Solvent-switchable Acetalization by Yb（OTf）3-Catalyzed Procedures

O,O＇Diethyl acetals were prepared in high yields under mild conditions via the reaction of triethyl orthoformate with aldehydes and ketones in absolute ethanol in the presence of as low as 0.1 tool% of Yb（OTf）3. Using the same catalyst in THF-H2O, these O,O＇-diethyl acetals could be converted to the corresponding carbonyl compounds efficiently. This new protection-deprotection protocol presents the advantages of ease of execution, high efficiency and good chemoselectivity.     

NMDA受体2A选择性抑制剂NVP-AAM077 的高效合成

本文报道一条以2,3-二氨基甲苯为原料，经过8步反应合成NMDA受体2A选择性抑制剂NVP-AAM077的高效率路线，其总收率为54%。合成中使用的关键反应包括NaIO₄/DMF介导的氧化芳苄溴到芳醛的反应以及亚膦酸酯对亚胺的加成反应等。     

An Efficient Synthesis of Selective Human NR2A Antagonist NVP-AAM077

A short and efficient synthesis of the selective human N-methyl-D-aspartate （NMDA） receptor 2A （NR2A） antagonist NVP-AAM077 is described. The target was achieved in 8 steps and in 54% overall yield from the commercially available chemical 3-methylbenzene-1,2-diamine. A NaIO4/DMF-based oxidation of the bromide to corresponding aldehyde and an addition of phosphinic acid ester to the aldimine successfully served as the key steps.