Ethylenediamine → N-(2-Amino-ethyl)-3-[(5,7-diamino-pyrimido[4,5-d]pyrimidin-2-yl)-(2-ethoxy-naphthalen-1-ylmethyl)-amino]-2-hydroxy-propionamide

Participants

Reaction Steps

To 3-[(5,7-diamino-pyrimido[4,5-d]pyrimidin-2-yl)-(2-ethoxy-naphthalen-1-ylmethyl)-amino]-2-hydroxy-propionic acid (200 mg, 0.445 mmol) in dry DMF (2 ml) was added BroP (249 mg, 0.534 mmol). After the mixture was stirred for 30 min, DIEA (126 mg, 0.979 mmol) was added. After stirring for another 20 min, ethylene diamine (53.5 mg, 0.89 mmol) was added. The mixture was then stirred at room temperature for 16 hours and was directly purified by prep HPLC to yield 35 mg (16%) of the title compound: MS m/z (M+H) 492.

Provenance & Evidence