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    Tetrahydrofuran derivatives having cis substituent, their intermediates, and their preparation method
    7.
    发明授权
    Tetrahydrofuran derivatives having cis substituent, their intermediates, and their preparation method 失效
    具有顺式取代基的四氢​​呋喃衍生物及其制备方法

    公开(公告)号：US07388101B1

    公开(公告)日：2008-06-17

    申请号：US11732602

    申请日：2007-04-04

    申请人： Yong Seo Cho ,  Hyunah Choo ,  Joo Hwan Cha ,  Ae Nim Pae ,  Satish N. Chavre ,  Kyung Il Choi

    发明人： Yong Seo Cho ,  Hyunah Choo ,  Joo Hwan Cha ,  Ae Nim Pae ,  Satish N. Chavre ,  Kyung Il Choi

    IPC分类号： C07D307/02

    CPC分类号： C07D307/12

    摘要： The present invention relates to a tetrahydrofuran compound having cis substituents, the derivatives thereof and a process for preparing the same, and in particular relates to a dihydrofuran-3-ylidene triflate compound having cis substituents at C2 and C5 positions prepared through Prins-type cyclization using a homopropargylic alcohol derivative as a starting material in the presence of Lewis acid catalyst, a tetrahydrofuran compound having cis substituents at C2, C3 and C5 positions prepared through the hydrolysis of triflate group in the derivatives of the dihydrofuran-3-ylidene triflate compound, and a preparation method thereof.The derivatives and the target tetrahydrofuran compound prepared according to the present invention are hydrofuran compounds with novel structures having cis substituents at C2, C3 and/or C5 positions, which are useful as a derivative for synthesizing drugs such as an antagonist for neurokinin receptor.

    摘要翻译： 本发明涉及具有顺式取代基的四氢​​呋喃化合物及其衍生物及其制备方法，特别涉及在C 2上具有顺式取代基的二氢呋喃-3-亚基三氟甲磺酸酯化合物和 在路易斯酸催化剂存在下，使用均二炔醇衍生物作为起始原料，在C 2 N 2上具有顺式取代基的四氢​​呋喃化合物，通过Prins-型环化制备的C 5 H 3位， 通过在二氢呋喃-3-亚基三氟甲磺酸酯化合物的衍生物中水解三氟甲磺酸酯基制备的C 3和C 5 H 3位及其制备方法。 根据本发明制备的衍生物和目标四氢呋喃化合物是具有在C 2，C 3和/或C 5上具有顺式取代基的新结构的氢呋喃化合物 其可用作合成药物的衍生物，例如用于神经激肽受体的拮抗剂。