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    4,5-디히드로옥사졸-2-일벤젠 유도체의 제조방법
    12.
    发明公开
    4,5-디히드로옥사졸-2-일벤젠 유도체의 제조방법 失效
    制备4,5-二羟基-2-甲基苯并噻唑衍生物的方法

    公开(公告)号：KR1020130075163A

    公开(公告)日：2013-07-05

    申请号：KR1020110143415

    申请日：2011-12-27

    Applicant: 주식회사 팜한농 ,  한국화학연구원

    Inventor： 류재욱 ,  고영관 ,  김종근 ,  서지수 ,  구동완 ,  김경성 ,  최인영 ,  홍미숙 ,  김태준 ,  안희근 ,  김시용

    IPC: C07D413/14 ,  C07D413/12 ,  C07D401/14 ,  A01N43/76

    Abstract: PURPOSE: A method for preparing 4,5-dihydrooxazol-2-ylbenzene derivatives is provided to have a relatively mild reaction condition, to easily handle a reagent, and to synthesize the 4,5-dihydrooxazol-2-ylbenzene derivatives with high yield. CONSTITUTION: A method for preparing 4,5-dihydrooxazole-2-ylbenzene compound of chemical formula 1 or a salt thereof comprises the step of cyclizing a hydroxyalkyl benzamide of chemical formula 2 under the presence of (diethylamino)sulfur trifluoride (DAST) or para-toluene sulfonate (TsOH). The cyclization is performed under the presence of a base selected from the group consisting of tray (C_1-C_6) alkyl amine, alkali metal or hydroxide of the alkali earth metal, hydroxide, and C_1-C_6 alkoxide. The base is selected from the group consisting of trimethyl amine, triethyl amine, diethyl isopropyl amine, lithium hydroxide, sodium hydroxide, calcium hydroxide, sodium hydroxide, potassium hydroxide, sodium methoxide, and potassium methoxide.

    Abstract translation: 目的：提供一种制备4,5-二氢恶唑-2-基苯衍生物的方法以具有相对温和的反应条件，容易处理试剂，并以高产率合成4,5-二氢恶唑-2-基苯衍生物。 构成：用于制备化学式1的4,5-二氢恶唑-2-基苯化合物或其盐的方法包括在（二乙基氨基）三氟化硫（DAST）或对位基团的存在下使化学式2的羟基烷基苯甲酰胺环化的步骤 - 甲苯磺酸盐（TsOH）。 环化是在碱土金属的碱土金属，碱金属或氢氧化物的塔板（C_1-C_6）烷基胺，碱金属或氢氧化物，C_1-C_6烷氧基化物的碱存在下进行的。 碱选自三甲胺，三乙胺，二乙基异丙胺，氢氧化锂，氢氧化钠，氢氧化钙，氢氧化钠，氢氧化钾，甲醇钠和甲醇钾组成的组。

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