Chloroform → 7-fluoro-1-(2-{4-[([1,3]oxathiolo[5,4-c]pyridin-6-ylmethyl)amino]-1-piperidinyl}ethyl)-2(1H)-quinolinone Dihydrochloride

関与物質

反応手順

A mixture of 1-[2-(4-amino-1-piperidinyl)ethyl]-7-fluoro-2(1H)-quinolinone (100 mg; 0.364 mmol) and [1,3]oxathiolo[5,4-c]pyridine-6-carbaldehyde (for a synthesis see WO2004058144, Example 61) (57 mg; 0.364 mmol) were dissolved in a 5:1 mixture of chloroform and methanol (5 ml: 1 ml) and stirred at rt under argon for 1 h. The mixture was then treated with NaBH(OAc)3 (231 mg; 1.092 mmol) and stirred for a further 1 h. The solvents were then removed and the crude residues purified by chromatography on silica gel using a 0-15% MeOH/DCM gradient to provide the title compound as free base (140 mg; 92%)

情報源と証拠