• 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 method of obtaining the derivatives of the 7 9-amino-3- (Z-3-cephem-4-carboxy. OOH acid total NH, -pY and COO-CHg where R is methyl, ethyl, 3-methyl-2-butenyl or diphenylmethyl , or their salts, characterized in that the compound of the formula Shg O) NY COO-CHg is reacted with a diazoalkane, such as diazomethane, diazoethane, 1-diazo-3-metip-2-butene or diphenyldiazomethane, in an inert solvent, followed by isolation of the target product in the form of a corresponding derivative in free form or in the form of a salt.
    公开号:SU1149879A3
    申请号:SU731972079
    申请日:1973-11-27
    公开日:1985-04-07
    发明作者:Раймонд Шоветт Роберт
    申请人:Эли Лилли Энд Компани (Фирма)；
    IPC主号:
    专利说明:

    3 side acid, which crystallizes from diethyl ether. Found,%: C A9.51, H 4.40, N 11.25. C, jH, 5 N, Ot, S Calculated,%: C 49.31, H 4.14 N, 11.50. IR absorption peaks at 2.99 µm (amide), 5.75 µm wide. carbonyl) t be alactam and ester) and 5.96 μm (carbonyl amide). IR (ethanol): maximum at 268 µm, b 14600. 5МР (ДР10): dg signals at 7.10 (broad, p. 2H,), 6.22 C Сс.2Н CjHj), 6.20 (p.ЗН , C methoxyp), 5.27s (d.GN, CgH) 4.93-0 (d. 1H,). 4.60 t (p. 2H, CHj of ester) and 2.35 - 1.6-С (sq. 4H, aromatic N.). : Example 3. 7-Amin-3-methox-3-cephem-4-carbrna acid. A solution of 730 mg of 7-amine-3-methoxy-3-cybam fem-4-carboxylic acid laranitrobenzyl ester (prepared as described in Example 2) in 20 ml of water and 20 MP acetonitride is quickly acidified to pH 1 with concentrated hydrochloric acid. acid and immediately titrated to a pH of 2.5 1 and. rast, the thief of sodium hydroxide. " The solution was evaporated to dryness and the residue was dissolved in a mixture of 40 MP of tetrahydrofuran, 80 ml of methanol and 6 ml of water. This solution is hydrogenated in the presence of 730 ml of 5% palladium on carbon (previously reduced to 794 in ethanol) for 2 hours at a hydrogen pressure of 3.5 kg / cm and room temperature. Then the catalyst is filtered off and washed with tetrahydrofuran and water. The combined washings and filtrate are evaporated and the aqueous residue is suspended in ethyl acetate. The pH of the suspension was adjusted to 3.5 and the aqueous layer was separated and dried with ethyl acetate. The aqueous layer was concentrated to a volume of 4 ml and cooled to precipitate 160 mg of 7-amine-3-methoxy-3-cepet-4-carboxylic acid as crystals. . M. Calculated.: C 41.73; H 4.38, N-12,17. Found: C 43.45, H 4.50, N 12.52. Infrared Absorption Maximum at 5.6m u (carbonyl beta-lactam). 51MP (daCO): signals at 6.35С (p. 2H, CjHj), 6.20 С (p. ЗН, С, methoxy), 5.30 € (d. 1H,) and 4.94 C d. 1H , SUN). UV (pH 7 with buffer): max. 268 microns. E 6500. The proposed cephalosporin derivatives are relatively little toxic, suitable for the fight against infections of warm-blooded animals when used parenterally in effective non-toxic doses. They are effective in treating infectious diseases in doses of 25 to 50 mg / kg body weight.
    权利要求:
    Claims (1)
    [1]
    The method of obtaining derivatives of 7 ^ -amino-3-OR-3-cephem-4-carboxylic acid of the general formula where R is methyl, ethyl, 3-methyl-2-butenyl- or diphenymethyl group, or their salts, characterized in that the compound the formulas are reacted with a diazoalkane, such as diazomethane, diazoethane, 1-diazo-3-methyl-2-butene or diphenyldiazomethane, in an inert solvent, followed by isolation of the target product in the form of the corresponding derivative in free form or in the form of a salt.
    类似技术:
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    同族专利:
    公开号 | 公开日
    CH599222A5|1978-05-12|
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    AR204984A1|1976-03-31|
    HU166847B|1975-06-28|
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    OA04512A|1980-03-30|
    HU166396B|1975-03-28|
    EG11046A|1976-11-30|
    DE2359353A1|1974-05-30|
    ES420870A1|1976-04-01|
    JPS4982693A|1974-08-08|
    BR7309298D0|1974-09-24|
    ATA993473A|1976-09-15|
    CS183723B2|1978-07-31|
    RO63112A|1978-08-15|
    NL7316178A|1974-05-30|
    BG21861A3|1976-09-20|
    PL94828B1|1977-08-31|
    YU310573A|1982-02-25|
    ATA993573A|1976-09-15|
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    NL7316177A|1974-05-30|
    GB1456221A|1976-11-24|
    FR2207697B1|1977-04-22|
    IL43661D0|1974-03-14|
    AU6276373A|1975-05-22|
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    FR2207697A1|1974-06-21|
    BG21414A3|1976-05-20|
    JPS49133394A|1974-12-21|
    OA04511A|1980-03-30|
    PH14698A|1981-11-10|
    DD110663A5|1975-01-05|
    YU310473A|1982-02-25|
    AR221315A1|1981-01-30|
    YU36526B|1984-02-29|
    EG11175A|1977-01-31|
    RO63081A|1978-07-15|
    CS183722B2|1978-07-31|
    ES420868A1|1976-04-01|
    PL94245B1|1977-07-30|
    DD110280A5|1974-12-12|
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    BR7309297D0|1974-09-24|
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    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    GB1241656A|1967-08-21|1971-08-04|Glaxo Lab Ltd|Improvements in or relating to cephalosporin compounds|
    GB1277415A|1968-06-14|1972-06-14|Glaxo Lab Ltd|Improvements in or relating to cephalosporin derivatives|AR206201A1|1972-06-29|1976-07-07|Ciba Geigy Ag|PROCEDURE FOR OBTAINING ACID COMPOUNDS 7BETA-AMINO-3-CEFEM-3-01-4-CARBOXILICO0-SUBSTITUIDOS|
    SE428022B|1972-06-29|1983-05-30|Ciba Geigy Ag|7BETA-AMINO-CEFAM-3-ON-4-CARBOXYLIC ACID COMPOUNDS FOR USE FOR THE PRODUCTION OF CEPHALOSPORINE DERIVATIVES|
    US4060688A|1972-11-28|1977-11-29|Eli Lilly And Company|Cephalosporin intermediates|
    US4053469A|1973-02-28|1977-10-11|Shionogi & Co., Ltd.|Intermediates for the preparation of 7-acylamino-3-oxyiminomethyl-3-cephem-4-carboxylic acids|
    CH605997A5|1974-08-30|1978-10-13|Ciba Geigy Ag|
    GB1485488A|1974-10-03|1977-09-14|Farmaceutici Italia|Preparation of cephalosporins|
    US3985746A|1975-03-25|1976-10-12|E. R. Squibb & Sons, Inc.|7-acetamido-3-cephem carboxylates|
    CH622802A5|1975-08-20|1981-04-30|Ciba Geigy Ag|
    US4031084A|1975-10-23|1977-06-21|Eli Lilly And Company|Process for cephalosporin antibiotic intermediates|
    US5350845A|1992-04-08|1994-09-27|Eli Lilly And Company|Process for preparing 7-substituted-amino-3-hydroxy-3-cephem-4-protected carboxy-sulfoxide esters|
    IN181695B|1992-08-10|1998-09-05|Ranbaxy Lab Ltd|
    US5604222A|1993-12-27|1997-02-18|Lupin Laboratories, Ltd.|Method for the preparation of 2-chloro sulfinyl azetidinones|
    US5578721A|1994-07-11|1996-11-26|Lupin Laboratories Limited|Process for preparation of 3-exomethylene cepham sulfoxide esters|
    IN184516B|1996-01-19|2000-09-02|Lupin Laoratories Ltd|
    CN112321611A|2020-10-29|2021-02-05|湖北凌晟药业有限公司|Preparation method of cefixadine mother nucleus|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    US310191A|US3917587A|1972-11-28|1972-11-28|Cephalosporin ethers|
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