5,6,7,8-tetrahydro-2,5(and 4,5)-dioxo-1-benzopyrans
    3.
    发明授权
    5,6,7,8-tetrahydro-2,5(and 4,5)-dioxo-1-benzopyrans 失效
    5,6,7,8-四氢呋喃-2,5(和4,5) - 二氧代-1-苯并噻吩

    公开(公告)号:US3823164A

    公开(公告)日:1974-07-09

    申请号:US31524772

    申请日:1972-12-14

    IPC分类号: C07D311/08 C07D7/26

    CPC分类号: C07D311/08

    摘要: COMPOUNDS OF THE FORMULA:

    2,3-(-X-O-),R,R2-CYCLOHEX-2-EN-1-ONE

    IN WHICH X IS THE MOIETY

    -CO-C(-R3)=C(-CO-Z)-

    Z IS A MEMBER SELECTED FOR THE GROUP CONSISTING OF

    -OR4, -N(-R5)-R6

    -CL,-BR, AND -OM; R, R2, R3, AND R5 ARE INDEPENDENTLY SELECTED FROM THE GROUP CONSISTING OF -H, LOWER ALKYL, PHENYL AND BENZYL, R6 IS SELECTED FROM THE GEOUP CONSISTING OF -H, LOWER ALKYL, PHEMYL, BENZYL, LOWER DIALKYLAMINOALKYL AND CYCLOALKYL OF 3 TO 10 CARBON ATOMS, AND WHEN TAKEN WITH R5 AND THE NITROGEN ATOM TO WHICH THEY ARE BONDED FORMS THE MORPHOLINO, PIPERIDINO AND PIPERAZINO GROUPS, AND M IS SELECTED FROM ALKALI METAL CATION AND -NH4, ARE IMMUNO-INFLAMMATORY AGENTS POSSESSING ANTIALLERGIC AND ANTIINFLAMMATORY ACTIVITY. THE COMPOUNDS OF THSI INVENTION ARE ALSO INTERMEDIATES FOR THE SYNTHESIS OF KNOWN CHROMONE AND COUMARIN DERIVATIVES.

    Retrosteroid a ring formation
    4.
    发明授权
    Retrosteroid a ring formation 失效
    回归环形成

    公开(公告)号:US3766213A

    公开(公告)日:1973-10-16

    申请号:US3766213D

    申请日:1971-01-06

    申请人: HOFFMANN LA ROCHE

    摘要: A PROCESS FOR PRODUCING KNOWN RETROSTEROIDS OF THE FORMULA:

    1-R1,2-R2,3-(O=),4-R4,6-R6,7-R7,11-R11,16-R16-ANDROST-4-

    ENE WHERE C17 IS Z

    WHEREIN: R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R2 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R6 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER AKLANOYLTHIO, AND HALO; R7 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER ALKANOYLTHIO, AND HALO; R11 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY AND LOWER ALKANOYLOXY; R16 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, HYDROXY, LOWER ALKOXY, LOWER ALKANOYLOXY, AND, WHEN THE 17B-SUBSTITUENT IS ACETYL OR SUBSTITUTED ACETYL, FLUORINE; Z IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF CARBONYL, (17B-HYDROXY-17-A-LOWER ALKANOIC ACID LACTONE), AND

    >C(-R17ALPHA)-R17BETA

    R17B IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROXY, LOWER ALKANOYLOXY, AND

    Y-CH2-CO-

    Y IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALO, AND HYDROXY; R17A, WHEN R17B IS HYDROXY AND LOWER ALKANOYLOXY, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALIPHATIC HYDROCARBYL, AND WHEN R17B IS

    Y-CH2-CO-

    IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN ALKYL, HYDROXY, LOWER ALKANOYLOXY, AND HALO; Q WHEN TAKEN ALONE, IS OXO; T1 WHEN TAKEN ALONE, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF ALKALI METAL OXY AND LOWER ALKOXY; AND T1 AND Q, WHEN TAKEN TOGETHER ARE NITROLO.

    Furfuryl amino-coumarins
    5.
    发明授权
    Furfuryl amino-coumarins 失效
    芳香族氨基酸

    公开(公告)号:US3726902A

    公开(公告)日:1973-04-10

    申请号:US3726902D

    申请日:1971-07-27

    IPC分类号: C07D311/16 C07D7/26

    CPC分类号: C07D311/16 Y10S514/929

    摘要: THE PRESENT INVENTION RELATES TO NEW COUMARIN COMPOUNDS USEFUL AS CORONARY DILATORS AND HAVING THE FORMULA

    2-(O=),3-(R-CH2-CH(-OOC-C6H4-(R3)M)-CH2-),4-R1,(R2)2-2H-

    CHROMENE

    OR THE HYDROCHLORIC ACID ADDITION SALTS THEREOF, AND TO METHODS OF PREPARING SAME EITHER BY ACYLATING, IN THE PRESENCE OF ACID-BINDING AGENTS, IF DESIRED, COUMARIN DERIVATIVES HAVING THE FORMULA

    2-(O=),3-(R''-CH2-CH(-OH)-CH2-),4-R1,(R2)2-2H-CHROMENE

    WITH ACYLATING AGENTS SELECTED FROM THE GROUP CONSISTING OF ALKOXYBENZOIC ACID HAVING THE FORMULA

    HOOC-C6H4-(R3)M

    AND FUNCTIONAL DERIVATIVES THEREOF, OR BY CONDENSING, IN THE PRESENCE OF ACID-BINDING AGENTS, IF DESIRED, COUMARIN DERIVATIVES HAVING THE FORMULA

    2-(O=),3-(R4-CH2-CH(-OOC-C6H4-(R3)M)-CH2-),4-R1,(R2)2-

    2H-CHROMENE

    WITH AN AMINE HAVING THE FORMULA RH, WHEREIN R IS SELECTED FROM SECONDARY FURFURYLAMINO AND SECONDARY TETRAHYDROFURFURLAMINO, WHICH IS BOUND VIA THE NITROGEN ATOM, R1 IS SELECTED FROM THE GROUP CONSISTING OF ALKYL RADICALS HAVING 1-4 CARBON ATOMS AND PHENYL, R2 IS SELECTED FROM THE GROUP CONSISTING OF 5,6-, 6,7-, AND 7,8POSITIONED ALKOXY GROUPS HAVING 1-4 CARBON ATOMS, R3 IS SELECTED FROM ALKOXY GROUPS HAVING 1-4 CARBON ATOMS, R4 IS SELECTED FROM THE GROUP CONSISTING OF CHLORINE AND BROMINE, R'' IS SELECTED FROM THE GROUP CONSISTING OF SECONDARY FURFURLAMINO AND SECONDARY TETRAHYDROFURFURYLAMINO, AND M IS SELECTED FROM THE GROUP CONSISTING OF 1, 2, AND 3.

    Naphthalides and phthalides
    9.
    发明授权
    Naphthalides and phthalides 失效
    萘甲酸酯和对苯二甲酸酯

    公开(公告)号:US3833615A

    公开(公告)日:1974-09-03

    申请号:US10386471

    申请日:1971-01-04

    申请人: POLAROID CORP

    发明人: SIMON M WALLER D

    摘要: THIS INVENTION RELATES TO PHENOL PHTHALEIN INDICATOR DYES CONTAINING AS THE RING-CLOSING MOIETY, A NAPHTHALIDE GROUP OR A CARBOXYPHTHALIDE GROUP POSSESSING A CARBOXY SUBSTITUENT IN EITHER THE 4- AND/OR 7-POSITION OF THE PHTHALIDE RING. IN A PREFERRED EMBODIMENT, THE PHENOL RADICALS ARE SUBSTITUTED WITH A HYDROGEN-BONDING GROUP ON A CARBON ATOM ADJACENT TO THE CARBON ATOM CONTAINING THE PHENOLIC -OH. THESE DYES, DUE TO THE NAPHTHALIDE OR CARBOXYPHTHALIDE RING-CLOSING MOIETY EXHIBIT IMPROVED STABILITY IN HIGHLY ALKALINE MEDIA AND WHEN SUBSTITUTED WITH HYDROGEN-BONDING GROUPS AS IN THE THE PREFERRED EMBODIMENT, POSSESS A RELATIVELY HIGH PKA AS WELL.

    Process for the preparation of 3-(beta dialkylamino-ethyl)-4-alkyl-7-carboethoxymethoxycoumarins
    10.
    发明授权
    Process for the preparation of 3-(beta dialkylamino-ethyl)-4-alkyl-7-carboethoxymethoxycoumarins 失效
    制备3-(β-二甲基氨基乙基)-4-烷基-7-碳代醇甲氧基甲基的方法

    公开(公告)号:US3813415A

    公开(公告)日:1974-05-28

    申请号:US27626272

    申请日:1972-07-28

    IPC分类号: C07D311/16 C07D7/26

    CPC分类号: C07D311/16

    摘要: 3 - (BETA-DIALKYLAMINOETHYL) - 4-ALKYL-7-CARBOETHOXYMETHOXYCOUMARIN OF THE FORMULA:

    3-(R2-N(-R3)-CH2-CH2-),4-R1,7-(C2H5-OOC-CH2-O-)-

    2H-CHROMEN-2-ONE

    IN WHICH R1, R2 AND R3 STAND FOR A LOWER ALKYL GROUP CONTAINING 1-3 CARBON ATOMS AND ITS HYDROHALIDES. THE ABOVE-MENTIONED COMPOUNDS PROVED TO BE DRUGS USED IN CASE OF CIRCULATORY SYSTEM DISEASES. THE SAID COMPOUNDS ARE PRODUCED IN THE REACTION OF RESORCINOL WITH A GAMMA-BUTYROLACTONE DERIVATIVE OF THE FORMULA:

    3-(R1-CO-)TETRAHYDROFURAN-2-ONE

    OR BY ADDITION OF A HYDROGEN HALIDE IN THE PRESENCE OF PHOSPHOROUS ACID (PIII) THEN THE THUS OBTAINED 3-(BETAHALOETHYL-4-ALKYL-7-HYDROXYCOUMARIN IS SUBJECTED TO REACTION WITH A HALOACETIC ACID ETHYL ESTER IN THE PRESENCE OF ALKALI METAL CARBONATE AND A CATALYTIC QUANTITY OF DIETHYLFORMAMIDE OR WATER AND POTASSIUM IODIDE. THE THUS OBTAINED 3-(BETA-HALOETHYL)-4-ALKYL-7-CARBOETHOXYMETHOXYCOUMARIN IS SUBJECTED TO REACTION WITH A DIALKYLAMINE AND THE THUS OBTAINED PRODUCT IS ISOLATED AS A COMPLEX COMPOUND WITH ZINC CHLORIDE AND IF NECESSARY CONVERTED TO THE HYDROHALIDE.