反应详情

To a solution of 4-methyl-phenyl-amino-phenyl-acetic acid (I244) (870 mg, 3.60 mmol) in dry THF (35 mL), are added DCC (891 mg, 4.32 mmol), HOBt (583 mg, 4.32 mmol) and 3(R)-quinuclidinol (915 mg, 7.20 mmol). The resulting mixture is stirred at RT for 48 hours (UPLC-MS monitoring: complete conversion). The solvent is evaporated and the residue is portioned between EtOAc and 1M K2CO3. The organic phase is dried over Na2SO4, filtered and evaporated to dryness. The resulting crude is dissolved in little DCM and filtered to remove the insoluble. The solution is concentrated under vacuum to obtain the title compound as a yellow solid, which is used in the next step without any further purification.

1. customThe solvent is evaporated
2. dry with materialThe organic phase is dried over Na2SO4
3. filtrationfiltered
4. customevaporated to dryness
5. dissolutionThe resulting crude is dissolved in little DCM
6. filtrationfiltered
7. customto remove the insoluble
8. concentrationThe solution is concentrated under vacuum