反应详情

PS-DCC (2.05 g, 2.57 mmol, loading: 1.25 mmol/g) is suspended in THF (15 mL) and shaken for few minutes. Then (2-methoxy-phenylamino)-phenyl-acetic acid hydrochloride (I36) (377 mg, 1.28 mmol) and HOBT (393 mg, 2.57 mmol) are added. After 10 minutes, (R)-quinuclidin-3-ol (490 mg, 3.85 mmol) is added and the mixture is shaken at RT for 16 hours (Conversion complete by UPLC/MS-UV). PS-DCC is filtered off and the filtrate is evaporated to dryness. The residue is dissolved in EtOAc and washed with sat. NaHCO3, water and brine. The organic layer is recovered, dried over Na2SO4, filtered and evaporated to afford the title compound as a yellow oil (548 mg, quantitative yield, mixture of diastereoisomers).

1. stirringthe mixture is shaken at RT for 16 hours (Conversion complete by UPLC/MS-UV)
2. filtrationPS-DCC is filtered off
3. customthe filtrate is evaporated to dryness
4. dissolutionThe residue is dissolved in EtOAc
5. washwashed with sat. NaHCO3, water and brine
6. customThe organic layer is recovered
7. dry with materialdried over Na2SO4
8. filtrationfiltered
9. customevaporated