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    6-substituted-13-polycarbon-alkyl-18 19-dinorpregn-4-en-3-ones
    2.
    发明授权
    6-substituted-13-polycarbon-alkyl-18 19-dinorpregn-4-en-3-ones 失效
    6-取代的13-多羧基 - 烷基-19-十九烷基-4-EN-3-ONES

    公开(公告)号：US3644440A

    公开(公告)日：1972-02-22

    申请号：US3644440D

    申请日：1969-05-19

    Applicant: AMERICAN HOME PROD

    Inventor： DOUGLAS GEORGE H ,  TELLER DANIEL M ,  SMITH HERCHEL

    IPC: A61K31/57 ,  C07J7/00 ,  E06B9/17 ,  C07C169/32 ,  C07C169/34

    CPC classification number: A61K31/57 ,  C07J7/00

    Abstract: NEW STEROIDS OF THE 13 - POLYCARBONALKYL-18,19-DINORPREGN-4-EN-3-ONE SERIES AND $6-DEHYDRO ANALOGS THEREOF, SUBSTITUTED AT C6 BY METHYL, CHLORO, BROMO OR FLUORO; AT C17 BY HYDROGEN, HYDROXY OR ACYLOXY, AND WHEREIN C20 IS CARBONYL, HYDROXYMETHYLENE OR ACYLOXYMETHYLENE (I) HAVE HORMONAL ACTIVITY, ESPECIALLY AS PROGESTATIONAL AND ANTI-ESTROGENIC AGENTS. MEANS TO OBTAIN THEM ARE PROVIDED COMPRISING (A) HYDROGENATING THE CORRESPONDING 6-METHYLENE COMPOUND (II) TO FORM THE 6A-MEHTYL-4-EN-3-ONE (ID); (B) REARRANGING (II) WITH A WEAK BASE+PD/C TO FORM THE 6-METHYL-4,6-DIEN-3-ONE (IE); (C) CHLORINATING OR BROMINATING THE CORRESPONDING 3-ENOL ESTER (III) TO FORM THE 6-CHLORO OR BROMO-4-EN-3-ONE (IF); AND (D) EITHER (1) DEHYDROGENATING (IF) WITH CHLORANIL TO FORM THE 6CHLORO OR -BROMO-4,6-DIEN-3-ONE (IG), OR PREFERABLY, (2) REACTING THE CORRESPONDING 6A,7A-EPOXIDE (IV) WITH HC1, HBR OR HF TO FORM THE CORRESPONDING 6-CHLORO, -BROMO OR -FLUORO-4,6-DIEN-3-ONE (IH).

    13beta-alkyl-17-hydroxygona-4,14-dien-3-ones
    4.
    发明授权
    13beta-alkyl-17-hydroxygona-4,14-dien-3-ones 失效
    13BETA-ALKYL-17-HYDROXYGONA-4,14-DIEN-3-ONES

    公开(公告)号：US3577410A

    公开(公告)日：1971-05-04

    申请号：US3577410D

    申请日：1968-07-30

    Applicant: AMERICAN HOME PROD

    Inventor： TELLER DANIEL M ,  DOUGLAS GEORGE H ,  SMITH HERCHEL

    IPC: C07J21/00 ,  C07C173/00

    CPC classification number: C07J21/00

    Abstract: NEW STEROIDS OF THE 13B-ALKYL-17B-HYDROXYGONA-4,14DIEN-3-ONE SERIES OPTIONALLY SUBSTITUTED AT C-7 AND C-17 BY A-METHYL (I) ARE PROVIDED BY EITHER (A) ISOMERIZING A CORRESPONDING 17-HYDROXY-13B-ALKYLGONA-5(10),14-DIEN-3ONE (II) OR (B) REACTING WITH A METHYL GRIGNARD REAGENT A CORRESPONDING 17-HYDROXY-13B-ALKYLGONA-4,6,14-TRIEN-3ONE (III). MEANS ARE PROVIDED TO PREPARE THE INTERMEDIATE COMPOUNDS II AND III. COMPOUNDS I AND IA ARE ANDROGENICALLY-ACTIVE IN WARM-BLOOD LOWER ANIMALS.

    {60 ,3-Diphenyl-2-oxazolidinemethanol compounds
    6.
    发明授权
    {60 ,3-Diphenyl-2-oxazolidinemethanol compounds 失效
    {60,3,3-二苯基-2-恶唑烷甲醇化合物

    公开(公告)号：US3891665A

    公开(公告)日：1975-06-24

    申请号：US42922373

    申请日：1973-12-28

    Applicant: AMERICAN HOME PROD

    Inventor： TELLER DANIEL M ,  GUINOSSO CHARLES J ,  BELL STANLEY C ,  DOUGLAS GEORGE H

    IPC: C07D263/06 ,  C07D85/26

    CPC classification number: C07D263/06

    Abstract: 2-Aroyloxazolidine 2-aroyltetrahydrooxazines and 2-( Alpha aralkanol)-oxazolidine derivatives possessing central nervous system depressant activity are prepared by condensing substituted phenyl glyoxals with 1-amino-2 alcohols or 1-amino-3- alcohols to form a ketone and subsequently alkylating the product to the tertiary alcohol.

    Abstract translation: 通过将取代的苯基乙二醛与1-氨基-2-醇或1-氨基-3-醇缩合形成酮，制备2-芳基恶唑烷2-芳酰基四氢恶嗪和具有中枢神经系统抑制活性的2-（α-烷基醇） - 恶唑烷衍生物 随后将产物烷基化成叔醇。

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