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    Processes for stereoselective synthesis of trans ISATX247
    1.
    发明授权
    Processes for stereoselective synthesis of trans ISATX247 有权
    用于立体选择性合成反式ISATX247的方法

    公开(公告)号：US07799756B2

    公开(公告)日：2010-09-21

    申请号：US11572833

    申请日：2005-07-26

    申请人： Bruce F. Molino ,  Zhicai Yang ,  Jun-Ho Maeng ,  David D. Manning

    发明人： Bruce F. Molino ,  Zhicai Yang ,  Jun-Ho Maeng ,  David D. Manning

    IPC分类号： A61K38/13 ,  A61K38/12

    CPC分类号： C07K7/645

    摘要： The present invention relates to a process for preparation of a trans ISATX247 compound of the formula: where R1═H or D; R2═H or D; and R3═H or D, by application of organozirconium chemistry. The process involves reacting an acetyl cyclosporin aldehyde with an organozirconium reagent to provide acetyl cyclosporin diene (the acetate of trans ISATX247) and deacetylating the acetyl cyclosporin diene to produce the trans-isomer of ISATX247. The present invention also relates to a process for preparing the same trans ISATX 247 compound, using olefin cross metathesis. The process involves: olefin cross metathesis of acetyl cyclosporin A to afford acetyl cyclosporin α,β-unsaturated aldehyde; Wittig reaction of the acetyl cyclosporin α,β-unsaturated aldehyde to provide acetyl cyclosporin diene; and deacetylation of the acetyl cyclosporin diene to produce the trans ISATX247 compound. Also disclosed are processes for preparing an acetyl cyclosporin α,β-unsaturated aldehyde compound and a cyclosporin triene analogue compound.

    摘要翻译： 本发明涉及制备下式的反式ISATX247化合物的方法：其中R1 = H或D; R2 = H或D; 和R3 = H或D，通过应用有机锆化学。 该方法包括使乙酰环孢菌素醛与有机锆试剂反应以提供乙酰环孢菌素二烯（反式ISATX247的乙酸酯），并使乙酰环孢素二烯脱乙酰以产生ISATX247的反式异构体。 本发明还涉及使用烯烃交叉复分解制备相同的ISATX 247化合物的方法。 该方法包括：乙酰环孢菌素A的烯烃交叉复分解，得到乙酰环孢菌素α，不饱和醛; 乙酰环孢菌素α和β-不饱和醛的维蒂希反应提供乙酰环孢素二烯; 和乙酰环孢菌素二烯的脱乙酰化产生反式ISATX247化合物。 还公开了制备乙酰环孢菌素α，β-不饱和醛化合物和环孢菌素三烯类似物化合物的方法。

    NOVEL PROCESSES FOR STEREOSELECTIVE SYNTHESIS OF TRANS ISATX247
    4.
    发明申请
    NOVEL PROCESSES FOR STEREOSELECTIVE SYNTHESIS OF TRANS ISATX247 有权
    用于ISATX247的立体选择性合成的新方法

    公开(公告)号：US20080021197A1

    公开(公告)日：2008-01-24

    申请号：US11572833

    申请日：2005-07-26

    申请人： Bruce Molino ,  Zhicai Yang ,  Jun-Ho Maeng ,  David Manning

    发明人： Bruce Molino ,  Zhicai Yang ,  Jun-Ho Maeng ,  David Manning

    IPC分类号： C07K7/64

    CPC分类号： C07K7/645

    摘要： The present invention relates to a process for preparation of a trans ISATX247 compound of the formula: where R1═H or D; R2═H or D; and R3═H or D, by application of organozirconium chemistry. The process involves reacting an acetyl cyclosporin aldehyde with an organozirconium reagent to provide acetyl cyclosporin diene (the acetate of trans ISATX247) and deacetylating the acetyl cyclosporin diene to produce the trans-isomer of ISATX247. The present invention also relates to a process for preparing the same trans ISATX 247 compound, using olefin cross metathesis. The process involves: olefin cross metathesis of acetyl cyclosporin A to afford acetyl cyclosporin α,β-unsaturated aldehyde; Wittig reaction of the acetyl cyclosporin α,β-unsaturated aldehyde to provide acetyl cyclosporin diene; and deacetylation of the acetyl cyclosporin diene to produce the trans ISATX247 compound. Also disclosed are processes for preparing an acetyl cyclosporin α,β-unsaturated aldehyde compound and a cyclosporin triene analogue compound.

    摘要翻译： 本发明涉及制备下式的反式ISA 247化合物的方法：其中R 1 -H或D; R 2 -H或D; 和R 3 -H或D，通过应用有机锆化学。 该方法包括使乙酰环孢菌素醛与有机锆试剂反应以提供乙酰环孢菌素二烯（反式ISA 247的乙酸酯）和乙酰环己烷二烯的脱乙酰化产生ISA的反式异构体 TX 247。 本发明还涉及使用烯烃交叉复分解制备相同的反式异构体化合物247的方法。 该方法包括：乙酰环孢菌素A的烯烃交叉复分解，得到乙酰环孢菌素α，β-不饱和醛; 乙酰环孢菌素α，β-不饱和醛维甲酸反应提供乙酰环孢菌素二烯; 和乙酰环孢菌素二烯的脱乙酰化以产生反式ISAX 247化合物。 还公开了制备乙酰环孢菌素α，β-不饱和醛化合物和环孢菌素三烯类似物化合物的方法。