A library consisting of a series of O,O'-diaryzoyl-L-(-)-tartaric acids (2) was designed and synthesized. The substituent on the aromatic ring of 2 significantly affects the diastereomeric excess and efficiency of...A library consisting of a series of O,O'-diaryzoyl-L-(-)-tartaric acids (2) was designed and synthesized. The substituent on the aromatic ring of 2 significantly affects the diastereomeric excess and efficiency of the resolution of racemic albuterol (1). Excel-lent resolving reagent 2a was selected for the resolution of rac-1 via the parallel approach. However,a family of three resolving reagents failed to improve the resolution efficiency of rac-1.展开更多
The reaction of 2-pyridylacetates andα,β-unsaturated pyrazolamides with DBU as the catalyst has been developed.A range of unexplored multisubstituted 2,3-dihydro-4H-quinolizin-4-ones are obtained with satisfactory y...The reaction of 2-pyridylacetates andα,β-unsaturated pyrazolamides with DBU as the catalyst has been developed.A range of unexplored multisubstituted 2,3-dihydro-4H-quinolizin-4-ones are obtained with satisfactory yields(up to 94%)and excellent diastereoselectivities(all cases>20:1 dr)via a dearomative[3+3]annulation process.This practical method also features transition metal free,mild reaction conditions,wide functional group tolerance,easy scale-up synthesis,and versatile further derivatization.展开更多
基金supported by the National Natural Science Foundation of China (29790125,29972039 and 20025205)
文摘A library consisting of a series of O,O'-diaryzoyl-L-(-)-tartaric acids (2) was designed and synthesized. The substituent on the aromatic ring of 2 significantly affects the diastereomeric excess and efficiency of the resolution of racemic albuterol (1). Excel-lent resolving reagent 2a was selected for the resolution of rac-1 via the parallel approach. However,a family of three resolving reagents failed to improve the resolution efficiency of rac-1.
基金the National Natural Science Foundation of China(No.22171029,21901024,21871252,21801024,and 21801026)the Sichuan Science and Technology Program(2021YFS0315)the Talent Program of Chengdu University(2081919035 and 2081921038).
文摘The reaction of 2-pyridylacetates andα,β-unsaturated pyrazolamides with DBU as the catalyst has been developed.A range of unexplored multisubstituted 2,3-dihydro-4H-quinolizin-4-ones are obtained with satisfactory yields(up to 94%)and excellent diastereoselectivities(all cases>20:1 dr)via a dearomative[3+3]annulation process.This practical method also features transition metal free,mild reaction conditions,wide functional group tolerance,easy scale-up synthesis,and versatile further derivatization.
