Buagafuran active pharmaceutical ingredient, preparation method and application thereof

    公开(公告)号:US10927090B2

    公开(公告)日:2021-02-23

    申请号:US16344026

    申请日:2018-04-18

    Inventor: Bo Song

    Abstract: A method suitable for large-scale production of buagafuran active pharmaceutical ingredient. A buagafuran active pharmaceutical ingredient (API) with a high purity prepared by the method includes an active ingredient of buagafuran, an impurity A, and an impurity B. In the buagafuran API, a content of the active ingredient of buagafuran is higher than 97.5%, and a total content of the impurity A and the impurity B is less than 0.04%. The buagafuran API can be applied to new drug development processes such as clinical research, pharmaceutical research and quality control research.

    Process for preparing 2-exo-(2-methylbenzyloxy)-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane

    公开(公告)号:US10710969B2

    公开(公告)日:2020-07-14

    申请号:US16334152

    申请日:2017-09-07

    Applicant: BASF Agro B.V.

    Abstract: This invention relates to a process for preparing (±)-2-exo-(2-Methylbenzyloxy)-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane of the formula (I) any of its individual enantiomers or any non-racemic mixture thereof, comprising the steps of (a) reacting (±)-2-exo-hydroxy-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane of the formula (II) any of its individual enantiomers or any non-racemic mixture thereof with a 2-Methylbenzyl compound of the formula (III) wherein X is a leaving group in the presence of at least one base capable of forming water or a C1-C4 alkyl alcohol under the reaction conditions, and at least one inert organic solvent, and (b) simultaneously removing water, the C1-C4 alkyl alcohol or any mixture thereof from the reaction mixture.

Patent Agency Ranking