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    • 46. 发明授权
    • Method of preparing optically pure precursors of paroxetine
    • 制备帕罗西汀光学纯的前体的方法
    • US5258517A
    • 1993-11-02
    • US926254
    • 1992-08-06
    • Charles M. ZeppYun GaoDonald L. Heefner
    • Charles M. ZeppYun GaoDonald L. Heefner
    • C07D211/22C07D211/88C12P41/00
    • C07D211/88C07D211/22C12P41/005
    • A biocatalytic method of preparing optically pure precursors of paroxetine and a method of preparing paroxetine therefrom are disclosed. A racemic trans ester precursor compound of paroxetine is first prepared. The racemic trans ester precursor compound comprises a mixture of (3S,4R) and (3R,4S) enantiomers. The (3R,4S) enantiomer is hydrolyzed biocatalytically to the corresponding (3R,4S)-trans carboxylic acid or alternatively, the (3S,4R) enantiomer is biocatalytically hydrolyzed the to (3S,4R)-trans carboxylic acid in a reaction catalyzed by a isolated enzyme or a microorganism. In the first instance, the unhydrolyzed (3S,4R) enantiomer is separated from the (3R,4S)-trans carboxylic acid, whereas in the second instance the (3S,4R)-trans carboxylic acid is separated from the unhydrolyzed (3R,4S) enantiomer. The (3S,4R) enantiomer obtained following the selective hydrolysis is reduced to form a (-)-trans-(3S,4R) primary alcohol precursor of paroxetine. Paroxetine is then formed from the (-)-trans-(3S,4R) primary alcohol precursor.
    • 公开了制备帕罗西汀光学纯的前体的生物催化方法及其制备帕罗西汀的方法。 首先制备帕罗西汀的外消旋转酯前体化合物。 外消旋反式酯前体化合物包含(3S,4R)和(3R,4S)对映异构体的混合物。 将(3R,4S)对映异构体生物催化水解生成至相应的(3R,4S) - 羧酸,或者(3S,4R)对映异构体在反应催化下生物催化水解成(3S,4R) - 反式羧酸 通过分离的酶或微生物。 在第一种情况下,从(3R,4R) - 反式羧酸分离出未水解的(3S,4R)对映异构体,而在第二种情况下,将(3S,4R) - 反式羧酸与未水解的(3R, 4S)对映异构体。 在选择性水解后获得的(3S,4R)对映异构体被还原形成帕罗西汀的( - ) - 反 - (3S,4R)伯醇前体。 然后由( - ) - 反 - (3S,4R)伯醇前体形成帕罗西汀。
    • 49. 发明申请
    • Folding Canopy
    • 折叠天篷
    • US20130068269A1
    • 2013-03-21
    • US13237127
    • 2011-09-20
    • Jian Yun Gao
    • Jian Yun Gao
    • E04H15/50
    • E04H15/50E04H15/58
    • A folding canopy has a canopy top made of flexible sheet material; and a canopy frame. The canopy top is adapted to attach onto the canopy frame, and the canopy frame includes a number of members. A pair of left cross support bars have a first left cross support bar, and a second left cross support bar. The first left cross support bar is pivotally connected to the second left cross support bar. A pair of right cross support bars includes a first right cross support bar, and a second right cross support bar. The first right cross support bar is pivotally connected to the second right cross support bar.
    • 折叠篷具有由柔性片材制成的顶盖; 和一个遮篷架。 顶篷适用于遮盖架,遮篷架包括多个构件。 一对左交叉支撑杆具有第一左交叉支撑杆和第二左交叉支撑杆。 第一左交叉支撑杆枢转地连接到第二左交叉支撑杆。 一对右交叉支撑杆包括第一右交叉支撑杆和第二右交叉支撑杆。 第一右交叉支撑杆枢转地连接到第二右交叉支撑杆。