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1.发明授权14.alpha.-hydroxy-4-androstene-3,6,17-trione hydrate and process for producing same 失效14α-羟基-4-雄甾烯-3,6,17-三酮水合物及其制备方法
公开(公告)号：US5648507A
公开(公告)日：1997-07-15
申请号：US453875
申请日：1995-05-30
IPC分类号： A61K31/565 , C07J1/00 , C07J75/00
CPC分类号： C07J1/0011
摘要： Provided are stable hydrate crystals of 14.alpha.-hydroxy-4-androstene-3,6,17-trione having a biological activity of human placenta-originating estrodiene synthesis enzyme inhibitory action. These hydrate crystals include two kinds of 14.alpha.-hydroxy-4-androstene-3,6,17-trione hydrate crystals having a diffraction pattern having characteristic peaks at diffraction angles in crystalline powder X-ray diffraction. Processes for producing these hydrate crystals are also provided.
摘要翻译： 提供了具有人胎盘起始雌二烯合成酶抑制作用的生物活性的14α-羟基-4-雄甾烯-3,6,17-三酮的稳定的水合物晶体。 这些水合晶体包括在结晶粉末X射线衍射中具有在衍射角具有特征峰的衍射图案的两种14α-羟基-4-雄甾烯-3,6,17-三酮水合物晶体。 还提供了生产这些水合物晶体的方法。
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公开(公告)号：US4582928A
公开(公告)日：1986-04-15
申请号：US716400
申请日：1985-03-27
IPC分类号： C07B57/00 , C07B31/00 , C07C67/00 , C07C227/34 , C07C229/36 , C07C101/08
CPC分类号： C07C227/34
摘要： This invention relates to a process for producing optically active phenylalanine, characterized by optically resolving DL-phenylalanine.optically active mandelic acid complexes in an aqueous solvent in the presence of an acidic compound having a pKa value of 0.90 to 2.10 and isolating optically active phenylalanine from the obtained optically active phenylalanine.optically active mandelic acid complex.According to the process of the present invention, it is possible to decrease the amount of a mother liquor of resolution to 1/5 to 1/10 of that when no acidic compound is used and to obtain optically active phenylalanine having an optical purity of as high as 96.5% or above without a step of optical purification when optically active phenylalanine is isolated from the obtained optically active phenylalanine.optically active mandelic acid complex.
摘要翻译： 本发明涉及一种光学活性苯丙氨酸的制备方法，其特征在于在pKa值为0.90至2.10的酸性化合物存在下，在水性溶剂中光学拆分DL-苯丙氨酸光学活性扁桃酸配合物，并将光学活性苯丙氨酸从 所得光学活性苯丙氨酸光学活性扁桃酸复合物。 根据本发明的方法，可以将分辨率降低至不使用酸性化合物时的1/5至1/10的量，并获得具有光学纯度的光学活性苯丙氨酸 光学活性苯丙氨酸光学活性苯丙氨酸复合物中分离出光学活性苯丙氨酸时，不需要光学纯化步骤，高达96.5％以上。
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3.发明授权14.alpha.-hydroxy-4-androstene-3,6,17-trione hydrate crystal and process for producing same 失效14α-羟基-4-雄甾烯-3,6,17-三酮水合物晶体及其制备方法
公开(公告)号：US5614651A
公开(公告)日：1997-03-25
申请号：US247778
申请日：1994-05-23
IPC分类号： A61K31/565 , C07J1/00
CPC分类号： C07J1/0011
摘要： Provided are stable hydrate crystals of 14.alpha.-hydroxy-4-androstene-3,6,17-trione having a biological activity of human placenta-originating estrodiene synthesis enzyme inhibitory action. These hydrate crystals include two kinds of 14.alpha.-hydroxy-4-androstene-3,6,17-trione hydrate crystals having a diffraction pattern having characteristic peaks at diffraction angles in crystalline powder X-ray diffraction. Processes for producing these hydrate crystals are also provided.
摘要翻译： 提供了具有人胎盘起始雌二烯合成酶抑制作用的生物活性的14α-羟基-4-雄甾烯-3,6,17-三酮的稳定的水合物晶体。 这些水合晶体包括在结晶粉末X射线衍射中具有在衍射角具有特征峰的衍射图案的两种14α-羟基-4-雄甾烯-3,6,17-三酮水合物晶体。 还提供了生产这些水合物晶体的方法。
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公开(公告)号：US4730076A
公开(公告)日：1988-03-08
申请号：US942146
申请日：1986-12-16
IPC分类号： C07K5/075 , C07C101/02
CPC分类号： C07K5/0613
摘要： The present invention relates to a process for producing .alpha.-aspartyl-phenylalanine ester represented by the general formula ##STR1## wherein R' represents an alkyl group having 1 to 4 carbon atoms, by reducing an N-protected-N-hydroxymethyl-.alpha.-aspartyl-phenylalanine ester represented by the general formula ##STR2## wherein R represents an organic mioety which can be substituted reductively by hydrogen, and R' is as defined above, with hydrogen gas or formic acid, in the presence of a reduction catalyst and an aromatic primary amine. According to the present invention, there can be obtained a high purity .alpha.-aspartyl-phenylalanine ester with a high yield.
摘要翻译： 本发明涉及通过还原N-保护的N-羟甲基-α-谷氨酰胺来制备由通式“IMAGE”表示的α-天门冬酰胺 - 苯丙氨酸酯的方法，其中R'代表具有1至4个碳原子的烷基， 由通式
表示的天冬氨酰基 - 苯丙氨酸酯，其中R表示可在氢还原催化剂和还原催化剂存在下用氢气或甲酸还原的氢被还原反应的R'和R'定义的有机二氧化物， 芳族伯胺。 根据本发明，可以高产率地得到高纯度的α-天冬氨酰基苯丙氨酸酯。
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