-oxobutylcarbamate (47 mg, 0.072 mmol) in MeCN (1 mL) at 0° C. was added TMSI (72 mg, 0.36 mmol). The mixture was stirred at room temperature for 2 hrs and purified on RP-HPLC using a mixture of acetonitrile and H2O to give N—(((R)-1-(4-aminobutanoyl)pyrrolidin-2-yl)methyl)-6-(2-cyanophenyl)-2-(2-(tetrahydro-2H-pyran-2-yl)ethylamino)nicotinamide (36 mg, 77%). LRMS (M+H+) m/z 519.3.

Provenance & Evidence