反应详情

To a stirred solution of the compound prepared in Example 434 (0.217 g,) in toluene (12 mL) was added tert-butyl 4-formylpiperidine-1-carboxylate (0.205 g). The mixture was evaporated in vacuo to remove water from imine formed. Sodium triacetoxyborohydride (0.244 g) was added, followed by acetic acid (0.4 mL). After stirring at room temperature for 1 hour, the reaction mixture was quenched with methanol slowly, to decompose excess borohydride, and then concentrated in vacuo. Ethyl acetate, was added to the residue and then washed with aqueous saturated sodium bicarbonate, dried, evaporated in vacuo to provide the title compound (0.262 g) with the following physical data.

1. customThe mixture was evaporated in vacuo
2. customto remove water from imine
3. customformed
4. customthe reaction mixture was quenched with methanol slowly
5. concentrationconcentrated in vacuo
6. additionEthyl acetate, was added to the residue
7. washwashed with aqueous saturated sodium bicarbonate
8. customdried
9. customevaporated in vacuo