Isopropanol → 2-(4-((4-(((7R,8aS)-5,5-dimethyloctahydroindolizin-7-yl)amino)-5-fluoropyrimidin-2-yl)amino)-2-fluorophenoxy)ethan-1-ol

Participants

Reaction Steps

The general displacement procedure described herein was used with 4-(2-((tert-butyldimethyl)silyl)oxy)ethoxy)-3-fluoroaniline (285 mg, 1.0 mmol), (7R,8aS)-N-(2-chloro-5-fluoropyrimidin-4-yl)-octahydro-5,5-dimethylindolizin-7-amine hydrochloride (336 mg, 1.0 mmol) and pTsOH.H2O (381 mg, 2.0 mmol) in IPA (10 mL) at reflux to give the product (143 mg, 33% yield) as a solid, after workup and purification by column chromatography on silica gel using DCM/2M NH3 in MeOH (1:0 to 9:1) as eluent.

Provenance & Evidence