FUNCTIONALIZED FLUOROALKYL SILANE, AND SYNTHETIC METHOD THEREFOR AND APPLICATION THEREOF

    公开(公告)号:US20230257402A1

    公开(公告)日:2023-08-17

    申请号:US18031243

    申请日:2021-11-01

    摘要: Disclosed in the present invention are a functionalized fluoroalkyl silane compound and a synthetic method therefor. The method comprises: dissolving a halosilane and a fluoroalkyl source in an organic solvent; and synthesizing functionalized fluoroalkyl silane under the effect of an alkali or a tertiary phosphine compound. The functionalized fluoroalkyl silane can not only be used for constructing a series of high added-value compounds such as fluoroalkyl substituted alcohols, ketones and amines that can be constructed by conventional TMSRf, but also can transfer, by means of appropriate conversion, a functional group on a silicon protecting group to the obtained addition product in an addition reaction, for synthesizing some fluorine-containing compounds that cannot be synthesized by using a conventional TMSRf reagent, thereby greatly improving the synthesis efficiency and the atom economy of reactions. Also disclosed in the present invention are more excellent reaction efficiency and enantioselectivity, compared with conventional TMSCF3, exhibited by trifluoromethyl chloromethylsilane in synthesis of a 2-trifluoromethylquinoline compound and in an asymmetric trifluoromethylation reaction with α,β-unsaturated ketones.

    Process for producing optically active benzhydrol compounds
    4.
    发明授权
    Process for producing optically active benzhydrol compounds 失效
    光学活性二苯甲醇化合物的制备方法

    公开(公告)号:US5780692A

    公开(公告)日:1998-07-14

    申请号:US772525

    申请日:1996-12-24

    CPC分类号: C07C29/145 C07C69/76

    摘要: A process for producing a benzhydrol compound (II) which comprises hydrogenating a benzophenone compound (I) in the presence of a hydrogenation catalyst consisting of a transition metal complex, a base and an optically active diamine compound: ##STR1## wherein R.sup.1 to R.sup.10 each represents H, OH, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkanoyl, etc., R.sup.2 and R.sup.3, and R.sup.8 and R.sup.9 may form --CH.dbd.CH--CH.dbd.CH--, or any two of R.sup.1 to R.sup.9 adjacent to each other may be bonded to thereby form --OCH.sub.2 O-- or --(CH.sub.2).sub.3 --. By using this process, optically active benzhydrol compounds which have a high purity and are useful as, for example, intermediates in the synthesis of drugs can be produced by simple procedures.

    摘要翻译: 一种二苯甲醇化合物(II)的制备方法,其包括在由过渡金属配合物,碱和光学活性二胺化合物组成的氢化催化剂存在下氢化二苯甲酮化合物(I):(I) (II)其中R 1至R 10各自表示H,OH,C 1-4烷基,C 1-4烷氧基,C 1-4烷酰基等,R 2和R 3,以及R 8和R 9可以形成-CH = CH-CH = CH - 或相邻的R 1至R 9中的任何两个可以键合,从而形成-OCH 2 O-或 - (CH 2)3 - 。 通过使用该方法,可以通过简单的方法制备具有高纯度并且可用作例如药物合成中的中间体的光学活性二苯甲基化合物。