Three diastereomers 1, 2, and 4 of a new glutamate analogue incorporating a 5-membered ring were synthesized in a stereocontrolled manner. 1′R-Isomers 2 and 4 were constructed from the α,β-unsaturated 2,2,2-trifluoroethyl esters 5b and 10b by a [3+2] cycloaddition with a Pd-trimethylenemethane (TMM) complex. The 1′S isomer 1 was synthesized by a 1,4-addition of TMM equivalent to the α,β-unsaturated
三个非对映体1,2,和4结合有5元环的新的谷
氨酸类似物的立体控制的方式合成。1' - [R -异构体2和4分别来自α构造,β不饱和
2,2,2-三氟乙基酯5B和图10b通过[3 + 2]环加成与Pd的trimethylenemethane(TMM)络合物。1 'S异构体1是通过与α,β-不饱和甲酯10a等效的TMM的1,4-加成合成的。折叠异构体4 在生理学上被表征为哺乳动物中枢神经系统中的有效的
海藻酸盐受体激动剂。