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    Process for preparation of 6-azido-4,6-bis-dehydro-steroids
    1.
    发明授权
    Process for preparation of 6-azido-4,6-bis-dehydro-steroids 失效
    6-AZIDO-4,6-BIS-DEHYDRO-STEROIDS的制备方法

    公开(公告)号：US3665017A

    公开(公告)日：1972-05-23

    申请号：US3665017D

    申请日：1970-07-24

    申请人： SCHERING CORP

    发明人： TEUTSCH GEORGE J ,  SHAPIRO ELLIOT L

    IPC分类号： C07J41/00 ,  C07C173/00

    CPC分类号： C07J41/0027

    摘要： 6-Azido-4,6-bis-dehydro-steroids are prepared by treating a 6 Beta -azido-7 Alpha -acyloxy-4-dehydro-steroid which is saturated at C-1 and C-2, with a tetraalkylammonium halide in an aprotic solvent. Preferred species include the preparation of 6-azido-4,6pregnadienes of the corticoid and progesterone series by treatment of a 6 Beta -azido-7 Alpha -acyloxy-4-pregene of the corticoid or progesterone series which is saturated at C-1 and at C-2 and wherein said 7 Alpha -acyloxy is a member selected from the group consisting of 7 Alpha -lower alkanoyloxy and 7 Alpha hydrocarbonsulfonyloxy having up to seven carbon atoms with a tetraalkylammonium halide in an aprotic solvent. 6-Azido-6-dehydrocortisone acetate having enhanced antiinflammatory activity is prepared by treating a member selected from the group consisting of 6 Beta -azido-7 Alpha acetoxy-4pregnene-17 Alpha ,21-diol-3,11,20-trione 21-acetate and 6 Beta azido-7 Alpha methanesulfonyloxy-4-pregnene-17 Alpha ,21-diol3,11,20-trione 21-acetate with tetramethylammoniumfluoride in acetonitrile.

    Process for the preparation of 6-azido-11beta-hydroxy-4,6-pregnadienes and novel intermediates produced thereby
    8.
    发明授权
    Process for the preparation of 6-azido-11beta-hydroxy-4,6-pregnadienes and novel intermediates produced thereby 失效
    制备6-AZIDO-11BETA-羟基-4,6-孕酮的方法及其生产的新型中间体

    公开(公告)号：US3707484A

    公开(公告)日：1972-12-26

    申请号：US3707484D

    申请日：1971-06-15

    申请人： SCHERING CORP

    发明人： RAUSSER RICHARD C ,  SHAPIRO ELLIOT L

    IPC分类号： C07J5/00 ,  C07J71/00 ,  C07C173/10

    CPC分类号： C07J5/0076 ,  C07J71/001 ,  Y10S435/85

    摘要： AN IMPROVED PROCESS FOR PREPARING PHARMACOLOGICALLY ACTIVE 6-AZIDO-11B-HYDROXY-4,6-PREGNADIENE-3,20-DIONES COMPRISES PREPARING AN 11B-ACYLOXY DERIVATIVE OF A 6A,7AOXIDO-11B-HYDROXY-4-PREGNENE-3,20-DIONE, SAID 11B-ACYLOXY BEING A MEMBER SELECTED FROM THE GROUP CONSISTING OF 11B-FORMYLOXY-, 11B-ACETOXY- AND 11B-HALOGENOACETOXY-; TREATING SAID 6A,7A-OXIDO-11B-ACYLOXY-4-PREGNENE-3,20DIONE WITH AN ALKALI METAL AZIDE IN A NON-REACTIVE, ORGANIC SOLVENT; TREATING THE THEREBY FORMED 6B-AZIDO-7A-HYDROXY11B-ACYLOXY-4-PREGNENE-3,20-DIONE OR A 7A-ESTER THEREOF WITH CONCENTRATED HYDROCHLORIC ACID IN A LOWER ALKANOIC ACID TOGETHER WITH AN INERT SOLVENT OR, ALTERNATIVELY, TREATING A 7A-ESTER THEREOF WITH A TETRAALKYLAMMONIUM HALIDE IN AN APROTIC SOLVENT, SAID 7A-ESTER BEING EITHER A 7A-LOWER ALKANOATE OR A 7A-HYDROCARBONSULFONATE; FOLLOWED BY HYDROLYSIS OF THE 6-AZIDO-11B-ACYLOXY-4,6-PREGNADIENE-3,20DIONE THEREBY FORMED. IF DESIRED, HYDROLYSIS OF THE 11ACYLOXY MAY BE CARRIED OUT ON THE 6B-AZIDO-7A-HYDROXY11B-ACYLOXY-4-PREGNENE-3,20 DIONE INTERMEDIATE. INTERMEDIATES DESCRIBED AND CLAIMED IN THIS PROCESS ARE 6B-AZIDO-7A-HYDROXY-11!-ACYLOXY-4PREGNENE-3,20DIONES, THE 7A-ESTERS THEREOF AND 6-AZIDO-11B-ACYLOXY-4,6PREGNADIENE-3,20-DIONES.