反应详情

To a solution of 2.7 g (10.9 mmol) of the compound of step 1 in 16.3 ml of a 2 M solution of oxalyl chloride in DCM (32.6 mmol), 80 mg of DMF were added and the mixture was stirred for 30 min at room temperature. The solvent was evaporated, 20 ml of DCM were added and the mixture was evaporated again. The residue was dissolved in 20 ml of DCM and the solution added within 5 min at 0° C. to a solution of 2.48 g (10.9 mmol) of 2-amino-indane-2-carboxylic acid methyl ester hydrochloride in 50 ml of DCM and 30 ml of a saturated sodium hydrogencarbonate solution. After stirring overnight, the phases were separated, the organic phase was dried over sodium sulfate, evaporated, and the residue was purified by silica gel chromatography (HEP/EA gradient). 1.1 g of the title compound were obtained.

1. customThe solvent was evaporated
2. addition20 ml of DCM were added
3. customthe mixture was evaporated again
4. dissolutionThe residue was dissolved in 20 ml of DCM
5. stirringAfter stirring overnight
6. customthe phases were separated
7. dry with materialthe organic phase was dried over sodium sulfate
8. customevaporated
9. customthe residue was purified by silica gel chromatography (HEP/EA gradient)