反应详情

温度

0 °C

To a stirred solution of 4-(N-(tert-butoxycarbonyl)methylsulfonamido)-3-(cyclopropylmethoxy)benzoic acid (for reference procedure see Example 18, WO 2010/089107, which is incorporated herein by reference in its entirety) (0.500 g, 1.297 mmol) in anhydrous THF (10 ml), BH3*THF complex (1M solution in THF, 2.59 ml, 2.59 mmol) was added drop wise at RT under nitrogen atmosphere. After 4 hours, the reaction was cooled to 0° C. and quenched with aqueous NH4Cl. The mixture was extracted with EtOAc and the organic phase was dried over Na2SO4 and evaporated under reduced pressure affording tert-butyl 2-(cyclopropylmethoxy)-4-(hydroxymethyl)phenyl(methylsulfonyl)carbamate as a colorless oil (0.430 g, 1.158 mmol, 89% yield, MS/ESI+ 394.2 [MNa]+). This product was used without purification.

1. customquenched with aqueous NH4Cl
2. extractionThe mixture was extracted with EtOAc
3. dry with materialthe organic phase was dried over Na2SO4
4. customevaporated under reduced pressure