反应详情

2 g of bimatoprost acid is dissolved in 20 ml of THF and to this solution are added at room temperature 1 g of N-hydroxy-phtalimide and 1 ml of N,N′-diisopropylcarbodiimide. The reaction mixture is stirred for 2 hours and then poured onto they mixture of 1N NaHSO4 solution and tert-butyl methyl ether (TBME). The phases are separated, the organic phase is washed with 1N NaHCO3 solution and the aqueous-alkaline phase is extracted with TBME. The united organic phase is dried over Na2SO4, filtered and evaporated. The residue is crystallized from hexane:acetone mixture to obtain 1.5 g white crystalline material.

1. customThe phases are separated
2. washthe organic phase is washed with 1N NaHCO3 solution
3. extractionthe aqueous-alkaline phase is extracted with TBME
4. dry with materialThe united organic phase is dried over Na2SO4
5. filtrationfiltered
6. customevaporated
7. customThe residue is crystallized from hexane