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1.发明授权Crystals of N-(trans-4-isopropylcyclohexycarbonyl)-D-phenylalanine and methods for preparing them 失效N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的晶体及其制备方法
公开(公告)号：US5488150A
公开(公告)日：1996-01-30
申请号：US166144
申请日：1993-12-14
IPC分类号： C07C231/24 , A61K31/13 , A61K31/195 , C07C211/43 , C07C231/22 , C07C233/63 , C07C239/00
CPC分类号： C07C231/22 , C07C233/63
摘要： Stable crystals of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine may be produced by treating this compound with a solvent at a temperature of at least 10.degree. C. and forming crystals in the solvent at a temperature of at least 10.degree. C. For example, crystals may be formed by crystallization out of solution, or may be formed from solid particles of the compound suspended in a solvent. Crystals formed in this way have different melting point, infra red spectrum and X-ray diffraction patterns from previously known forms of the compound and have enhanced processability, eg. stability to grinding.
摘要翻译： N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的稳定晶体可以通过在至少10℃的温度下用溶剂处理该化合物并在溶剂中在至少10℃的温度下形成晶体来制备 例如，可以通过从溶液中结晶而形成晶体，或者可以由悬浮在溶剂中的化合物的固体颗粒形成晶体。 以这种方式形成的晶体具有来自先前已知形式的化合物的不同的熔点，红外光谱和X射线衍射图，并具有增强的可加工性，例如。 稳定磨削。
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2.发明授权Crystals of N- (trans-4-isopropylcyclohexlycarbonyl)-D-phenylalanine and methods for preparing them 失效N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的晶体及其制备方法
公开(公告)号：US5463116A
公开(公告)日：1995-10-31
申请号：US190460
申请日：1994-02-02
IPC分类号： C07C231/22 , C07C233/63 , C07C229/00
CPC分类号： C07C231/22 , C07C233/63 , C07B2200/13 , C07C2101/14
摘要： Stable crystals of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine may be produced by treating this compound with a solvent at a temperature of at least 10.degree. C. and forming crystals in the solvent at a temperature of at least 10.degree. C. For example, crystals may be formed by crystallization out of solution, or may be formed from solid particles of the compound suspended in a solvent. Crystals formed in this way have different melting point, infra red spectrum and X-ray diffraction patterns from previously known forms of the compound and have enhanced processability, e.g., stability to grinding.
摘要翻译： N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的稳定晶体可以通过在至少10℃的温度下用溶剂处理该化合物并在溶剂中在至少10℃的温度下形成晶体来制备 例如，可以通过从溶液中结晶而形成晶体，或者可以由悬浮在溶剂中的化合物的固体颗粒形成晶体。 以这种方式形成的晶体具有来自先前已知形式的化合物的不同的熔点，红外光谱和X射线衍射图，并且具有增强的加工性，例如研磨的稳定性。
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公开(公告)号：US20050101672A1
公开(公告)日：2005-05-12
申请号：US10965171
申请日：2004-10-15
IPC分类号： A61K31/198 , C07C233/63 , C07C233/76
CPC分类号： C07C233/63 , C07C2601/14
摘要： New nateglinide crystals, i.e. nateglinide A-type crystals (main peaks in powder X-ray diffraction: 4.4°, 5.2°, 15.7°, 18.5°(2θ)), M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8°(2θ)) and P-type crystals (main peaks in powder X-ray diffraction: 4.8°, 5.3°, 14.3°, 15.2°(2θ)), can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble or, alternatively, by dissolving nateglinide in a mixed solvent composed of a solvent in which nateglinide is highly soluble and another solvent in which it is difficultly soluble, cooling the nateglinide solution to form crystals, filtering the mixture and drying the crystals at a specified temperature.
摘要翻译： 新那格列奈晶体，即那格列奈A型晶体（粉末X射线衍射中的主峰：4.4°，5.2°，15.7°，18.5°（2θ）），M型晶体（粉末X射线衍射中的主峰： 6.0°，14.2°，15.2°，18.8°（2θ））和P型晶体（粉末X射线衍射中的主峰：4.8°，5.3°，14.3°，15.2°（2θ））可以通过 将那格列奈溶解在那格列奈高度溶解的溶剂中，然后加入那格列奈难以溶解的溶剂，或者通过将那格列奈溶解在由那格列奈高度溶解的溶剂和其中所述的其他溶剂组成的混合溶剂中 难以溶解，冷却那格列奈溶液形成晶体，过滤混合物并在特定温度下干燥晶体。
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公开(公告)号：US07888531B2
公开(公告)日：2011-02-15
申请号：US12485156
申请日：2009-06-16
IPC分类号： C07C229/00 , C07C51/15
CPC分类号： C07C233/63 , C07C2601/14
摘要： Nateglinide M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2θ)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble.
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公开(公告)号：US07586001B2
公开(公告)日：2009-09-08
申请号：US12098118
申请日：2008-04-04
IPC分类号： C07C229/00 , C07C51/15
CPC分类号： C07C233/63 , C07C2601/14
摘要： New nateglinide crystals, i. e. nateglinide A-type crystals (main peaks in powder X-ray diffraction: 4.4°, 5.2°, 15.7°, 18.5° (2θ)), M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2θ)) and P-type crystals (main peaks in powder X-ray diffraction: 4.8°, 5.3°, 14.3°, 15.2° (2θ)), can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble or, alternatively, by dissolving nateglinide in a mixed solvent composed of a solvent in which nateglinide is highly soluble and another solvent in which it is difficultly soluble, cooling the nateglinide solution to form crystals, filtering the mixture and drying the crystals at a specified temperature.
摘要翻译： 新奈格列奈晶体， e。 那格列奈A型晶体（粉末X射线衍射中的主峰：4.4°，5.2°，15.7°，18.5°（2θ）），M型晶体（粉末X射线衍射中的主峰：6.0°，14.2° ，15.2°，18.8°（2θ））和P型晶体（粉末X射线衍射中的主峰：4.8°，5.3°，14.3°，15.2°（2θ））可以通过将那格列奈溶解在溶剂中 其中那格列奈高度可溶，然后加入那格列奈难以溶解的溶剂，或者通过将那格列奈溶解在由那格列奈高度溶解的溶剂和难溶于其中的溶剂组成的混合溶剂中，冷却 那格列奈溶液形成晶体，过滤混合物并在特定温度下干燥晶体。
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公开(公告)号：US07977507B2
公开(公告)日：2011-07-12
申请号：US12969013
申请日：2010-12-15
IPC分类号： C07C229/00 , C07C51/15
CPC分类号： C07C233/63 , C07C2601/14
摘要： Nateglinide M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2θ)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble.
摘要翻译： 那格列奈M型晶体（粉末X射线衍射中的主峰：6.0°，14.2°，15.2°，18.8°（2θ））可以通过将那格列奈溶解在那格列奈高度溶解的溶剂中，然后加入 那格列奈难以溶解的溶剂。
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公开(公告)号：US07411089B2
公开(公告)日：2008-08-12
申请号：US10965171
申请日：2004-10-15
IPC分类号： C07C229/00 , C07C51/15
CPC分类号： C07C233/63 , C07C2601/14
摘要： New nateglinide crystals, i.e. nateglinide A-type crystals (main peaks in powder X-ray diffraction: 4.4°, 5.2°, 15.7°, 18.5°(2θ)), M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8°(2θ)) and P-type crystals (main peaks in powder X-ray diffraction: 4.8°, 5.3°, 14.3°, 15.2°(2θ)), can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble or, alternatively, by dissolving nateglinide in a mixed solvent composed of a solvent in which nateglinide is highly soluble and another solvent in which it is difficultly soluble, cooling the nateglinide solution to form crystals, filtering the mixture and drying the crystals at a specified temperature.
摘要翻译： 新那格列奈晶体，即那格列奈A型晶体（粉末X射线衍射中的主峰：4.4°，5.2°，15.7°，18.5°（2θ）），M型晶体（粉末X射线衍射中的主峰： 6.0°，14.2°，15.2°，18.8°（2θ））和P型晶体（粉末X射线衍射中的主峰：4.8°，5.3°，14.3°，15.2°（2θ））可以通过 将那格列奈溶解在那格列奈高度溶解的溶剂中，然后加入那格列奈难以溶解的溶剂，或者通过将那格列奈溶解在由那格列奈高度溶解的溶剂和其中所述的其他溶剂组成的混合溶剂中 难以溶解，冷却那格列奈溶液形成晶体，过滤混合物并在特定温度下干燥晶体。
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公开(公告)号：US5336770A
公开(公告)日：1994-08-09
申请号：US917357
申请日：1992-07-23
IPC分类号： A61K31/52 , A61K31/522 , A61P31/12 , C07D239/26 , C07D239/42 , C07D473/00 , C07D473/18 , C07D473/30 , C07D473/34 , C07H19/16 , C07B43/04
CPC分类号： C07D473/00 , C07D473/18 , C07H19/16
摘要： Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar.
摘要翻译： 本文公开了一种用于从核糖核苷合成无环型核苷如阿昔洛韦和更昔洛韦的新颖且工业上有利的方法，该方法包括向核糖核苷如鸟苷和无环糖的酯衍生物的溶液中加入酸催化剂和酸酐， 并加热混合物，由此在核糖核苷的核糖部分和无环糖的酯衍生物之间发生反缩糖反应。
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9.发明授权Process for producing acyclic nucleosides and process for separating purine nucleosides 失效用于生产无环核苷的方法和用于分离嘌呤核苷的方法
公开(公告)号：US5792868A
公开(公告)日：1998-08-11
申请号：US214756
申请日：1994-03-18
IPC分类号： C07D473/00 , C07D473/18 , C07H19/16 , C07D473/16 , C07D473/30 , C07D473/34
CPC分类号： C07D473/00 , C07D473/18 , C07H19/16
摘要： Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar. Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.
摘要翻译： 本文公开了一种用于从核糖核苷合成无环型核苷如阿昔洛韦和更昔洛韦的新颖且工业上有利的方法，该方法包括向核糖核苷如鸟苷和无环糖的酯衍生物的溶液中加入酸催化剂和酸酐， 并加热混合物，由此在核糖核苷的核糖部分和无环糖的酯衍生物之间发生反缩糖反应。 本文还公开了用于分离9-取代嘌呤核苷的工业上有利的方法，其是从核糖核苷合成无环核苷如阿昔洛韦，更昔洛韦等的重要中间体，该方法包括仅将9-异构体从 通过冷却溶液或/和通过向其中加入结晶溶剂而含有9-取代的嘌呤核苷和7-取代的嘌呤核苷的溶液或悬浮液。
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10.发明授权Method for producing &bgr;-D-ribofuranose derivatives or optical isomers thereof 失效制备β-D-呋喃核糖衍生物或其旋光异构体的方法公开(公告)号：US06800742B2
公开(公告)日：2004-10-05
申请号：US10100909
申请日：2002-03-20
IPC分类号： C07H1500
摘要： The present invention provides a method for efficiently producing &bgr;-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series products. The method comprises a step of producing 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate or an optical isomer thereof by allowing &bgr;-D-ribofuranose-1,2,3,5-tetraacetate or an optical isomer thereof to react with a benzyl alcohol in the presence of acid catalysts and a step of hydrolyzing the resulting 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate in the presence of a base to produce 1-O-benzyl-&bgr;-D-ribofuranose or an optical isomer thereof.
摘要翻译： 本发明提供了有效生产β-D-呋喃核糖衍生物或其光学异构体的方法，其可用作药物核酸系列产品的合成中间体。 该方法包括通过使β-D-呋喃核糖-1,2,3,5-四乙酸酯或其制备方法制备1-O-苄基-β-D-呋喃核糖-2,3,5-三乙酸酯或其旋光异构体的步骤 其光学异构体在酸催化剂存在下与苄醇反应，并在碱的存在下水解所得的1-O-苄基-β-D-呋喃核糖-2,3,5-三乙酸酯以产生1 -O-苄基-β-D-呋喃核糖或其旋光异构体。
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