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10 条记录 (耗时 0.019 秒)

    25-Hydroxy-24-oxocholestane derivatives and preparation thereof
    1.
    发明授权
    25-Hydroxy-24-oxocholestane derivatives and preparation thereof 失效
    25-羟基-24-氧代胆乙醇衍生物及其制备

    公开(公告)号：US4292249A

    公开(公告)日：1981-09-29

    申请号：US121857

    申请日：1980-02-15

    申请人： Osamu Nishikawa ,  Kenji Ishimaru ,  Toru Takeshita ,  Hideki Tsuruta

    发明人： Osamu Nishikawa ,  Kenji Ishimaru ,  Toru Takeshita ,  Hideki Tsuruta

    IPC分类号： C07J9/00 ,  C07J17/00

    CPC分类号： C07J17/00 ,  C07J9/00

    摘要： This invention relates to novel 25-hydroxy-24-oxocholestane derivatives and a process for preparing them.The novel 25-hydroxy-24-oxocholestane derivatives of this invention can easily be converted to 24,25-dihydroxycholecalciferol or 1.alpha.,24,25-trihydroxycholecalciferol which is known as useful for medicine controlling the calcium metabolism of warm-blooded animals. Moreover, 25-hydroxy-24-oxocholestane derivatives can be converted to novel 25-hydroxy-24-oxocholecalciferol expressed by the following formula ##STR1## and novel 1.alpha.,25-dihydroxy-24-oxocholecalciferol of the formula ##STR2## which are useful for medicine. The new 25-hydroxy-24-oxocholestane derivatives in the present invention are very useful as the intermediates for the synthesis of a variety of active vitamin D.sub.3.

    摘要翻译： 本发明涉及新的25-羟基-24-氧代胆乙醇衍生物及其制备方法。 本发明的新型25-羟基-24-氧代胆乙醇衍生物可以容易地转化为24,25-二羟基胆钙化甾醇或1α，24,25-三羟基胆钙化甾醇，其已知可用于控制温血动物钙代谢的药物。 此外，可以将25-羟基-24-氧代胆乙醇衍生物转化为由下式表示的新型25-羟基-24-氧代胆钙化甾醇和式（IMAGE）的新型1α，25-二羟基-24-氧代胆钙化甾醇，其为 有用的药物。 本发明中的新的25-羟基-24-氧代胆乙醇衍生物作为合成各种活性维生素D3的中间体是非常有用的。

    Process for the preparation of active-type vitamin D.sub.3 compounds
    3.
    发明授权
    Process for the preparation of active-type vitamin D.sub.3 compounds 失效
    活性型维生素D3化合物的制备方法

    公开(公告)号：US4388243A

    公开(公告)日：1983-06-14

    申请号：US371870

    申请日：1982-04-26

    申请人： Osamu Nishikawa ,  Kenji Ishimaru ,  Toru Takeshita ,  Hideki Tsuruta

    发明人： Osamu Nishikawa ,  Kenji Ishimaru ,  Toru Takeshita ,  Hideki Tsuruta

    IPC分类号： C07J9/00

    CPC分类号： C07J9/00 ,  Y02P20/55 ,  Y02P20/582

    摘要： The present invention relates to a novel process for the preparation of active-type vitamin D.sub.3 compounds and their intermediates. In accordance with the present invention, a large amount of an active-type vitamin D.sub.3 compounds, for example 1.alpha.-hydroxycholecalciferol, 1.alpha.,25-dihydroxycholecalciferol and the like, is efficiently prepared with high industrial advantages by a novel processes, which comprises (i) reacting hydroxycholesta-5-enes having the hydroxyl groups protected with lower alkoxycarbonyl group as a starting material with allylic brominating agent and dehydrobrominating agent to prepare the corresponding hydroxycholesta-5,7-dienes, (ii) exposing the hydroxycholesta-5,7-dienes to ultraviolet irradiation or to a combination of the irradiation with thermal isomerization to obtain a mixture of the unreacted hydroxycholesta-5,7-dienes and previtamin D.sub.3 compounds or a mixture of the unreacted hydroxycholesta-5,7-dienes and the protected active-type vitamin D.sub.3 compounds, (iii) separating the mixture into the unreacted hydroxycholesta-5,7-dienes and previtamin D.sub.3 compounds or the protected active-type vitamin D.sub.3 compounds, (iv) recycling the unreacted hydroxycholesta-5,7-dienes as reuse and (v) thermally isomerizing the remaining compounds and/or splitting off the protective groups. The process for the preparation of active-type vitamin D.sub.3 compounds, in the present invention, is of very high industrial value, capable of carrying out by simple operation and adaptable to large scale commercial production.

    摘要翻译： 本发明涉及一种制备活性型维生素D3化合物及其中间体的新方法。 根据本发明，通过新工艺有效地制备了大量活性型维生素D3化合物，例如1α-羟基胆钙化甾醇，1α，25-二羟基胆钙化甾醇等，具有高工业优势，其包括 （i）使具有被低级烷氧基羰基保护的羟基作为起始原料的羟基胆甾-5-烯与烯丙基溴化剂和脱溴溴化剂反应以制备相应的羟基胆甾-5,7-二烯，（ii）将羟基胆甾-5， 7-二烯对紫外线照射或通过热异构化的照射的组合，得到未反应的羟基胆甾-5,7-二烯和维生素D3化合物的混合物或未反应的羟基胆甾-5,7-二烯与受保护的 活性型维生素D3化合物，（iii）将混合物分离成未反应的羟基胆甾-5,7-二烯和维生素D3化合物或受保护的活性 （iv）将未反应的羟基胆甾-5,7-二烯再循环使用，和（v）使其余化合物热异构化和/或分离保护基团。 在本发明中制备活性型维生素D3化合物的方法具有非常高的工业价值，能够通过简单的操作进行并适应于大规模的商业生产。

    Process for producing steroid compounds having an oxo group in the side chain
    4.
    发明授权
    Process for producing steroid compounds having an oxo group in the side chain 失效
    在侧链中具有氧代基的类固醇化合物的制备方法

    公开(公告)号：US4298537A

    公开(公告)日：1981-11-03

    申请号：US97980

    申请日：1979-11-28

    申请人： Osamu Nishikawa ,  Kenji Ishimaru ,  Toru Takeshita ,  Hideki Tsuruta

    发明人： Osamu Nishikawa ,  Kenji Ishimaru ,  Toru Takeshita ,  Hideki Tsuruta

    IPC分类号： C07J9/00 ,  C07J53/00

    CPC分类号： C07J9/005 ,  C07J9/00 ,  Y02P20/55

    摘要： A process for producing a steroid compound having an oxo group in the side chain, which comprises condensing an acid halide having a steroid skeleton with an organozinc compound at the halocarbonyl group of the acid halide in an inert organic medium in the presence of a catalytic amount of an ether capable of forming a complex with the organozinc compound, and if desired, hydrolyzing the product. The process produces the steroid compound at a high yield, and often at an almost quantitative yield. The steroid compound is an important intermediate for the production of vitamin D.sub.3 analogs such as active forms of vitamin D.sub.3. In one preferred embodiment, an industrially advantageous process from the standpoint of operation is provided.

    摘要翻译： 一种制备侧链中具有氧代基的类固醇化合物的方法，该方法包括在惰性有机介质中，在催化量存在下将具有类固醇骨架的酰卤与有机锌化合物在酰卤的卤代羰基 的能够与有机锌化合物形成络合物的醚，如果需要，水解产物。 该方法以高产率产生类固醇化合物，并且通常以几乎定量的产率。 类固醇化合物是生产维生素D3类似物（如活性形式的维生素D3）的重要中间体。 在一个优选实施例中，提供了从工作角度出发的工业上有利的工艺。

    3-Methylene cephalosporanic acid derivatives and process for preparation thereof
    8.
    发明授权
    3-Methylene cephalosporanic acid derivatives and process for preparation thereof 失效
    3-亚甲基头孢菌酸衍生物及其制备方法

    公开(公告)号：US4138553A

    公开(公告)日：1979-02-06

    申请号：US841321

    申请日：1977-10-11

    申请人： Sachio Ishimoto ,  Hisao Yamaguchi ,  Yoshinori Kato ,  Takeo Oba ,  Kenji Ozawa ,  Yataro Ichikawa ,  Koji Nakagawa ,  Hideki Tsuruta

    发明人： Sachio Ishimoto ,  Hisao Yamaguchi ,  Yoshinori Kato ,  Takeo Oba ,  Kenji Ozawa ,  Yataro Ichikawa ,  Koji Nakagawa ,  Hideki Tsuruta

    IPC分类号： C07D499/00 ,  C07D501/10 ,  C07D501/02

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： Novel substituted hydrazide derivatives of 7-(substituted)amino-3-methylene-cepham-4-carboxylic acids expressed by the formula ##STR1## wherein R.sub.1 represents alkyl containing at least 3 carbon atoms, cycloalkyl, or optionally substituted aryl, and one of R.sub.2 and R.sub.3 represents hydrogen with the other being hydrogen or the same as R.sub.1 ; or R.sub.1 and R.sub.2 form a heterocyclic ring optionally through a hetero atom together with the attached nitrogen and R.sub.3 represents hydrogen atom; and Z.sub.1 represents amino or protected amino; and acid addition salts thereof, which are useful as intermediates for synthesizing cephalosporin antibiotics. These compounds can be prepared in high yields from the corresponding substituted hydrazide derivatives of 6-substituted amino-1-oxide-2, 2-dimethyl-penam-3-carboxylic acids, which are readily available at low costs, by heating them in the presence of a thermal rearrangement promotor such as organic sulfonic acids and optionally in the further presence of a tertiary nitrogen-containing cyclic compound, followed if desired by splitting off the amino-protecting group and converting the product to acid addition salts.

    摘要翻译： 由式“IMAGE”表示的7-（取代的）氨基-3-亚甲基 - 头孢烯-4-羧酸的新型取代的酰肼衍生物，其中R 1表示含有至少3个碳原子的烷基，环烷基或任选取代的芳基， R2和R3代表氢，另一个是氢或与R1相同; 或R 1和R 2与所连接的氮一起任选地通过杂原子形成杂环，并且R 3表示氢原子; Z1表示氨基或被保护的氨基; 其酸加成盐，其可用作合成头孢菌素抗生素的中间体。 这些化合物可以以相当于6-取代的氨基-1-氧化物-2,2-二甲基 - 对甲苯磺酸的取代的酰肼衍生物的高收率制备，它们以低成本容易获得，通过在 存在热重排促进剂如有机磺酸，并且任选地在另外存在叔氮气环状化合物的情况下，如果需要的话，分解氨基保护基并将产物转化成酸加成盐。