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    PROCESS FOR PREPARING CYCLIC COMPOUNDS
    1.
    发明授权
    PROCESS FOR PREPARING CYCLIC COMPOUNDS 失效

    公开(公告)号：KR810000630B1

    公开(公告)日：1981-06-10

    申请号：KR770001948

    申请日：1977-08-22

    Applicant: HOFFMANN LA ROCHE

    Inventor： ROUGE M ,  CONFALONE P ,  USKOKOVIC M ,  PIZZOLATO G

    IPC: A61K31/38 ,  C07D333/36

    Abstract: Title compds. [I; R1 = low alkyl, aryl, aralkyl; R2= H, hydroxy, low alkoxy, amino; R3, R4 = low alkyl, aralkyl, H and their salts, with antiobese and hypolipemic effect, were prepd. Thus. compd.II(R2 = low alkoxy) was reacted with acid to give compd. [Ia , and if necessary, low carbalkoxy group is converted o carboxy, formyl or carbamoyl group, and/or amino group is alkylated with low alkylating agent or aralkylating agent.

    3-(2-chloroethyl)-4-piperidineacetic acid and esters thereof
    4.
    发明授权
    3-(2-chloroethyl)-4-piperidineacetic acid and esters thereof 失效
    3-（2-氯乙基）-4-哌啶酸及其酯

    公开(公告)号：US3833593A

    公开(公告)日：1974-09-03

    申请号：US36730773

    申请日：1973-06-05

    Applicant: HOFFMANN LA ROCHE

    Inventor： GRETHE G ,  USKOKOVIC M

    IPC: C07D211/34 ,  C07D29/24

    CPC classification number: C07D211/34

    Abstract: CIS OR TRANS 2-(1-ACYL-3-VINYL-4-PIPERIDINE)ACETIC ACID ESTERS AND CIS OR TRANS 3-(1-ACYL-3-VINYL-4-PIPERIDINE)PROPIONIC ACID ESTERS, ANTIPODES AND RACEMATES THEREOF, ARE PREPARED, INTER ALIA, FROM THE CORRESPONDING CIS OR TRANS 2OR 3-1 1-ACYL-3-(2-CHLOROETHYL)-4-PIPERIDINE! ACETIC OR PROPIONIC ACID ESTERS, RESPECTIVELY. THE CIS OR TRANS 2- OR 3-(1ACYCL-3-VINYL-4-PIPERIDINE)ACETIC OR PROPIONIC ACID ESTERS ARE USEFUL AS INTERMEDIATES FOR THE SYNTHESIS OF QUININE AND QUINIDINE AND ANALOGS AND STEROISOMERS THEREOF.

    Processes for the preparation of desa-androst-9-en-5-ones and desa-pregn-9-en-5-ones
    7.
    发明授权
    Processes for the preparation of desa-androst-9-en-5-ones and desa-pregn-9-en-5-ones 失效
    制备DESA-ANDROST-9-EN-5-ONES和DESA-PREGN-9-EN-5-ONES的方法

    公开(公告)号：US3847945A

    公开(公告)日：1974-11-12

    申请号：US73732968

    申请日：1968-06-17

    Applicant: HOFFMANN LA ROCHE

    Inventor： USKOKOVIC M

    IPC: C07C59/215 ,  C07C59/80 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07D11/00

    CPC classification number: C07C309/73 ,  C07C59/215 ,  C07C59/80 ,  C07C309/65 ,  C07C309/66 ,  C07C2603/14 ,  C07C2603/16

    Abstract: 1. A PROCESS FOR THE PREPARATION OF A DESA-ANDROST-9EN-5-ONE OF THE FORMULA:

    2-R3,3-R1,3-R2,3A,6-DI(H3C-),7-(O=),X-PERHYDRO-5A,6-

    DIDEHYDRO-BENZ(E)INDENE

    WHEREIN R1 IS HYDROXY, LOWER ALKANOYLOXY, CARBOXYLOWERALKANOYLOXY, BENZOYLOXY, TETRAHYDROPYRANYLOXY, BENZYLOXY, BENZHYDRYLOXY, TRITYLOXY, ALLYLOXY, OR LOWER ALKOXYLOWER ALKOXY; R2 IS HYDROGEN OR LOWER ALKYL; R1 AND R2 TAKEN TOGETHER ARE SELECTED FROM THE GROUP CONSISTING OF (17B-OH, 17A-LOWER ALKANOIC ACID LACTONE), LOWER ALKYLENEDIOXY AND OXO; R3 IS HYDROGEN, LOWER ALKYL, HYDROXY, LOWER ALKANOYLOXY, CARBOXYLOWERALKANOYLOXY, BENZOYLOXY, TETRAHYDROPYRANYLOXY, BENZYLOXY, BENZHYDRLOXY, TRITYLOXY, ALLYLOXY, OR LOWER ALKOXY-LOWER ALKOXY; AND X IS A SUBSTITUENT IN THE 6- OR 7-POSITION SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER ALKANOYLTHIO AND HALOGEN; COMPRISING ESTERIFYING AN 11-HYDROXY-ANDROST-4-EN-3-ONE HAVING THE FORMULA:

    3-(O=),11-(HO-),16-R3,17-R1,17-R2-ANDROSTAN-4(5)-ENE

    WHERE R1,R2,R3 AND X ARE AS ABOVE; TO FORM A LEAVING GROUP IN THE 11-POSITION SELECTED FROM THE GROUP CONSISTING OF TOLUENE SULFONATE, LOWER ALKYL SULFONATE AND NITROPHENYL SULFONATE; SUBJECTING THE RESULTING ANDROST-4-EN-3-ONE WITH THE LEAVING GROUP IN THE 11-POSITION TO OXIDATIVE RING OPENING TO FORM THE CORRESPONDING 5 - OXO - 11 - (LEAVING GROUP)-3,5-SECOA-NORANDROSTAN-3OIC ACID, FORMING AN ALKAI METAL SALT OF SAID ACID; AND PYROLYZING SAID ALKALI METAL SALT BY HEATING SAID ALKALI METAL SALT TO A TEMPERATURE OF ABOUT 200*C. TO ABOUT 350* C. TO FORM SAID DESA-ANDROST-9-EN-5-ONE.

    Process and intermediates for quinine,quinidine and derivatives thereof
    10.
    发明授权
    Process and intermediates for quinine,quinidine and derivatives thereof 失效
    喹啉，喹啉及其衍生物的方法和中间体

    公开(公告)号：US3753992A

    公开(公告)日：1973-08-21

    申请号：US3753992D

    申请日：1971-12-27

    Applicant: HOFFMANN LA ROCHE

    Inventor： GUTZWILLER J ,  USKOKOVIC M

    IPC: C07D211/34 ,  C07D211/92 ,  C07D401/06 ,  C07D453/04 ,  C07D43/24

    CPC classification number: C07D401/06 ,  C07D211/34 ,  C07D211/92 ,  C07D453/04 ,  Y10S514/821

    Abstract: QUININE, QUINIDINE, THEIR ANTIPODES OR RACEMATES AND DERIVATIVES THEREOF, ARE PREPARED BY (A) CYCLIZING THE CORRESPONDINGLY SUBSTITUTED 4 - (3-(1-CHLORO-3(R)-ALKYL(OR ALKENYL) - 4(R)-PIPERIDYL)-1-OXOPROPYL)QUINOLINES, ANTIPODES OR RACEMATES THEREOF, TO THE CORRESPONDING 4-(5-(R)ALKYL(OR ALKENYL)-4(S)-QUINUCLIDIN-2(S) OR 2 (R)-YLCARBONYL)QUINOLINES, ANTIPODES OR RACEMATES THEREOF, AND (B) STEREOSELECTIVELY REDUCING THE PRODUCTS OF STEP (A) TO A(S)-(5(R)-ALKYL(OR ALKENYL)-4(S)-QUINUCLIDIN-2(R)-YL)4-QUINOLINEMETHANOLS, ANTIPODES OR RACEMATES THEREOF USING DI ALKYLALUMINUM HYDRIDE, AND A(R)-(5(R)-ALKYL(OR ALKENYL)-4(S)-QUINUCLIDIN-2(S)-YL) - 4 - QUINOLINEMETHANOLS, ANTIPODES OR RACEMATES THEREOF. VARIOUS INTERMEDIATES AND THE END PRODUCTS ARE USEFUL ANTIMALARIAL AND ANTIARRHYTHMIC AGENTS.

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