Chloroform → (R)-2-(2-benzyl-1H-imidazol-1-yl)-8-cyclopentyl-7-ethyl-5-methyl-7,8-dihydropteridin-6(5H)-one

関与物質

反応条件

反応手順

(R)-2-(2-bromo-1H-imidazol-1-yl)-8-cyclopentyl-7-ethyl-5-methyl-7,8-dihydropteridin-6(5H)-one (Example 65, 0.21 g, 0.518 mmol), Pd2(dba)3, CHCl3 (53 mg, 0.0518 mmol) and biphenyl-2-yldi-tert-butylphosphine (30 mg, 0.103 mmol) were placed in a screw cap vial and a solution of benzyl zinc bromide (1.5 mL, 0.777 mmol in THF) was added. A stream of nitrogen was bubbled through the mixture for 2 minutes and then the vial was sealed and the resulting solution was stirred at 90° C. for 18 h. The reaction mixture was filtered, then purified by flash chromatography with a silica gel column by eluting with a mixture of Hexane:EtOAc and then further purified by preparative HPLC to give the title compound (126 mg). LCMS: 417.2 m/z (M+H)+; ret. Time: 3.80 min (Analytical Method A).

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