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![Processes for preparation of cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives](/abs-image/US/2004/08/31/US06784172B2/abs.jpg.150x150.jpg)
1.发明授权Processes for preparation of cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives 失效制备环戊二烯并[b] [1,4]二氮杂[6,7,1-hi]吲哚及其衍生物的方法公开(公告)号：US06784172B2
公开(公告)日：2004-08-31
申请号：US10016420
申请日：2001-11-02
申请人： Annmarie Louise Sabb , Robert Lewis Vogel , Madelene Miyoko Antane , Panolil Raveendranath , Sreenivasulu Megati , Michael David Smith , James Albert Nelson
发明人： Annmarie Louise Sabb , Robert Lewis Vogel , Madelene Miyoko Antane , Panolil Raveendranath , Sreenivasulu Megati , Michael David Smith , James Albert Nelson
IPC分类号： A61K3155
CPC分类号： C07D487/06
摘要： This invention provides processes for synthesizing compounds of formula I: wherein R is H or alkyl; R1, R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, alkyl sulfonamide, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or aroyl; R3 and R4 are H, alkyl or cycloalkyl; the dashed line indicates an optional double bond; as well as intermediates and pharmaceutically acceptable salts thereof.
摘要翻译： 本发明提供了合成式I化合物的方法：其中R是H或烷基; R1，R2是H，烷基，烷氧基，卤素，氟化烷基，-CN，烷基磺酰胺，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基或芳酰基。 R3和R4是H，烷基或环烷基; 虚线表示可选的双键; 以及其中间体和药学上可接受的盐。
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公开(公告)号：US07342119B2
公开(公告)日：2008-03-11
申请号：US10948004
申请日：2004-09-23
IPC分类号： C07D43/02
CPC分类号： C07D209/48 , C07D209/18
摘要： A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then, heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.
摘要翻译： 一种制备取代的吲哚化合物的方法，包括以下步骤：使化合物在非质子极性溶剂中在催化剂存在下反应形成中间体化合物，其中Ph和X如本文所定义; 然后在催化剂存在下，在溶剂中加热该中间体化合物，形成取代的吲哚化合物。本发明还包括通过该方法形成的化合物。
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公开(公告)号：US20050070723A1
公开(公告)日：2005-03-31
申请号：US10948004
申请日：2004-09-23
IPC分类号： C07D209/18 , C07D209/48 , C07D43/02
CPC分类号： C07D209/48 , C07D209/18
摘要： A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then, heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.
摘要翻译： 一种制备取代的吲哚化合物的方法，包括以下步骤：使化合物在非质子极性溶剂中在催化剂存在下反应形成中间体化合物，其中Ph和X如本文所定义; 然后在催化剂存在下，在溶剂中加热该中间体化合物，形成取代的吲哚化合物。本发明还包括通过该方法形成的化合物。
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5.发明申请Processes for the preparation of 16beta-alkoxy, 17alpha-hydroxy steroids and steroidal 16beta, 17alpha-diols from 16alpha, 17alpha-epoxy steroids 审中-公开用于制备16α-烷氧基，17α-羟基类固醇和16α，17α-环氧类固醇的甾体16beta，17α-二醇的方法公开(公告)号：US20060014973A1
公开(公告)日：2006-01-19
申请号：US11182557
申请日：2005-07-15
IPC分类号： C07J1/00
CPC分类号： C07J1/00
摘要： The present invention provides processes for the preparation of 16β-alkoxy, 17α-hydroxy steroids via the reaction of a 16α,17α-epoxy steroid with an appropriate alcohol in the presence of base. The present invention also provides processes for the preparation of 16β-alkoxy, 17α-hydroxy steroids.
摘要翻译： 本发明提供了通过在碱存在下通过16α，17α-环氧类固醇与适当的醇反应制备16b-烷氧基，17α-羟基类固醇的方法。 本发明还提供了制备16beta-烷氧基，17α-羟基类固醇的方法。
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公开(公告)号：US20050049296A1
公开(公告)日：2005-03-03
申请号：US10930534
申请日：2004-08-31
申请人： Christoph Dehnhardt , Sreenivasulu Megati , Ronald Michalak , Panolil Raveendranath , Jianxin Ren , Charles Wu , Yangzhong Wu
发明人： Christoph Dehnhardt , Sreenivasulu Megati , Ronald Michalak , Panolil Raveendranath , Jianxin Ren , Charles Wu , Yangzhong Wu
IPC分类号： C07D209/14 , A61K31/405
CPC分类号： C07D209/14
摘要： A process for making the compound of formula (I) wherein Ac represents acetate; X represents O or CH2; Y represents C1-C6alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF3, OCF3, OH, C1-C6alkyl, C1-C6alkoxy, C1-C6thioalkyl, NH2, N(C1-C6alkyl)2, NH(C1-C6alkyl), NC(O)-(C1-C6alkyl), and NO2. In his process, a compound of formula (II) is reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).
摘要翻译： 制备式（I）的化合物的方法，其中Ac表示乙酸酯; X表示O或CH2; Y表示C1-C6烷基; 和Z选自H，卤素，CN，CHO，CF 3，OCF 3，OH，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，NH 2，N（C 1 -C 6烷基）2，NH（C 1 -C 6烷基 ），NC（O） - （C1-C6烷基）和NO2。 在其工艺中，将式（II）化合物与肼反应以形成伯烷基胺，然后将伯烷基胺与乙酸酐反应，生成式（I）化合物。
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公开(公告)号：US07582771B2
公开(公告)日：2009-09-01
申请号：US10930534
申请日：2004-08-31
申请人： Christoph M. Dehnhardt , Sreenivasulu Megati , Ronald S. Michalak , Panolil Raveendranath , Jianxin Ren , Charles C. Wu , Yangzhong Wu
发明人： Christoph M. Dehnhardt , Sreenivasulu Megati , Ronald S. Michalak , Panolil Raveendranath , Jianxin Ren , Charles C. Wu , Yangzhong Wu
IPC分类号： C07D209/10 , C07D209/14
CPC分类号： C07D209/14
摘要： A process for making the compound of formula (I) wherein Ac represents acetate; X represents O or CH2; Y represents C1-C6alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF3, OCF3, OH, C1-C6alkyl, C1-C6alkoxy, C1-C6thioalkyl, NH2, N(C1-C6alkyl)2, NH(C1-C6alkyl), NC(O)—(C1C6alkyl), and NO2. In his process, a compound of formula (II) is reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).
摘要翻译： 制备式（I）的化合物的方法，其中Ac表示乙酸酯; X表示O或CH2; Y表示C1-C6烷基; 和Z选自H，卤素，CN，CHO，CF 3，OCF 3，OH，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，NH 2，N（C 1 -C 6烷基）2，NH（C 1 -C 6烷基 ），NC（O） - （C 1 -C 6烷基）和NO 2。 在其工艺中，将式（II）化合物与肼反应以形成伯烷基胺，然后将伯烷基胺与乙酸酐反应，生成式（I）化合物。
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公开(公告)号：US20080177085A1
公开(公告)日：2008-07-24
申请号：US12041988
申请日：2008-03-04
IPC分类号： C07D209/20
CPC分类号： C07D209/48 , C07D209/18
摘要： A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then, heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.
摘要翻译： 一种制备取代的吲哚化合物的方法，包括以下步骤：使化合物在非质子极性溶剂中在催化剂存在下反应形成中间体化合物，其中Ph和X如本文所定义; 然后在催化剂存在下，在溶剂中加热该中间体化合物，形成取代的吲哚化合物。本发明还包括通过该方法形成的化合物。
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公开(公告)号：US20050288268A1
公开(公告)日：2005-12-29
申请号：US11209066
申请日：2005-08-22
CPC分类号： C07J1/00
摘要： This invention relates to a process for the preparation of 6-hydroxyequilenins, which are useful as estrogenic agents.
摘要翻译： 本发明涉及一种制备可用作雌激素剂的6-羟基平滑蛋白的方法。
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