反应详情

A solution of 3-bromo-5-fluoroaniline (CAS 134168-97-1) (380 mg, 2.0 mmol) and 1-(2-chloroethyl)pyrrolidine (CAS 505041-9) (380 mg, 2.2 mmol) in NMP (20 mL) was heated to 120° C. overnight. The solution was diluted with EtOAc (100 mL) and washed with saturated Na2CO3 aqueous solution (3×40 mL). The combined organic layer were dried over Na2SO4, concentrated and purified by prep-TLC (DCM:MeOH=10:1) to give the titled product (290 mg, 50%). LCMS (0-60 AB), RT=1.076 min, M+H, 289.0

1. washwashed with saturated Na2CO3 aqueous solution (3×40 mL)
2. dry with materialThe combined organic layer were dried over Na2SO4
3. concentrationconcentrated
4. custompurified by prep-TLC (DCM:MeOH=10:1)