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    • 25. 发明授权
    • Method for producing five-membered ring-containing compound
    • 生产五元环化合物的方法
    • US08716500B2
    • 2014-05-06
    • US14113611
    • 2012-04-27
    • Yujiro Hayashi
    • Yujiro Hayashi
    • C07D307/02
    • C07D307/45C07B53/00C07C67/30C07C69/732C07C69/738C07C201/12C07C205/05C07C2601/08C07C2601/14C07D307/42C07C205/18C07C205/44C07C205/41C07C205/55
    • The present invention provides a method that allows production of stereospecific and asymmetrical five-membered ring-containing compounds serving as synthetic intermediates for formation of five-membered rings of prostaglandins and the like, with high yield and excellent stereoselectivity in terms of diastereoselectivity and enantioselectivity in a short process without requiring troublesome procedures such as optical resolution. The method for producing a five-membered ring-containing compound includes a cyclization step of condensing and cyclizing an α,β-unsaturated nitro compound represented by the following chemical formula (I) with a 1,4-butanedione compound, in the presence of a catalyst formed by a compound having a pyrrolidine ring and an optically active α-carbon relative to the nitrogen on the ring, in a water-insoluble organic solvent and/or a non-oxygen atom-containing water-soluble organic solvent so as to produce the five-membered ring-containing compound represented by the following chemical formula (II).
    • 本发明提供了一种制备用于形成前列腺素等五元环的合成中间体的立体有择和不对称的五元环化合物的方法,其在非对映选择性和对映选择性方面具有高产率和优异的立体选择性 一个简单的过程,而不需要麻烦的程序,如光学分辨率。 含有五元环的化合物的制造方法包括在下述化学式(I)表示的α,β-不饱和硝基化合物与1,4-丁二酮化合物的存在下, 由具有吡咯烷环和光学活性α-碳的化合物相对于环上的氮形成的催化剂在水不溶性有机溶剂和/或非含氧原子的水溶性有机溶剂中形成的催化剂,以便 以制备由以下化学式(II)表示的含五元环的化合物。
    • 26. 发明申请
    • METHOD FOR PRODUCING FIVE-MEMBERED RING-CONTAINING COMPOUND
    • 生产含五元环的化合物的方法
    • US20140051874A1
    • 2014-02-20
    • US14113611
    • 2012-04-27
    • Yujiro Hayashi
    • Yujiro Hayashi
    • C07D307/45C07C205/05C07C69/738C07C201/12C07C67/30C07C69/732
    • C07D307/45C07B53/00C07C67/30C07C69/732C07C69/738C07C201/12C07C205/05C07C2601/08C07C2601/14C07D307/42C07C205/18C07C205/44C07C205/41C07C205/55
    • The present invention provides a method that allows production of stereospecific and asymmetrical five-membered ring-containing compounds serving as synthetic intermediates for formation of five-membered rings of prostaglandins and the like, with high yield and excellent stereoselectivity in terms of diastereoselectivity and enantioselectivity in a short process without requiring troublesome procedures such as optical resolution. The method for producing a five-membered ring-containing compound includes a cyclization step of condensing and cyclizing an α,β-unsaturated nitro compound represented by the following chemical formula (I) with a 1,4-butanedione compound, in the presence of a catalyst formed by a compound having a pyrrolidine ring and an optically active α-carbon relative to the nitrogen on the ring, in a water-insoluble organic solvent and/or a non-oxygen atom-containing water-soluble organic solvent so as to produce the five-membered ring-containing compound represented by the following chemical formula (II).
    • 本发明提供了一种制备用于形成前列腺素等五元环的合成中间体的立体有择和不对称的五元环化合物的方法,其在非对映选择性和对映选择性方面具有高产率和优异的立体选择性 一个简单的过程,而不需要麻烦的程序,如光学分辨率。 制备含五元环的化合物的方法包括在下列化学式(I)表示的α,β-不饱和硝基化合物与1,4-丁二酮化合物的存在下缩合和环化的环化步骤: 由具有吡咯烷环和光学活性α-碳的化合物相对于环上的氮,在水不溶性有机溶剂和/或非含氧原子的水溶性有机溶剂中形成的催化剂,以便 产生由以下化学式(II)表示的含五元环的化合物。