• 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:
    A compound having pharmacological properties comprising the structural formula <IMAGE> (I) wherein R is selected from the isopropyl, n-octyl, n-butyl or isobutyl groups; R1 is selected from the 1-naphthyloxymethyl, (2-allylphenoxy)-methyl, 4-nitrophenyl, {2-[(tetrahydrofurfuryl)oxy-]-phenoxy}-methyl, [4-(2-methoxyethyl)phenoxy]methyl, 4-isopropylthiophenyl, 4-acetaminophenoxymethyl groups; and R2 represents a hydrogen atom or a methyl group. A method for synthetizing the compound is also disclosed comprising the cyclization of aminoalcohol or halogenurethane.
    公开号:SU947160A1
    申请号:SU782664731
    申请日:1978-09-22
    公开日:1982-07-30
    发明作者:Пестеллини Витторио；Гелардони Марио；Бъянкини Клаудио；Дел Сольдато Пъеро；Вольтерра Джованна；Мели Альберто
    申请人:А.Менарини С.А.С. (Фирма)；
    IPC主号:
    专利说明:

    (54) 3-I-OKTIL-4-METHYL-5- (4GIZOPROPYLTIOPHENYL) - .2-OXAZOLIDON OWNE WATER-EXTENDING
    one .
    The invention relates to new biologically active chemical sedans, Specifically to 3-n-octyl-4-methyl-5- (4-isopropyl-lithi-Sch1l) -2-oxazole to the formula I / t
    dHs
    -N-H- (ijH ,,
    SNS
    dH
    having a vasodilatory effect.
    This property suggests the possibility of using this compound in medicine.
    It is known to use as adjuvants with a vasodilator effect, prizvodnyh isoquinoline, purine and pyrimidine 1.
    The purpose of the invention is to expand the arsenal of means of influencing a living organism and the vasodilator effect among new classes of compounds.
    ACTION
    This goal is achieved by combining formula 1 as a vasodilator substance.
    3-n-Octyl-4-metip-5- (4-isopropyl-thiophenyl) -2-oxazolidone is obtained by cyclization of 1- (4-isopropyl-thiophenyl) -2-n-α-octylaminopropanol of the formula G1
    (iH- - /-- (JH- с1нз
    10 (he 1Sh-n-1vN, 7.
    with carbonyl chloride in an appropriate solvent, for example in dioxane, in an alkaline medium, or by cyclization of 1- (4-isopropylthiophenyl 2-chloropropyl-K- (n-oxyl) carbamate of the formula UI
    (1Нз
    (1n4n-enz
    dHI -.
    yn /
    o- (i-NH-H- (i, H, 7
    about
    权利要求:
    Claims (2)
    [1]
    in the presence of Pcr1 oxide meta / la. 947 Example 1. 0.11 MOS. 20% of the ого th | jQc№opa carbonyl-hp-li-b is slowly added to 0.1 mol. 1- (4-iso-; propipti ofennl) -2nn-okgyl-aminopropanol (g.pl. 62-63 0) in 100 ml of a common pump solvent, such KaKjBHOKcaH, and Yu ml of trt lamnna. After the mixture was stirred for several hours at room temperature, the mixture (} glutrutot and concentrated. The resulting residue was recrystallized from dioxane. Example
    [2]
    2. About / 1 mol, crude 1- (4- and 90-propyl-thiophenyl) -2-eslorprop-1-1- (n-oxgyl) carbamate obtained by treatment with 1- (4-isopropyl-Iophenyl) -2-x-Lorelnopole nol with n-octylisodienate, is heated in reverse cooler in 100 ml of a suitable solvent, such as ethanol or water, containing 0.11 mol. alkaline hydroxide to etalla. The solvent is distilled off in vacuo, the 1 Puffy product is recrystallized from the corresponding solvent. 3-H Octyl-4-broom-5- (4-.isopropylthiophenyl) -2-oxazolidide has a melting point of 4850 C .... .-- IR spectrum V „,, clause (cm -): 1735JCO) .: YAM FL.cneKTD (DM Cq,). (G (ppm): 0.8 /,, O, 9-1.6 (mЗxCHз- 6xCH2), 2.8- -3.4 (g. СНг + СН). 4.0-4.4Cw.CHJ , 5,6 (d, CH) 7,1-7,5 (nCt, H4). 3-n-Octyl-4-methyl-5- {4 41 zproylgallio-. Feil) -2-oxazolido shows sousi a) expanding effect at the cerebral level. When tested for protective action against anoky caused by cerebral asphyxia, it was found that the effect was still intense even a few hours after applying egogoggolgoo, LD 5O (OS) above 15OO mg / kg for mice. Claims of the invention 3-n-Octyl-4-methyl-5- (4-isopropylthiofesh1l) -2-oxazolion of the formula -dHj Hz7 -H-deHo yn-A1D7D nobladakcii vasodilating ayeshviy. Sources of information taken into account during the examination 1. Mashkovsky M. D. Lekarsgvennoy means. M., "Mediaea, t. 1, 1972, p. 345-357.
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    同族专利:
    公开号 | 公开日
    JPS5459271A|1979-05-12|
    IT1109002B|1985-12-16|
    ES473547A1|1979-04-16|
    GB2005261A|1979-04-19|
    AR218933A1|1980-07-15|
    NL7809647A|1979-03-26|
    DD138978A5|1979-12-05|
    DK416278A|1979-03-23|
    DE2839907A1|1979-04-05|
    AU519531B2|1981-12-10|
    BE870675A|1979-01-15|
    ZA785249B|1979-09-26|
    FR2404001B1|1980-10-31|
    CA1118779A|1982-02-23|
    US4188323A|1980-02-12|
    SE7809935L|1979-03-23|
    FR2404001A1|1979-04-20|
    YU225278A|1983-01-21|
    GB2005261B|1982-03-17|
    HU177872B|1982-01-28|
    AU4005978A|1980-03-27|
    AT362368B|1981-05-11|
    ATA674278A|1980-10-15|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    FR1284520A|1958-11-03|1962-02-16|American Cyanamid Co|Process for the preparation of novel 2-oxazolidinone compounds|
    US3062826A|1959-06-19|1962-11-06|Robins Co Inc A H|3, 4-disubstituted phenoxymethyl oxazolidones|
    US3062828A|1962-02-27|1962-11-06|Robins Co Inc A H|5--2-oxazolidones|
    US3637852A|1963-08-26|1972-01-25|Boehringer Sohn Ingelheim|1-phenoxy-2-hydroxy-3-isopropylamino-propanes and salts thereof|
    US3459782A|1963-08-26|1969-08-05|Boehringer Sohn Ingelheim|1-substituted phenoxy-2-hydroxy-3-isopropylamino-propanes|
    US3331850A|1964-05-13|1967-07-18|Upjohn Co|5--2-oxazolidinethiones|
    CH490405A|1965-07-09|1970-05-15|Ciba Geigy|Process for the preparation of new oxazolidine derivatives|
    US3541130A|1967-02-06|1970-11-17|Boehringer Sohn Ingelheim|1--2-hydroxy-3-tert.-butylamine propanes|
    GB1180089A|1967-10-20|1970-02-04|Delalande Sa|Acetylenic Derivatives of 2-Oxazolidinones and processes of preparation|
    SE354851B|1970-02-18|1973-03-26|Haessle Ab|
    FR2338268B1|1976-01-16|1980-06-20|Nativelle Spa|US4754047A|1979-08-16|1988-06-28|American Cyanamid Company|Phenylethanolamine derivatives and acid addition salts thereof for enhancing the growth rate of meat-producing animals and/or improving the efficiency of feed utilization thereby|
    US4522822A|1980-12-22|1985-06-11|American Cyanamid Company|Phenylethane derivatives and acid addition salts thereof for increasing lean meat deposition and/or improving lean meat to fat ratio in warm blooded animals|
    US4501751A|1980-12-22|1985-02-26|American Cyanamid Company|Phenylethanolamine derivatives and acid addition salts thereof for enhancing the growth rate of meat-producing animals and improving the efficiency of feed utilization thereby|
    US4728661A|1985-11-13|1988-03-01|Merrell Dow Pharmaceuticals Inc.|Cardiotonic phenyl oxazolones|
    US4698353A|1985-11-13|1987-10-06|Merrell Dow Pharmaceuticals Inc.|Cardiotonic heterocyclic oxazolones|
    US4670450A|1985-11-13|1987-06-02|Merrell Dow Pharmaceuticals Inc.|Cardiotonic thiazolones|
    DE69132691T2|1990-06-07|2002-06-20|Astrazeneca Ab|Indole derivatives as 5-HT1-like agonists|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    IT779578A|IT1109002B|1977-09-22|1977-09-22|DERIVATIVES OF 2 OXAZOLIDONE AND THEIR PREPARATION METHODS|
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