反应详情

4-Amino-3-(2-pyrrolidin-1-yl-ethylamino)-benzoic acid methyl ester (xii) (1.14 g, 4.33 mmol) and triethylorthoformate (20 mL, 120 mmol) were heated at 120° C. for 18 h before being evaporated to dryness. The residue was taken in EtOAc and aqueous saturated NaHCO3. The aqueous layer was extracted 2 times with EtOAc. The combined organic layers were washed with brine, dried over Na2SO4, filtered and evaporated to dryness to afford the title compound as a brown oil (tR 1.83 min (conditions 8), MH+=274).

1. custombefore being evaporated to dryness
2. extractionThe aqueous layer was extracted 2 times with EtOAc
3. washThe combined organic layers were washed with brine
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. customevaporated to dryness