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公开(公告)号：US08420683B2
公开(公告)日：2013-04-16
申请号：US12601304
申请日：2008-06-03
IPC分类号： A61K31/4166 , C07D233/76
CPC分类号： C07D209/42 , C07D209/52 , C07D233/76 , C07D233/78 , C07D233/80
摘要： The present invention relates to 5-substituted hydantoins, a process for the preparation of 5-substituted hydantoins and the use of 5-substituted hydantoins in the preparation of enantiomerically enriched α-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel 5-substituted hydantoins.
摘要翻译： 本发明涉及5-取代的乙内酰脲，制备5-取代的乙内酰脲的方法和5-取代的乙内酰脲在制备对映体富集的α-氨基酸中的用途。 此外，本发明涉及使用新的5-取代的乙内酰脲制备药物活性产物如培哚普利和雷米普利。
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公开(公告)号：US20100174092A1
公开(公告)日：2010-07-08
申请号：US12601304
申请日：2008-06-03
IPC分类号： C07D235/02 , C07D233/72
CPC分类号： C07D209/42 , C07D209/52 , C07D233/76 , C07D233/78 , C07D233/80
摘要： The present invention relates to 5-substituted hydantoins, a process for the preparation of 5-substituted hydantoins and the use of 5-substituted hydantoins in the preparation of enantiomerically enriched α-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel 5-substituted hydantoins.
摘要翻译： 本发明涉及5-取代的乙内酰脲，制备5-取代的乙内酰脲的方法和5-取代的乙内酰脲在制备对映体富集的α-氨基酸中的用途。 此外，本发明涉及使用新的5-取代的乙内酰脲制备药物活性产物如培哚普利和雷米普利。
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公开(公告)号：US20080249329A1
公开(公告)日：2008-10-09
申请号：US12088159
申请日：2006-09-26
IPC分类号： C07C229/52
CPC分类号： C07C67/10 , C07C229/36 , C07C69/78
摘要： The invention relates to a sulphonic acid salt of an amino acid alkyl ester The invention further relates to a process for the esterification of an organic acid into the corresponding organic acid ester comprising bringing the organic acid into contact with a strong acid and a solution comprising dialkylcarbonate in a reaction mixture. The invention further relates to the use of a sulphonic acid salt of an amino acid alkyl ester in the synthesis of a β-lactam antibiotic.
摘要翻译： 本发明涉及氨基酸烷基酯的磺酸盐本发明还涉及将有机酸酯化成相应的有机酸酯的方法，包括使有机酸与强酸和包含二烷基碳酸酯的溶液接触 在反应混合物中。 本发明还涉及氨基酸烷基酯的磺酸盐在β-内酰胺抗生素的合成中的用途。
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公开(公告)号：US20130303779A1
公开(公告)日：2013-11-14
申请号：US13980154
申请日：2012-01-13
IPC分类号： C07D417/12 , C07D405/12
CPC分类号： C07D417/12 , C07D405/12 , C07D413/12 , C07D419/12
摘要： The present invention relates to a process for the preparation of a diol sulfone derivative comprising reaction of a halomethyl substrate with a thio-aryl compound to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.
摘要翻译： 本发明涉及一种制备二醇砜衍生物的方法，包括卤甲基底物与硫代 - 芳基化合物的反应，得到硫醚化合物，并将硫代醚化合物氧化为相应的砜。 在手性卤代甲基底物的情况下，所得手性二醇砜衍生物适合作为他汀类化合物的结构单元。
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公开(公告)号：US09126975B2
公开(公告)日：2015-09-08
申请号：US13979976
申请日：2012-01-13
IPC分类号： C07D405/06 , C07D413/12 , C07D419/12
CPC分类号： C07D405/06 , C07D413/12 , C07D419/12
摘要： The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.
摘要翻译： 本发明涉及在碱金属烷氧基的存在下，通过醛和砜衍生物之间的朱莉娅 - 科奇宁斯基反应制备他汀类药物的方法。 所得衍生物适合作为他汀类化合物如西立伐他汀，氟伐他汀，匹伐他汀和罗苏伐他汀的结构单元。
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公开(公告)号：US20110263871A1
公开(公告)日：2011-10-27
申请号：US13126871
申请日：2009-10-27
申请人： Ben De Lange , Dennis Heemskerk
发明人： Ben De Lange , Dennis Heemskerk
IPC分类号： C07D209/52
CPC分类号： C07D209/52
摘要： The present invention relates to a process for the preparation of octahydrocyclopenta[b]pyrrole-2-carboxylic acid and esters thereof of general formula (1) in the presence of a cobalt and/or nickel comprising catalyst and to the use of compounds of general formula (1) in the synthesis of ramipril.
摘要翻译： 本发明涉及在含有钴和/或镍的催化剂存在下制备通式（1）的八氢环戊并[b]吡咯-2-羧酸及其酯的方法，以及使用一般化合物 式（1）中雷米普利的合成。
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公开(公告)号：US09150562B2
公开(公告)日：2015-10-06
申请号：US13980154
申请日：2012-01-13
IPC分类号： C07D405/12 , C07D417/12 , C07D413/12 , C07D419/12
CPC分类号： C07D417/12 , C07D405/12 , C07D413/12 , C07D419/12
摘要： The present invention relates to a process for the preparation of a diol sulfone derivative comprising reaction of a halomethyl substrate with a thio-aryl compound to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.
摘要翻译： 本发明涉及一种制备二醇砜衍生物的方法，包括卤甲基底物与硫代 - 芳基化合物的反应，得到硫醚化合物，并将硫代醚化合物氧化为相应的砜。 在手性卤代甲基底物的情况下，所得手性二醇砜衍生物适合作为他汀类化合物的结构单元。
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公开(公告)号：US20130296561A1
公开(公告)日：2013-11-07
申请号：US13979976
申请日：2012-01-13
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07D413/12 , C07D419/12
摘要： The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.
摘要翻译： 本发明涉及在碱金属烷氧基的存在下，通过醛和砜衍生物之间的朱莉娅 - 科奇宁斯基反应制备他汀类药物的方法。 所得衍生物适合作为他汀类化合物如西立伐他汀，氟伐他汀，匹伐他汀和罗苏伐他汀的结构单元。
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公开(公告)号：US08263784B2
公开(公告)日：2012-09-11
申请号：US13126871
申请日：2009-10-27
申请人： Ben De Lange , Dennis Heemskerk
发明人： Ben De Lange , Dennis Heemskerk
IPC分类号： C07D209/02
CPC分类号： C07D209/52
摘要： The present invention relates to a process for the preparation of octahydrocyclopenta[b]pyrrole-2-carboxylic acid and esters thereof of general formula (1) in the presence of a cobalt and/or nickel comprising catalyst and to the use of compounds of general formula (1) in the synthesis of ramipril.
摘要翻译： 本发明涉及在含有钴和/或镍的催化剂存在下制备通式（1）的八氢环戊并[b]吡咯-2-羧酸及其酯的方法，以及使用一般化合物 式（1）中雷米普利的合成。
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10.发明授权Process for the preparation of 2,4-dideoxyhexoses and 2,4,6-trideoxyhexoses 有权2,4-二脱氧己糖和2,4,6-三脱氧己糖的制备方法公开(公告)号：US07439046B2
公开(公告)日：2008-10-21
申请号：US11206574
申请日：2005-08-17
申请人： Joannes Gerardus Kierkels , Daniel Mink , Sven Panke , Franciscus Alphons Lommen , Dennis Heemskerk
发明人： Joannes Gerardus Kierkels , Daniel Mink , Sven Panke , Franciscus Alphons Lommen , Dennis Heemskerk
IPC分类号： C12P17/06
摘要： The invention relates to a process for the preparation of a 2,4-dideoxyhexose or a 2,4,6-trideoxyhexose from a substituted or unsubstituted carbonyl compound with at least 2 carbon atoms and at least one α-hydrogen atom and a substituted or unsubstituted aldehyde in the presence of an aldolase and water, the reaction between the substituted or unsubstituted carbonyl compound with at least 2 carbon atoms and at least one α-hydrogen atom and the substituted or unsubstituted aldehyde being carried out at a carbonyl concentration of at most 6 moles/l of reaction mixture and the final concentration of the 2,4-dideoxyhexose or the 2,4,6-trideoxyhexose being at least 2 mass % of the reaction mixture. The invention also relates to the use of a 2,4-dideoxyhexose or a 2,4,6-trideoxyhexose obtained by means of a process according to the invention in the preparation of a medicine, particularly in the preparation of a statine.
摘要翻译： 本发明涉及从具有至少2个碳原子和至少一个α-氢原子的取代或未取代的羰基化合物和取代或未取代的羰基化合物制备2,4-二脱氧己糖或2,4,6-三脱氧己糖的方法， 未取代的醛在醛缩酶和水的存在下，取代或未取代的羰基化合物与至少2个碳原子和至少一个α-氢原子之间的反应和取代或未取代的醛以最多羰基浓度进行 6摩尔/升的反应混合物，2,4-二脱氧己糖或2,4,6-三脱氧己糖的最终浓度为反应混合物的至少2质量％。 本发明还涉及通过根据本发明的方法获得的2,4-二脱氧己糖或2,4,6-三脱氧己糖在制备药物中的用途，特别是在制备他汀类药物中的用途。
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