Highly diastereoselective synthesis of new, carbostyril-based type of conformationally-constrained β-phenylserines
作者:Hisanori Ueki、Trevor K Ellis、Masood A Khan、Vadim A Soloshonok
DOI:10.1016/s0040-4020(03)01172-4
日期:2003.9
prearranged carbonyl and glycine moieties, under strongly basic conditions easily undergo complete and highly diastereoselective cyclization, affording a generalized and practical access to the conformationally constrained phenylserine derivatives 4. High chemical yields, virtually complete diastereoselectivity combined with the operational convenience of the experimental procedures render this method useful
我们已经证明,在强碱性条件下,容易获得的酰胺基-酮基化合物5,具有预先安排的羰基和甘氨酸部分,很容易发生完全和高度非对映选择性的环化反应,从而提供了对构象受限的苯基丝氨酸衍生物4的通用且实用的途径。较高的化学收率,几乎完全的非对映选择性以及实验程序的操作便利性,使得该方法可用于制备这些非对映体纯的衍生物。