（R）-2-Chloro-l-（m-chlorophenyl）ethanol,a precursor of（R）-3-chlorostyrene oxide which is the key chiral intermediate for the preparation of severalβ3-adrenergic receptor agonists was prepared in 40%yield and 99%...（R）-2-Chloro-l-（m-chlorophenyl）ethanol,a precursor of（R）-3-chlorostyrene oxide which is the key chiral intermediate for the preparation of severalβ3-adrenergic receptor agonists was prepared in 40%yield and 99%ee by the Lipozyme TL IM-catalyzed second resolution of the corresponding racemate in the presence of vinyl acetate.展开更多
Kinetic resolution of racemic 2-chloro-1-（3,4-dichlorophenyl）ethanol was performed by free Alcaligene sp. lipase-catalyzed irreversible transesterification affording the （R）-isomer with ≥95% ee and the （S）-isom...Kinetic resolution of racemic 2-chloro-1-（3,4-dichlorophenyl）ethanol was performed by free Alcaligene sp. lipase-catalyzed irreversible transesterification affording the （R）-isomer with ≥95% ee and the （S）-isomer with ≥90% ee. The activity of lipase Alcaligene sp. strongly depends on the basicity of the reaction system, and an organic base such as triethylamine can enhance the activity of the lipase and enantioselectivity markedly.展开更多
基金support from the National Natural Science Foundation of China(No20672110)
文摘（R）-2-Chloro-l-（m-chlorophenyl）ethanol,a precursor of（R）-3-chlorostyrene oxide which is the key chiral intermediate for the preparation of severalβ3-adrenergic receptor agonists was prepared in 40%yield and 99%ee by the Lipozyme TL IM-catalyzed second resolution of the corresponding racemate in the presence of vinyl acetate.
基金Project supported by the Doctoral Foundation of Qingdao University of Science and Technology （No. 0022266）, the Program for New Century Excellent Talents in Universities （No. NCET-04-0649）, and the Natural Science Foundation of Shandong Province （No. Z2006B01）.
文摘Kinetic resolution of racemic 2-chloro-1-（3,4-dichlorophenyl）ethanol was performed by free Alcaligene sp. lipase-catalyzed irreversible transesterification affording the （R）-isomer with ≥95% ee and the （S）-isomer with ≥90% ee. The activity of lipase Alcaligene sp. strongly depends on the basicity of the reaction system, and an organic base such as triethylamine can enhance the activity of the lipase and enantioselectivity markedly.
