反应详情

To a stirred solution of (6-methoxy-2-(2,2,2-trifluoroethylamino)quinolin-3-yl)methanol SLA 41068 (1.45 g, 5.07 mmol) in dry CH2Cl2 (20 mL) in a 100 mL round-bottomed flask equipped with a magnetic stirrer was added dropwise SOCl2 (7.35 mL, 101.3 mmol). The mixture was stirred for 2 h at RT then concentrated to dryness at 40° C. under vacuum. The residue was then taken up in CH2Cl2 (20 mL) before concentration back to dryness at 40° C. under vacuum (done 3 times) to give 3-(chloromethyl)-6-methoxy-N-(2,2,2-trifluoroethyl)quinolin-2-amine hydrochloride SLA 41070 as a yellow solid (1.74 g, >100% yield).

1. concentrationthen concentrated to dryness at 40° C. under vacuum
2. concentrationThe residue was then taken up in CH2Cl2 (20 mL) before concentration back to dryness at 40° C. under vacuum (done 3 times)