开发了一种有效的四步方案,用于功能化茚满的构建。通过与溴酸酯(2-溴丙酸乙酯,溴乙酸乙酯或2-溴丁酸乙酯)的Reformatsky反应,将1-Tetralones转化为不饱和酯,然后将所形成的β-羟基酯脱水。酯部分的还原导致带有内环双键的均烯丙基醇。这些3-烯醇的氧化重排是通过三硝酸th(TTN)在AcOH / H 2 O的2:1混合物中进行的,导致环收缩产物的产率适中至非常好。研究了该序列的十四个例子。还研究了用TTN氧化由2-四氢萘酮制备的3-链烯醇。对于这些底物,未观察到环收缩反应。
[EN] GPR120 RECEPTOR AGONISTS AND USES THEREOF<br/>[FR] AGONISTES DU RÉCEPTEUR GPR120 ET LEURS UTILISATIONS
申请人:METABOLEX INC
公开号:WO2011159297A1
公开(公告)日:2011-12-22
GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
[EN] GPR120 RECEPTOR AGONISTS AND USES THEREOF<br/>[FR] AGONISTES DE RÉCEPTEURS GPR 120 ET LEURS APPLICATIONS
申请人:METABOLEX INC
公开号:WO2010080537A1
公开(公告)日:2010-07-15
GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Facile access to chiral 4-substituted chromanes through Rh-catalyzed asymmetric hydrogenation
作者:Lin Tao、Qingyang Zhao、Xumu Zhang、Xiu-Qin Dong
DOI:10.1016/j.cclet.2020.01.001
日期:2020.7
Rh/ZhaoPhos-catalyzed asymmetrichydrogenation of a series of (E)-2-(chroman-4-ylidene)acetates was successfully developed to prepare various chiral 4-substituted chromanes with high yields and excellent enantioselectivities (up to 99% yield, 98% ee). Moreover, the gram-scale hydrogenation could be performed well in the presence of 0.02 mol% catalyst loading (TON = 5000), the hydrogenation product was easily
GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.