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145 条记录 (耗时 0.02 秒)

    5.beta.-Hydroxy-.DELTA..sup.6 -steroids and process for the preparation thereof
    71.
    发明授权
    5.beta.-Hydroxy-.DELTA..sup.6 -steroids and process for the preparation thereof 失效
    5β-羟基-DTATA 6-类固醇及其制备方法

    公开(公告)号：US4472310A

    公开(公告)日：1984-09-18

    申请号：US359713

    申请日：1982-03-11

    申请人： Dieter Bittler ,  Henry Laurent ,  Klaus Nickisch ,  Robert Nickolson ,  Rudolf Wiechert

    发明人： Dieter Bittler ,  Henry Laurent ,  Klaus Nickisch ,  Robert Nickolson ,  Rudolf Wiechert

    IPC分类号： C07J1/00 ,  C07J21/00 ,  C07J53/00 ,  C07J71/00

    CPC分类号： C07J21/003 ,  C07J1/0025 ,  C07J53/008 ,  C07J71/001

    摘要： The disclosure concerns 5.beta.-hydroxy-.DELTA..sup.6 -steroids of the general formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower alkyl, or the tetrahydropyranyl residue andR.sup.2, R.sup.3 individually are respectively hydrogen or jointly are methylene andX stands for oxygen, the groupings ##STR2## (wherein R.sup.4 means hydrogen or acyl) and ##STR3## (wherein R.sup.5 means hydrogen or lower alkyl) and a process for the preparation thereof by reacting corresponding 7.alpha.-chloro-5.beta.,6.beta.-epoxy steroids in an inert solvent with metallic zinc in a lower aliphatic carboxylic acid or dilute mineral acid at temperatures of between room temperature and 100.degree. C., preferably at 40.degree.-70.degree. C.The compounds producible by this method are intermediates for the preparation of 3-keto-.DELTA..sup.4 -6.beta.,7.beta.-methylene steroids constituting pharmacologically valuable compounds, for example aldosterone antagonists.

    摘要翻译： PCT No.PCT / DE81 / 00111 Sec。 371日期1982年3月11日 102（e）1982年3月11日PCT PCT。 公开号WO82 / 00294 日本1982年2月4日。该公开内容涉及通式为“IMAGE”的5ββ-羟基-DTATA-类固醇，其中R 1为氢，酰基，低级烷基或四氢吡喃基，R2，R3分别为氢或共同 （其中R 4表示氢或酰基）和（其中R 5表示氢或低级烷基）及其制备方法，通过使相应的7α- 氯代-5β，6β-环氧类固醇在惰性溶剂中与金​​属锌在低级脂族羧酸或稀无机酸中在室温至100℃之间，优选40℃-70℃的温度下进行。化合物 通过该方法可生产的是制备构成药理学上有价值的化合物的3-酮-TATA4-6β，7β-亚甲基甾族化合物的中间体，例如醛固酮拮抗剂。

    Process for the preparation of 17.alpha.-(3-iodobenzoyloxy)-9.alpha.-chloro-4-pregnene-3,20-diones and their D-homo homologs
    75.
    发明授权
    Process for the preparation of 17.alpha.-(3-iodobenzoyloxy)-9.alpha.-chloro-4-pregnene-3,20-diones and their D-homo homologs 失效
    17α-（3-碘苯甲酰氧基）-9α-氯-4-孕烯-3,20-二酮及其D-同系物的制备方法

    公开(公告)号：US4260464A

    公开(公告)日：1981-04-07

    申请号：US953323

    申请日：1978-10-20

    申请人： Ulrich Kerb ,  Manfred Stahnke ,  Rudolf Wiechert

    发明人： Ulrich Kerb ,  Manfred Stahnke ,  Rudolf Wiechert

    IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J63/00 ,  B01J19/08

    CPC分类号： C07J5/0076 ,  C07J5/0053 ,  C07J63/00 ,  C07J7/0045 ,  Y10S204/90 ,  Y10S204/914

    摘要： Novel 17.alpha.-(3-iodobenzoyloxy)-9.alpha.-chloro-4-pregnene-3,20-diones and the D-homo homologs thereof, of the formula ##STR1## wherein n is 1 or 2;C.sub.1 -----C.sub.2 represents a C--C single or C.dbd.C double bond;R.sub.1 is hydrogen, hydroxy, or lower acyloxy;R.sub.2 is hydrogen or methyl;R.sub.3 is hydrogen, methyl or fluorine; andwhen n is 1, C.sub.15 -----C.sub.16 represents a C--C single or C.dbd.C double bond; and when n is 2, C.sub.16 -----C.sub.17 represents a C--C single or C.dbd.C double bond;which have valuable pharmacological properties and also serve as intermediates in the preparation of known pharmacologically active compounds, can be prepared by irradiating a 17.alpha.-(3-iodobenzoyloxy)-4-pregnene-3,20-dione or a D-homo homolog thereof of the formula ##STR2## with long wavelength ultraviolet radiation in the presence of phenyliodine dichloride.

    摘要翻译： 新型17α-（3-碘苯甲酰氧基）-9α-氯-4-孕烯-3,20-二酮及其同型同系物，其中n为1或2; C1 ----- C2表示C-C单或C = C双键; R1是氢，羟基或低级酰氧基; R2是氢或甲基; R3是氢，甲基或氟; 当n为1时，C15 ----- C16表示C-C单或C = C双键; 当n为2时，C16 ---- -C17表示C-C单或C = C双键; 其具有有价值的药理学性质并且还可用作制备已知的药理学活性化合物的中间体，可以通过照射17α-（3-碘苯甲酰氧基）-4-孕烯-3,20-二酮或其D-同源同系物 在具有二碘化苯二碘的存在下，具有长波长紫外线辐射的式“IMAGE”。

    .DELTA..sup.9 (11) -5.alpha.-D-homo-20-keto steroids
    78.
    发明授权
    .DELTA..sup.9 (11) -5.alpha.-D-homo-20-keto steroids 失效
    {66 {HU 9（11）{B -5 {60-D-homo-20-keto类固醇

    公开(公告)号：US4097678A

    公开(公告)日：1978-06-27

    申请号：US693847

    申请日：1976-06-08

    申请人： Ulrich Kerb ,  Rudolf Wiechert ,  Otto Engelfried

    发明人： Ulrich Kerb ,  Rudolf Wiechert ,  Otto Engelfried

    IPC分类号： C07J63/00

    CPC分类号： C07J63/008

    摘要： 3.alpha.-Hydroxy and 3.alpha.-acyloxy- .DELTA..sup.9(11) -5.alpha.-D-homo-20-ketopregnenes of the formula ##STR1## wherein R is hydrogen or acyl, R.sub.1 is hydrogen or methyl and R.sub.2 is methyl or ethyl, are produced by esterifying a corresponding 3.beta.-hydroxy-5.alpha.-20-keto pregnane of the formula ##STR2## wherein R.sub.1 and R.sub.2 have the values given above, with m-iodo-benzoic acid with inversion of the 3.beta.-oxy group to a 3.alpha.-oxy group; chlorinating the thus-produced 3.alpha.-m-iodobenzoyl ester with dichloroiodobenzene under irradiation; and treating the reaction product with a dehydrohalogenating silver salt. Optionally thereafter, the 3.alpha.-iodobenzoyl group is split off in a conventional manner to produce the corresponding 3.alpha.-hydroxy steroid and optionally the thus-produced 3.alpha.-hydroxy steroid is esterified to produce a desired 3-ester thereof.

    摘要翻译： 3α-羟基和3α-酰氧基-TATA 9（11）-5α-D-高-20-酮戊二酸，其中R是氢或酰基，R 1是氢或甲基，R 2是甲基或乙基 通过酯化相应的具有上述给出的值的式“IMAGE”的相应的3β-羟基-5α-20-酮孕烷与通过3β-氧代反相的间 - 碘 - 苯甲酸 组成3个α氧基; 在照射下用二碘碘苯氯化如此制备的3α-碘代苯甲酰基酯; 并用脱卤化氢的银盐处理反应产物。 此后任选地，以常规方式将3α-碘代苯甲酰基分离出来以产生相应的3α-羟基类固醇，任选地，由此产生的3α-羟基类固醇被酯化以产生所需的3-酯。

    Process for the preparation of estrene-3,17-dione derivatives
    80.
    发明授权
    Process for the preparation of estrene-3,17-dione derivatives 失效
    雌激素-3,17-二酮衍生物的制备方法

    公开(公告)号：US4036695A

    公开(公告)日：1977-07-19

    申请号：US633415

    申请日：1975-11-19

    申请人： Karl Petzoldt ,  Rudolf Wiechert

    发明人： Karl Petzoldt ,  Rudolf Wiechert

    IPC分类号： C12P33/12 ,  C07J1/00 ,  C07J21/00 ,  C07J31/00 ,  C07J53/00 ,  C12R1/80 ,  C07B29/02

    CPC分类号： C07J31/006 ,  C07J1/0059 ,  C07J21/006 ,  C07J53/008 ,  Y10S435/929 ,  Y10S435/933 ,  Y10S435/935

    摘要： Estrene-3,17-diones of the formula ##STR1## wherein X is oxo, or ketalized oxo, preferably alkylenedioxy of 2-6 carbon atoms or o-phenylenedioxy;.DELTA. is a carbon atom linked to the adjacent carbon atoms by a double bond and two single bonds;R.sub.1 is methyl or ethyl, andR.sub.2 and R.sub.3 collectively are a carbon-to-carbon bond or methylene, useful as intermediates for the production of pharmacologically active steroids, are prepared by fermenting 18-ethyl-4-estrene-3,17-dione or 18-methyl-4-estrene-3,17-dione with a fungal culture of the genus Penicillium or Fusarium to produce the corresponding 15.alpha.-hydroxy-steroid;In either order, converting the hydroxy group of the thus-produced 15.alpha.-hydroxy steroid to a sulfonic acid ester thereof and ketalizing the 3-keto group thereof; andTreating the ketalized and esterified steroid with a base to form a .DELTA..sup.15 -compound or with dimethylsulfoxonium methylide to form a 15.beta.,16.beta.-methylene compound and, optionally, hydrolyzing the 3-ketal group.

    摘要翻译： 其中X是氧代或缩酮化的氧代，优选2-6个碳原子的亚烷基二氧基或邻苯二氧基的式（III）的雌二烯-3,17-二酮; DELTA是通过双重债券和两个单一债券连接到相邻碳粉的碳钢; R1是甲基或乙基，R2和R3统称为碳 - 碳键或亚甲基，可用作制备药理活性类固醇的中间体，是通过发酵18-乙基-4-雌酮-3,17-二酮 或18-甲基-4-雌二烯-3,17-二酮与青霉属或镰刀菌属的真菌培养物反应以产生相应的15α-羟基类固醇; 无论如何，将THUS生产的15α-羟基甾体的羟基转化为硫酸酯，并将其3-酮醇酯组进行KETAL化; 并用碱处理酮化和纯化的甾体以形成DELTA 15化合物或用二甲基甲硅烷基甲酸酯形成15β，16β-乙烯基化合物，并且有选择地水解3-KETAL基团。