The present invention is to provide a method for producing an optically active erythro-3-amino-2-hydroxybutyric ester as an important intermediate of pharmaceutical agents, specifically HIV protease inhibitor, at a high purity and at a high yield.
More specifically, the present invention relates to a method for producing an optically active erythro-3-amino-2-hydroxybutyric ester,
compwashing oxidizing the hydroxyl group at the 2-position of an optically active 3-amino-2-hydroxybutyric ester, optically active at 3-position, as represented by the formula (I);
(wherein R1 represents phenyl group or cyclohexyl group; R2 represents a protective group and R3 represents alcohol residue; the steric configuration of *1 represents S configuration or R configuration), and then reducing erythro-selectively the resulting product by using aluminium alkoxide.
本发明旨在提供一种高纯度、高收率生产光学活性红-3-
氨基-2-羟基
丁酸酯的方法,该光学活性红-3-
氨基-2-羟基
丁酸酯是一种重要的药物中间体,特别是艾滋病毒蛋白酶抑制剂。
更具体地说,本发明涉及一种生产光学活性红-3-
氨基-2-羟基
丁酸酯的方法、
将光学活性 3-
氨基-2-羟基
丁酸酯 2 位的羟基进行复合洗涤氧化,其 3 位的光学活性由式(I)表示;
(其中 R1 代表苯基或环己基;R2 代表保护基团;R3 代表醇残基;*1 的立体构型代表 S 构型或 R 构型),然后用氧化铝对所得产物进行赤式选择性还原。