反应详情

To a solution of 4-(methoxycarbonyl)-1H-pyrrole-3-carboxylic acid (2.35 g) in DMF (49 ml) there are added diisopropylethylamine (2.11 ml) and HATU (4.9 ml). After stiffing for 15 minutes at 40° C., morpholine (1.35 ml) is added. After stiffing for 9 hours at 60° C. and at ambient temperature over a weekend, the mixture is diluted with CH2Cl2 and 1N sodium hydroxide solution. The aqueous phase is extracted 3 times with CH2Cl2 and the organic phases are combined. The organic phase is dried over magnesium sulphate, filtered and evaporated to dryness to yield the title product, which is used directly in the next Step.

1. waitAfter stiffing for 9 hours at 60° C. and at ambient temperature over a weekend
2. extractionThe aqueous phase is extracted 3 times with CH2Cl2
3. dry with materialThe organic phase is dried over magnesium sulphate
4. filtrationfiltered
5. customevaporated to dryness