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    D-homo-20-ketopregnanes and method for inducing anesthesia or narcosis
    1.
    发明授权
    D-homo-20-ketopregnanes and method for inducing anesthesia or narcosis 失效
    D-均聚-20-酮戊二酸和诱导麻醉或麻醉的方法

    公开(公告)号：US4056633A

    公开(公告)日：1977-11-01

    申请号：US641602

    申请日：1975-12-17

    申请人： Ulrich Kerb ,  Rudolf Wiechert ,  Helmut Wachtel ,  Otto Engelfried ,  Klaus Kieslich

    发明人： Ulrich Kerb ,  Rudolf Wiechert ,  Helmut Wachtel ,  Otto Engelfried ,  Klaus Kieslich

    IPC分类号： A61K31/12 ,  A61K31/56 ,  C07J63/00 ,  C07J71/00 ,  C01B33/24

    CPC分类号： C07J71/001 ,  C07J63/008

    摘要： D-homo-20-ketopregnanes of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, alkyl, alkoxy, or azido;R.sub.2 is oxygen, ##STR2## and R.sub.7 is hydrogen, lower alkyl, or acyl of up to 5 carbon atoms; R.sub.3 is hydrogen or methylR.sub.4 is oxygen, two hydrogens, ##STR3## R.sub.5 is hydrogen, hydroxy, alkoxy, azido, mercapto, thiocyano, cyano, dialkylamino, morpholino, thiomorpholino, or piperazino;R.sub.6 is methyl or ethyl;The hydrogen atom in the 5-position is of the .alpha.- or .beta.-configuration;And acid addition salts thereof, possess narcotic-anesthetic activity.

    摘要翻译： 其中R 1是氢，氟，氯，溴，烷基，烷氧基或叠氮基的D-均聚-20-酮戊酸; R2是氧，R7是氢，低级烷基或至多5个碳原子的酰基; R3是氢或甲基R4是氧，两个氢，R5是氢，羟基，烷氧基，叠氮基，巯基，硫氰基，氰基，二烷基氨基，吗啉代，硫代吗啉代或哌嗪基; R6是甲基或乙基; 5位氢原子是α - 或β - 配位体; 和酸添加剂，它的最佳的NARCOTIC-ANESTHETIC活动。

    .DELTA..sup.9(11) -5.alpha.-20-KETO STEROIDS AND PROCESS FOR THEIR PRODUCTION
    4.
    发明授权
    .DELTA..sup.9(11) -5.alpha.-20-KETO STEROIDS AND PROCESS FOR THEIR PRODUCTION 失效
    {66 {HU 9（11）{B -5 {60 -20-KETO STEROIDS AND PROCESS FOR PRODUCRECTION

    公开(公告)号：US4061661A

    公开(公告)日：1977-12-06

    申请号：US693848

    申请日：1976-06-08

    申请人： Rudolf Wiechert ,  Ulrich Kerb ,  Otto Engelfried

    发明人： Rudolf Wiechert ,  Ulrich Kerb ,  Otto Engelfried

    IPC分类号： C07J7/00 ,  C07J1/00

    CPC分类号： C07J7/002

    摘要： 3.alpha.-Hydroxy and 3.alpha.-acyloxy- .DELTA..sup.9(11) -5.alpha.-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-iodobenzoic 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-α-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，由 酯化相应的具有式（IMAGE）的3β-羟基-5α-20-酮孕烷，其中R1和R2具有上述给出的值，将间苯二甲酸与3β-氧基转化为3α- 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。

    D-Homopregnanes
    8.
    发明授权
    D-Homopregnanes 失效

    公开(公告)号：US4202841A

    公开(公告)日：1980-05-13

    申请号：US973336

    申请日：1978-12-26

    申请人： Leo Alig ,  Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Klaus Kieslich ,  Rudolf Wiechert

    发明人： Leo Alig ,  Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Klaus Kieslich ,  Rudolf Wiechert

    IPC分类号： C07J63/00 ,  C12P33/02 ,  C12P33/08 ,  C07C49/00

    CPC分类号： C07J63/008 ,  C12P33/02 ,  C12P33/08

    摘要： D-Homopregnanes of the formula ##STR1## wherein the dotted line in the 1,2-position together with the corresponding solid line denotes a single or double carbon-carbon bond; R.sup.6 is hydrogen, fluoro, chloro or methyl; R.sup.9 is hydrogen, fluoro, chloro or bromo; R.sup.11 is hydroxyl, acyloxy, fluoro or chloro; and R.sup.17a is hydroxyl or acyloxy with the proviso that when R.sup.9 is fluoro, chloro or bromo and R.sup.11 is fluoro or chloro, the atomic number of R.sup.11 is less than or equal to that of R.sup.9 ; and with the further proviso that when R.sup.6 is hydrogen, and R.sup.11 and R.sup.17a are hydroxy or when R.sup.6 is fluoro, R.sup.11 and R.sup.17a are hydroxyl and the dotted line in the 1,2-position together with the corresponding solid line denotes a single carbon-carbon bond, R.sup.9 is fluoro, chloro or bromo and processes for the preparation thereof are disclosed.

    摘要翻译： 式Ⅰ的D-homopregnanes其中1,2位虚线连同相应实线表示单碳双键; R6是氢，氟，氯或甲基; R9是氢，氟，氯或溴; R11是羟基，酰氧基，氟或氯; 并且R 17a是羟基或酰氧基，条件是当R 9是氟时，氯或溴，R 11是氟或氯，R 11的原子数小于或等于R 9的原子数; 并且进一步的条件是当R6为氢时，R11和R17a为羟基或当R6为氟时，R11和R17a为羟基，1,2-位与虚线相应的实线表示单个碳 - 碳键，R9是氟，氯或溴，并且其制备方法被公开。

    .DELTA..sup.9 (11) -5.alpha.-D-homo-20-keto steroids
    9.
    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。