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    Process for the synthesis of 6-bromo-17,21-dihydroxy 3,11,20-trioxo-1,4-pregnadienes 17,21-diesters
    1.
    发明授权
    Process for the synthesis of 6-bromo-17,21-dihydroxy 3,11,20-trioxo-1,4-pregnadienes 17,21-diesters 失效
    合成6-溴-17,21-二羟基3,11,20-三氧代-1,4-孕es烯17,21-二酯的方法

    公开(公告)号：US4440690A

    公开(公告)日：1984-04-03

    申请号：US453844

    申请日：1982-12-27

    申请人： Elliot L. Shapiro ,  Lawrence E. Finkenor

    发明人： Elliot L. Shapiro ,  Lawrence E. Finkenor

    IPC分类号： C07J5/00

    CPC分类号： C07J5/0076 ,  C07J5/0053

    摘要： Disclosed is an improved process for the synthesis of 6-bromo-17,21-dihydroxy-3,11,20-trioxo-1,4,-pregnadienes 17,21-diesters. In particular, this invention relates to the conversion of 17,21-dihydroxy-3,11,20-trioxo-1,4-pregnadienes 17,21-diesters to 6-borom-17,21-dihyroxy-3,11,20-trioxo-1,4-pregnadienes-17-21-diesters via bromination under ionic conditions, e.g. bromine in acetic acid.

    摘要翻译： 公开了一种用于合成6-溴-17,21-二羟基-3,11,20-三氧代-1,4-辛二烯17,21-二酯的改进方法。 特别地，本发明涉及将17,21-二羟基-3,11,20-三氧代-1,4-孕代二烯17,21-二酯转化成6-硼烷-17,21-二羟基-3,11,20 通过在离子条件下的溴化，例如，三氧杂-1,4-孕二烯-17-21-二酯 溴在乙酸中。

    Process for the preparation of 7.alpha.-halogeno-3-oxo-4-dehydro steroids and novel 7.alpha.-halogeno derivatives produced thereby
    2.
    发明授权
    Process for the preparation of 7.alpha.-halogeno-3-oxo-4-dehydro steroids and novel 7.alpha.-halogeno derivatives produced thereby 失效
    制备7 {60-卤代-3-氧代-4-脱氢类固醇和由此产生的新型7 {60-卤代衍生物的方法

    公开(公告)号：US4076708A

    公开(公告)日：1978-02-28

    申请号：US753257

    申请日：1976-12-22

    申请人： Michael J. Green ,  Ho-Jane Shue ,  Elliot L. Shapiro ,  Margaret A. Gentles

    发明人： Michael J. Green ,  Ho-Jane Shue ,  Elliot L. Shapiro ,  Margaret A. Gentles

    IPC分类号： C07J5/00 ,  C07J21/00 ,  C07J71/00

    CPC分类号： C07J21/003 ,  C07J21/00 ,  C07J5/0076 ,  C07J5/0084

    摘要： 3-Oxo-6-unsubstituted-7.alpha.-halogeno-4-dehydro steroids, wherein said halogen is chlorine, bromine or iodine, are prepared by reaction of a 3-oxo-6,7-di-unsubstituted-4,6-bis-dehydro steroid with at least an equimolar quantity of the corresponding hydrogen halide in a non-reactive organic solvent at temperatures no higher than about 30.degree. C, and then are isolated by removal of said solvent and any excess acid at temperatures no higher than about 25.degree. C without subjecting said 3-oxo-6-unsubstituted-7.alpha.-halogeno-4-dehydro steroid to a basic medium.A preferred species of this process is that wherein the starting steroid is a 3,20-dioxo-9-unsubstituted-11-oxygenated-1,4,6-pregnatriene-17,21-diol or ester thereof, preferably a 17,21-di-lower alkanoate or a 17-benzoate 21-lower alkanoate ester thereof, whereby is prepared in good yields a 3,20-dioxo-7.alpha.-halogeno-1,4-pregnadiene-17.alpha.,21-diol or ester thereof, useful as topical anti-inflammatory agents.Also described are novel 3,20-dioxo-7.alpha.-halogeno-4-pregnene-17.alpha.,21-diols and esters thereof having anti-inflammatory activity as well as 3-oxo-7.alpha.-halogeno-17.alpha.-4-pregnene-21,17.beta.-carbolactone aldosterone antagonists.

    摘要翻译： 3-氧代-6-未取代-7α-卤代-4-脱氢甾族化合物，其中所述卤素是氯，溴或碘，通过3-氧代-6,7-二 - 未取代的4,6- 在不高于约30℃的温度下，在非反应性有机溶剂中至少具有等摩尔量的相应卤化氢的双脱氢甾族化合物，然后通过除去所述溶剂和任何过量的酸在不高于 约25℃，而不将所述3-氧代-6-未取代的-7α-卤代-4-脱氢甾族化合物转化为碱性介质。

    -Azido-4,6-pregnadieno(3,2-c)pyrazoles, processes for their preparation and intermediates useful therein
    3.
    发明授权
    -Azido-4,6-pregnadieno(3,2-c)pyrazoles, processes for their preparation and intermediates useful therein 失效
    （3,2-c）吡唑，其制备方法和其中有用的中间体

    公开(公告)号：US3932388A

    公开(公告)日：1976-01-13

    申请号：US462687

    申请日：1974-04-22

    申请人： Thomas L. Popper ,  Richard W. Draper ,  Elliot L. Shapiro ,  Arthur S. Watnick

    发明人： Thomas L. Popper ,  Richard W. Draper ,  Elliot L. Shapiro ,  Arthur S. Watnick

    IPC分类号： C07J71/00 ,  C07J1/00

    CPC分类号： C07J71/0047 ,  Y10S514/899 ,  Y10S514/96 ,  Y10S514/962 ,  Y10S514/969

    摘要： Steroidal 6-azido-4,6-pregnadieno[3,2-c]pyrazoles having glucocorticoid activity are prepared by treating a 6-unsubstituted-4,6-pregnadieno[3,2-c]pyrazole with a halogen azide followed by treatment of the thereby formed 6-azido-7-halogeno-6,7-dihydro-4-pregnene[3,2-c]pyrazole with a dehydrohalogenating agent. Other methods of preparing these compounds are described, including the process of treating a 6-azido-17.alpha.,20; 20,21-bismethylenedioxy-4,6-pregnadiene-3-one with an alkyl formate in the presence of base followed by treatment of the resulting 2-hydroxymethylene derivative with a hydrazine or, alternatively, by converting said 2-hydroxymethylene to a 2-alkoxymethylene derivative followed by treatment thereof with a hydrazine.Preferred compounds include 6-azido-11.beta.,17.alpha.,21-trihydroxy-20-keto-4,6-pregnadieno[3,2-c]pyrazoles, particularly 2'-phenyl-9.alpha.-fluoro(and 9.alpha.-chloro)-16-methyl-derivatives thereof which possess potent anti-inflammatory activity. Of interest is 2'-phenyl-6-azido-9.alpha.-fluoro-11.beta.,17.alpha.,21-trihydroxy-16.alpha.-methyl-20-keto-4,6-pregnadieno[3,2-c]pyrazole.

    摘要翻译： 具有糖皮质激素活性的甾体6-叠氮基-4,6-孕雌二烯并[3,2-c]吡唑通过用卤素叠氮化物处理6-未取代的4,6孕烯二烯并[3,2-c]吡唑，然后进行处理 由此形成的6-叠氮基-7-卤代-6,7-二氢-4-孕烯[3,2-c]吡唑与脱卤化氢剂反应。 描述了制备这些化合物的其它方法，包括处理6-叠氮基-17α，20; 在碱的存在下，与甲酸烷基酯反应，然后用肼处理所得2-羟基亚甲基衍生物，或者通过将所述2-羟基亚甲基转化为2 - 烷氧基亚甲基衍生物，随后用肼处理。