Tetrahydrofuran → 3-{2-(3-Chloro-5-fluorophenyl)-5-[(4-oxoimidazolidin-1-yl)carbonyl]thiophen-3-yl}benzenecarbonitrile

Participants

Reaction Steps

40.5 mg of the compound from Example 19A having a purity of 76% (0.08 mmol), 24.9 mg (0.13 mmol) of the compound from Example 4A and 88.4 mg (0.17 mmol) of PyBOP are provided in 2 ml of tetrahydrofuran, and 0.04 ml (0.24 mmol) of N,N-diisopropylethylamine are added at room temperature. The reaction mixture is stirred at room temperature overnight and subsequently purified by preparative HPLC (RP18 column; eluent: acetonitrile/water gradient with addition of 0.1% formic acid). 16.8 mg (46% of theory) of the title compound are obtained.

Provenance & Evidence