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1.发明授权7α-hydroxy-pregn-4-en-3-one-20-carbaldehyde, process for producing the same, and process for producing 7α, 21-dihydroxy-20-methyl-pregn-4-en-3-one from the same 失效7α-羟基孕甾-4-烯-3-酮-20-甲醛，其制备方法，以及从其制备7α，21-二羟基-20-甲基孕烯-4-烯-3-酮的方法公开(公告)号：US07153988B2
公开(公告)日：2006-12-26
申请号：US10488808
申请日：2002-07-30
申请人： Masao Tsuji , Yoko Nakano , Shigeo Ohzono , Makoto Nakazawa
发明人： Masao Tsuji , Yoko Nakano , Shigeo Ohzono , Makoto Nakazawa
IPC分类号： C07J9/00
摘要： 7α-Hydroxy-pregn-4-en-3-one-20-carbaldehyde, a production method thereof and a method for producing 7α,21 -dihydroxy-20-methyl-pregn-4-en-3-one, which is useful as a synthetic intermediate for pharmaceuticals such as squalamine and the like, efficiently at high purity from the carbaldehyde.
摘要翻译： 7α-羟基孕甾-4-烯-3-酮-20-甲醛，其制备方法和制备7α，21-二羟基-20-甲基孕-4-烯-3-酮的方法是有用的 作为用于药物例如角鲨胺等的合成中间体，可以高效地从甲醛中纯化。
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公开(公告)号：US20070149494A1
公开(公告)日：2007-06-28
申请号：US10594164
申请日：2005-03-31
摘要： The present invention relates to a method of producing 5α-pregnane derivatives represented by the formula (II), which is characterized by reacting a pregnane derivative represented by the formula (I) with a metal selected from alkali metals and alkaline earth metals in the presence of a proton donor and an amine and/or ammonia. According to the present invention, a method capable of producing 5α-pregnane derivatives useful as synthetic intermediates for squalamine, in a high yield from easily available raw materials, can be provided: wherein R1 is a hydroxyl-protecting group, and R2, R11 and R12 are each independently a hydrogen atom or a hydroxyl-protecting group and R3 and R4 are each hydrogen atoms in combination form a bond.
摘要翻译： 本发明涉及一种生产由式（II）表示的5α-孕烷衍生物的方法，其特征在于使式（I）表示的孕烷衍生物与选自碱金属和碱土金属的金属在存在下反应 的质子供体和胺和/或氨。 根据本发明，可以提供一种能够从容易获得的原料以高产率制备可用作鲨烯胺的合成中间体的5α-孕烷衍生物的方法：其中R 1是羟基 - R 12，R 11和R 12各自独立地为氢原子或羟基保护基，R 1，R 2， 3和R 4各自是氢原子组合形成一个键。
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公开(公告)号：US06180835B2
公开(公告)日：2001-01-30
申请号：US09245305
申请日：1999-02-05
申请人： Goro Asanuma , Kazuya Takaki , Shigeo Ohzono , Manzo Shiono
发明人： Goro Asanuma , Kazuya Takaki , Shigeo Ohzono , Manzo Shiono
IPC分类号： C07C2710
CPC分类号： C07D307/20 , C07C1/20 , C07C33/05 , C07C2601/02 , Y02P20/55 , C07C13/04
摘要： A cyclopropylacetylene derivative of the formula (V): is prepared by reacting a propynol derivative of the formula (I): with a propane derivative of the formula (VI): in the presence of a base in an amount of 2 or more equivalents relative to the propynol derivative to give a cyclopropane derivative of the formula (III): deprotecting the protecting group for the hydroxyl group of the cyclopropane derivative to give a cyclopropylpropynol derivative of the formula (IV): and subjecting the cyclopropylpropynol derivative to retro-ethynylation. In the above formulas R1, R2, R3, R4 and R5 represent hydrogen; or an alkyl, alkenyl, aryl or aralkyl group, each of which may have a substituent, R6 and R7 is hydrogen; or an alkyl, alkenyl, aryl or aralkyl group, each of which may have a substituent, or R6 and R7 taken together form a ring, R8 is a protecting group for the hydroxyl group and X and Y are each a leaving group.
摘要翻译： 式（Ⅴ）的环丙基乙炔衍生物通过使式（I）的丙炔醇衍生物与式（Ⅵ）的丙烷衍生物在碱的存在下反应制备：碱的量为2或更多当量相对 与丙炔衍生物反应，得到式（III）的环丙烷衍生物：使环丙烷衍生物的羟基的保护基脱保护，得到式（IV）的环丙基丙炔醇衍生物：使环丙基丙炔衍生物进行逆乙炔化反应。 在上式中，R 1，R 2，R 3，R 4和R 5表示氢; 或者可以具有取代基的烷基，烯基，芳基或芳烷基，R6和R7是氢; 或烷基，链烯基，芳基或芳烷基，其各自可以具有取代基，或者R6和R7一起形成环，R8是羟基的保护基，X和Y各自是离去基团。
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公开(公告)号：US20070197490A1
公开(公告)日：2007-08-23
申请号：US10594163
申请日：2005-03-31
摘要： The present invention relates to a method of producing a mixture of 5α-pregnane derivatives represented by the formula (II) and the formula (III), which is characterized by reacting a pregnane derivative represented by the formula (I) with a metal selected from alkali metals and alkaline earth metals in the presence of a proton donor and an amine and/or ammonia. According to the present invention, a method capable of producing 5α-pregnane derivatives useful as synthetic intermediates for squalamine, in a high yield from easily available raw materials, can be provided: wherein R1 is a hydroxyl-protecting group, and R2, R11 and R12 are each independently a hydrogen atom or a hydroxyl-protecting group.
摘要翻译： 本发明涉及一种制备由式（II）和式（III）表示的5α-仲戊基衍生物的混合物的方法，其特征在于使由式 （I）与选自碱金属和碱土金属的金属在质子供体和胺和/或氨的存在下反应。 根据本发明，可以提供一种能够从容易获得的原料以高产率生产可用作角鲨烷的合成中间体的5α-仲戊烷衍生物的方法：其中R 1 羟基保护基，R 2，R 11和R 12各自独立地为氢原子或羟基 保护组。
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