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    • 4. 发明授权
    • 광학활성 플루옥세틴 또는 노르플루옥세틴의 제조방법
    • 制备具有光活性的氟环丁酯或异氟维酮的方法
    • KR100852364B1
    • 2008-08-14
    • KR1020070050832
    • 2007-05-25
    • 한국화학연구원
    • 이기인이도민고수영강수미
    • C07C217/14C07C217/12C07C217/26
    • A method for preparing an optically active fluoxetine or norfluoxetine is provided to improve optical activity and the easiness of preparation by using an intermediate having a leaving group reacting easily with NaCN, NaN3, an amine, etc. A method for preparing an optically active fluoxetine or norfluoxetine represented by the formula 1a or 1b comprises the steps of reducing a compound represented by the formula 2 by asymmetric transfer hydrogenation in the presence of [R,R]-TsDPEN-RhCl-Cp or [S,S]-TsDPEN-RhCl-Cp and a hydrogen donor; reacting the obtained compound with a nitrile compound; reducing the obtained compound in the presence of BH3; and reacting the obtained compound with a 4-substituted benzotrifluoride compound, wherein R is H or a methyl group; and X is a leaving group selected from a tosyloxy (OTs) group and a mesyloxy (OMs) group.
    • 提供了制备光学活性氟西汀或诺氟西汀的方法,以提高光学活性和使用具有与NaCN,NaN 3,胺等容易反应的离去基团的中间体的制备容易性。一种制备光学活性氟西汀或 由式1a或1b表示的异氟西汀包括以下步骤:在[R,R] -TsDP-RhCl-Cp或[S,S] -TsDPEN-RhCl-CpC)存在下,通过不对称转移氢化还原式2表示的化合物, Cp和氢供体; 使所得化合物与腈化合物反应; 在BH3存在下还原得到的化合物; 并使所得化合物与4-取代三氟甲苯化合物反应,其中R为H或甲基; 并且X是选自甲苯磺酰氧基(OTs)基团和甲磺酰氧基(OMs)基团的离去基团。