• 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 invention relates to heterocyclic compounds, in particular 5-
    公开号:SU1274624A3
    申请号:SU823455996
    申请日:1982-06-23
    公开日:1986-11-30
    发明作者:Буске Андре；Эймес Ален
    申请人:Санофи (Фирма)；
    IPC主号:
    专利说明:

    This invention relates to an improved process for the preparation of 5- (2-chlorobenzyl) -5,6,7,7a-tetrahydro-4H-thieno (3,2-e) pyridinone-2, which has biological activity in terms of preventing the formation of blood clots. The aim of the invention is to increase the yield of 5- (2-chlorobeneyl) -5,6, 7,7a-tetrahydro-4H-thieno (3,2-e) pyridinone-2 by using N-opto-, chlorobenzyl as the starting material. -2- (5-tertbutoxy (2-thienyl) -ethylamine. EXAMPLE A. With vigorous stirring and while maintaining the temperature, 12.94 g (0.04 mol) of N-orthochlorobenzyl 2- is introduced into the reaction. 5-tert-butoxy) -2-thienyl) / ethylamine and 14 g (0.16 mol) of an aqueous 35% formaldehyde solution. After adding the reagents, keep the reaction medium under stirring for 15 minutes, then 15 MP of chlorine is added to it high methylene. The organic phase is taken up, washed with an aqueous solution of sodium chloride, then dried over sodium sulfate. B. To the solution thus obtained, 8.25 ml of a solution of 4.85 N hydrochloric acid gas in dimethylformamide are added with stirring and at a temperature between 20 and 25 ° C. After 20 minutes of additional stirring, the reaction medium is introduced to 48 ml of aqueous IN sodium bicarbonate solution. The organic phase is introduced, then evaporated under vacuum at a temperature below. Residual aslo is ground into powder by dividing it with 20 ml of ethanol. Thus, after sintering and drying, 5.8 g of 5- (2-chloroenzyl) -5,6,7,7a-tetrahydro-4H-thieno (3,2-s) pyridinone-2 (yield 52%) are obtained. . M.p. 73C. Hemihydrate hydrochloride: so pl. 180 ° C (decomp.). formula of the invention. Method for producing 5- (2-chlorobenzsh1) 5, 6,7,7a-tetrahydro-4H-thieno (3,2-e) pyridinone-2 of the formula g-rk-sn-O, v x-H / P by the interaction a derivative of 2-tertbutoxythiophene with an acidic agent, o tl and h aa yi, and so that, in order to increase the yield of the target product, N-orthochlorobenzyl-2- 5-tertbutoxy- (2- thienyl) 3 ethylamine formula. , NH-CHx-O (CHslsC-O-ilgAj which is reacted with formalin, followed by treatment with hydrogen chloride in dimethylformamide, and the process is carried out at ambient temperature.
    权利要求:
    Claims (1)
    [1]
    Claim
    The method of obtaining 5- (2-chlorobenzyl) 5,6,7,7a-tetrahydro-4H-thieno (3,2-c) pyridinone-2 of the formula by reacting a 2-tert-butoxythiophene derivative with an acid agent, about 25 l and h In order to increase the yield of the target product, Ν-ορτοχπορbenzyl-2- [5-tert-butoxy- (2-thienyl) 3 is used as a derivative of 2-tert-butoxythiophene
    - ethylamine of the formula. _
    35 which is subjected to interaction with formalin, followed by treatment with hydrogen chloride in dimethylformamide, and the process is carried out at ambient temperature.
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    同族专利:
    公开号 | 公开日
    DK291882A|1982-12-31|
    FI822319A0|1982-06-29|
    YU143082A|1985-03-20|
    DE3263114D1|1985-05-23|
    FR2508459A1|1982-12-31|
    FR2508459B1|1984-01-06|
    ES8305372A1|1983-04-01|
    AR231448A1|1984-11-30|
    EP0069001B1|1985-04-17|
    DK153488C|1988-12-19|
    NO157654C|1988-04-27|
    NO822229L|1983-01-03|
    ES514102A0|1983-04-01|
    FI822319L|1982-12-31|
    NO157654B|1988-01-18|
    ZA824619B|1983-04-27|
    NZ200857A|1985-08-30|
    FI71738C|1987-02-09|
    FI71738B|1986-10-31|
    KR840000556A|1984-02-25|
    AU8475482A|1983-01-06|
    CS236483B2|1985-05-15|
    JPS5810583A|1983-01-21|
    HU186944B|1985-10-28|
    PT75157A|1982-07-01|
    IE821315L|1982-11-30|
    CA1187880A|1985-05-28|
    EP0069001A1|1983-01-05|
    IL65985D0|1982-09-30|
    AU548640B2|1985-12-19|
    IE52993B1|1988-04-27|
    AT12772T|1985-05-15|
    GR77202B|1984-09-11|
    US4458074A|1984-07-03|
    DD206556A5|1984-02-01|
    PT75157B|1984-02-21|
    DK153488B|1988-07-18|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    FR53950E|1945-02-02|1947-01-13|Edouard Bataille Sa|Apparatus for the treatment or separation of various materials|
    US4127580A|1975-02-07|1978-11-28|Parcor|Process for the preparation of thieno-pyridine derivatives|
    FR2319642B2|1975-07-30|1979-04-20|Parcor|
    FR2495158B1|1980-11-28|1983-07-22|Sanofi Sa|FR2495156B1|1980-11-28|1983-08-05|Sanofi Sa|
    JP2523045Y2|1989-01-07|1997-01-22|アスモ株式会社|Metering pump|
    FI101150B|1991-09-09|1998-04-30|Sankyo Co|A process for the preparation of tetrahydrothienopyridine derivatives useful as medicaments|
    CA2367373C|1999-03-17|2011-09-20|Daiichi Pharmaceutical Co., Ltd.|Medicinal compositions|
    TWI618906B|2015-06-08|2018-03-21|Ihi Corp|Reactor|
    JP6819199B2|2016-10-13|2021-01-27|株式会社Ihi|Pressure vessel|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    FR8113067A|FR2508459B1|1981-06-30|1981-06-30|
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