反应详情

A mixture of methyl 3-[1-(4-chlorobenzyl)-3-trimethylacetyl-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoate (EP 419,049; Example 8, Step A) (15.64 g), ZnI2 (25.2 g), and NaBH3CN (16.4 g) in 210 mL dichloroethane was stirred using a mechanical stirrer at r.t. for 30 minutes and then at 73° C. for 3 hours. The reaction mixture was allowed to cool, poured onto NH4OAc (aq), and extracted (3x EtOAc). The organic phase was dried (MgSO4), evaporated, and the residue chromatographed (silica gel; ether/hexane 1:3) to give the title compound as a solid.

1. customat r.t.
2. customfor 30 minutes
3. temperatureto cool
4. additionpoured onto NH4OAc (aq)
5. extractionextracted (3x EtOAc)
6. dry with materialThe organic phase was dried (MgSO4)
7. customevaporated
8. customthe residue chromatographed (silica gel; ether/hexane 1:3)