反应详情

温度

0 °C

A solution of 80 mg (0.14 mmol) (R)-1-(4-methyl-2-oxo-2,3-dihydro-benzoxazol-6-ylmethyl)-2-oxo-2-(4-oxo-piperidin-1-yl)-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate and 32 mg (0.27 mmol) thiomorpholin-1-oxide in 5 mL DCM was stirred overnight at RT. After the solution had been cooled to 0° C., 15 μL (0.27 mmol) of AcOH and 50 mg (0.33 mmol) of sodium triacetoxyborohydride were added and the reaction mixture was stirred for 4 h at this temperature. It was evaporated down i.vac., the residue was taken up in 1 mL MeOH, filtered to remove any insoluble constituents and the crude product was purified by HPLC. The fractions containing the product were combined and lyophilised.

1. customIt was evaporated down i.vac
2. filtrationfiltered
3. customto remove any insoluble constituents
4. customthe crude product was purified by HPLC
5. additionThe fractions containing the product