• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    The mixture, 3rd 1,2-bis- (di-N-propyl acetate) -glycerol of the formula H2-1 H- € H2 (H9 eee € ii (it- "sH,) 2 CHa-iiH-CHj () etC9 o he is the CC (k- € S) -g: with respect to 1.43-1.54, possessing anticonvulsant activity.
    公开号:SU1052507A1
    申请号:SU813276796
    申请日:1981-05-04
    公开日:1983-11-07
    发明作者:Шиняк Мишель；Грэн Клод；Жаммо Фернар；Пижероль Шарль；Эймар Пьер；Ферранде Бернар
    申请人:Санофи (Фирма)；
    IPC主号:
    专利说明:

    The invention relates to a novel compound, a mixture of 1,3- and 1,2-bis (di-h-propyl acetate) -glycerin, possessing anticonvulsant activity. S 5-ethyl-5-fennbarbarbitur acid is known. (Phenobarbital), formulas,. 1GI-CO CjHj oOladouchego anticonvulsant active nostyo OQ. However, this compound also has a strong soporific effect. The purpose of the invention is to expand the senal of the means of action on a living organism. The goal is achieved by a new compound - a mixture of 1,3- and 1,2-bis (di-propyl) -glycerol () BUT ve0Sh ("7S5Ng) g ... - CRz-fH-CHe {«- (jH7) jeHeco j neosc-SaH b: With respect to 1 / 43-1 54, with anticonvulsant activity. This compound is prepared by the reaction of a halide alkali with a sodium salt of a carboxylic acid according to method 21, namely, 1,3-dichloropropanol-x with sodium di-n-propyl acetate, in the presence of a base. The resulting mixture provides a gradual and slow release of di-H-propylacetic acid (also called valproic acid, which is a known anti-elyleptic agent. Thus, this mixture is penetrated by di-H-propylacetic acid. Mixture It is prepared in a two-liter flask, B-liter flask in a 2 liter flask. reverse refrigeration 4, placed 893 g (900 ml) of 11,11-dimethylformamide, 77.4 g (0.6 mol | 1,3-dichloropropanol-2 and 206.4 g (1.24 mol :) D-C-propyl sodium.with gentle stirring in an atmosphere a This mixture is heated to, then maintained at this temperature for 8 hours, after which 893 g of distillate are distilled off at a pressure of 20 lm Hg. To the residue are added 300 ml of distilled water and 537 g (620 ml) of toluene, aqueous the phase is separated, the organch # npoMbmaioT are successively 300 ml of distilled water: br, dissolve and 30 g of sodium carbonate in 400 ml of water and in 300 ml of several times distilled water to obtain a neutral reaction (pH). It is then dried over sodium sulfate, the solvent is distilled off at a reduced pressure in the rotor, a crude mixture of the final Products is obtained, 201 g, yield 97.3%. The mixture is rectified into a vacuum, a fraction having (0.2 mm Hg, Ex 1.4476, the ratio of the 1EZ isomer to 1,2-bis- (di m-propyl acetate) glycerol is 1.54, the amount of glycerol 1-di-n-propyl acetate is 1%, tri- (di-N-propyl acetate) Glycerol not detected, the starting 1,3-dichloropropanol-2 is 0.002%. When using the resulting mixture (at an oral dose of 1000 mg), the half-life of di-propylacetic acid released from it acid is 20–20 mi, which is significantly higher than with the use of sodium di-N-propi-acetic acid — 11 hours and 35 minutes. This mixture has an increased anticonvulsant activity, as it leads to a more stable therapeutic urn of di-n-propyl acetic acid in the blood In addition, it has low toxicity. 7ac, rats when orally administered is 5000 mg / kg, and intraperitoneally, 2368 mg / kg; LD fo for myaia - when administered orally - 5597 mg / kg, with intraperitoneal administration of 1920 mg / kg.
    权利要求:
    Claims (1)
    [1]
    Smes1,3- and 1,2-bis (di-n-propyl) glycerin ene of formula CH 2 -ene-2 is not 0SO € n ( "- e e n 7) 2 CHO and CH 2 I II NVG 2 (i-C e H 7) 2 CH0 <50 o OH COOH (k e n e-7) 2 in respect 1,43-1, 54, possess anticonvulsant activity.
    类似技术:
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    同族专利:
    公开号 | 公开日
    JPS6315256B2|1988-04-04|
    HU188840B|1986-05-28|
    DD151931A5|1981-11-11|
    YU61580A|1983-04-30|
    CY1209A|1983-12-31|
    ES8103015A1|1981-02-16|
    DE3061960D1|1983-03-24|
    DD158773A5|1983-02-02|
    HU183072B|1984-04-28|
    FI800683A|1980-09-07|
    NO152899B|1985-09-02|
    ZA801081B|1981-03-25|
    SU1225481A3|1986-04-15|
    AU534007B2|1983-12-22|
    SG61583G|1985-02-15|
    OA06568A|1981-08-31|
    AR224394A1|1981-11-30|
    IE800445L|1980-09-06|
    NZ192944A|1984-07-06|
    PT70904A|1980-04-01|
    YU292382A|1983-09-30|
    FI69449B|1985-10-31|
    IE49539B1|1985-10-30|
    YU42064B|1988-04-30|
    DK93880A|1980-09-07|
    SU1195901A3|1985-11-30|
    PL222446A1|1981-01-30|
    IL59407A|1983-12-30|
    IN152492B|1984-01-28|
    YU41699B|1987-12-31|
    EP0018342B1|1983-02-16|
    CS216526B2|1982-11-26|
    AU5587280A|1980-09-11|
    ES489250A0|1981-02-16|
    HK22384A|1984-03-23|
    GR70703B|1983-01-04|
    JPS55141436A|1980-11-05|
    US4423071A|1983-12-27|
    IL59407D0|1980-05-30|
    EP0018342A1|1980-10-29|
    PL124023B1|1982-12-31|
    MY8500075A|1985-12-31|
    NO152899C|1985-12-11|
    NO800626L|1980-09-08|
    CA1162928A|1984-02-28|
    FI69449C|1986-02-10|
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    GB7907932|1979-03-06|
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