Disclosed herein are pyrazole glucokinase activators of the formula (I)
useful for the treatment of metabolic diseases and disorders, preferably diabetes mellitus.
Catalytic Enantioselective Conjugate Addition of Grignard Reagents to Cyclic Enones Using<i>C</i><sub>1</sub>-1,1′-Bisisoquinoline-Based Chiral Ligands
作者:Gao Qi、Zaher M. A. Judeh
DOI:10.1080/00397911.2010.541969
日期:2012.6
Abstract New highly constrained chiral C 1-1,1′-bisisoquinoline ligands were examined in the enantioselectiveconjugateaddition of Grignard reagents to cyclohexenone and cyclopentenone. The desired 1,4-adducts were obtained in excellent yield and moderate enantiomeric excess (up to 35%). GRAPHICAL ABSTRACT
摘要 在格氏试剂与环己烯酮和环戊烯酮的对映选择性共轭加成中,研究了新的高度受限的手性 C 1-1,1'-双异喹啉配体。以极好的收率和适度的对映体过量(高达 35%)获得了所需的 1,4-加合物。图形概要
Cu<sup>I</sup>
-Catalysed Enantioselective Alkyl 1,4-Additions to (<i>E</i>
)-Nitroalkenes and Cyclic Enones with Phosphino-Oxazoline Ligands
New phosphino‐oxazoline ligands have been developed, and the ligands have been used for Cu‐catalysed enantioselective conjugate additions to (E)‐nitroalkenes.
report the use of phosphinoazomethinylate salts as chiral efficient ligands for the copper-catalyzedasymmetricconjugateaddition (ACA) of dialkylzinc to various enones. These tridentate P,N,O ligands are straightforwardly obtained in a one-step procedure from commercially available enantiopure α-aminoacids. Performing the conjugateaddition in the greener AcOEt solvent, high enantioselectivities were reached
在本文中,我们报道了膦基次甲基次膦酸酯盐作为手性有效的配位体,用于铜催化的二烷基锌向各种烯酮的不对称共轭加成(ACA)。这些三齿P,N,O配体可以一步一步从市售对映纯α-氨基酸直接获得。在较绿的AcOEt溶剂中进行共轭物加成,环状和非环状烯酮的对映选择性都达到了较高的对映选择性,分别介于72%到98%ee和96%到> 99%。获得高对映选择性所需的2/1 Cu /配体比率使我们设想了用于该转化的铜-铜双金属催化体系。
Asymmetric Catalysis. Asymmetric Catalytic Intramolecular Hydroacylation of 4-Pentenals Using Chiral Rhodium Diphosphine Catalysts
作者:Richard W. Barnhart、Xianqi Wang、Pedro Noheda、Steven H. Bergens、John Whelan、B. Bosnich
DOI:10.1021/ja00084a025
日期:1994.3
Catalysts of the type [Rh(chiral diphosphine)] + convert 4-substituted 4-pentenals into the corresponding 3-substituted cyclopentanones with generally high turnover numbers and frequencies at 25 o C. The enantioselectivities of various substituted 4-pentenals with two chiral diphosphines have been explored. It was found that with the binap catalyst, almost complete enantioselectivity is observed for
[Rh(手性二膦)] + 类型的催化剂在 25 o C 下将 4-取代的 4-戊烯醛转化为相应的 3-取代的环戊酮,其转换数和频率通常很高。 具有两个手性二膦的各种取代的 4-戊烯醛的对映选择性已被探索。发现使用 binap 催化剂,对于带有 4-取代叔取代基的 4-戊烯醛底物和酯基,观察到几乎完全的对映选择性。酮取代基具有非常高的对映选择性