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1. 发明申请

US20080167500A1 Process for the Preparation of a Diastereomerically Enriched Compound 审中-公开
标题翻译：制备非对映异构体的化合物的方法
公开(公告)号：US20080167500A1
公开(公告)日：2008-07-10
申请号：US11632699
申请日：2005-07-20
申请人： Quirinus Bernardus Broxterman , Ben De Lange , Henrius Leonardus Marie Elsenberg , Matthias Weber
发明人： Quirinus Bernardus Broxterman , Ben De Lange , Henrius Leonardus Marie Elsenberg , Matthias Weber
IPC分类号： C07C211/01
CPC分类号： C07C209/28 , C07C2601/02 , C07C211/17 , C07C211/27 , C07C211/29
摘要： The present invention relates to a process for the preparation of a diastereomerically enriched compound, wherein a first compound according to formula (I), is contacted with a second compound according to formula (II), to form a third compound according to formula (III), whereby the compound according to formula (III) is subsequently reduced and thereby converted into a compound according to formula (IV), in which formulas: R1=a cycloalkyl group whereby R1 # R2, R2=a substituted or unsubstituted: (cyclo)alkyl group, (cyclo)alkenyl group, aryl group, cyclic or acyclic heteroalkyl group or heteroaryl group, R3=an alkyl group, R4=a substituted or unsubstituted: phenyl- or naphthyl-group, *=a chiral center. The invention furthermore relates to a diastereomerically enriched compound according to formula (IV) and its use in the preparation of pharmaceutical and agrochemically active compounds. The invention further relates to a process for the preparation of enantiomerically enriched compounds of formula (V), through hydrogenolysis of diastereomerically enriched compounds of formula (IV), wherein R1 and R2 have the meanings given above.
摘要翻译：本发明涉及一种制备非对映体富集的化合物的方法，其中根据式（I）的第一化合物与式（II）的第二化合物接触，以形成式（III）的第三化合物），由此将式（III）化合物随后还原，从而转化成式（Ⅳ）化合物，其中R 1 =环烷基，其中R 1 （环）烷基，（环）烯基，芳基，环状或无环杂烷基的取代或未取代的或杂芳基，R 3 =烷基，R 4 =取代或未取代的：苯基或萘基，* =手性中心。本发明还涉及根据式（IV）的非对映异构体富集的化合物及其在制备药物和农业化学活性化合物中的用途。本发明还涉及通过氢解非对映体富集的式（Ⅳ）化合物来制备对映体富集的式（Ⅴ）化合物的方法，其中R 1和R 2， SUB>具有上述含义。

2. 发明申请

US20110008852A1 CONVERGENT SYNTHESIS OF RENIN INHIBITORS AND INTERMEDIATES USEFUL THEREIN 失效
标题翻译：雷尼辛抑制剂和中间体的合成合成
公开(公告)号：US20110008852A1
公开(公告)日：2011-01-13
申请号：US12810220
申请日：2008-12-19
申请人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Boogers , Quirinus Bernardus Broxterman
发明人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Boogers , Quirinus Bernardus Broxterman
IPC分类号： C12P13/00 , C07C253/16 , C07C255/20 , C07F7/18 , C07D307/33 , C07C43/205
CPC分类号： C07D307/33 , C07C231/02 , C07C231/18 , C07D307/32 , C07F1/02 , C07F7/1804 , C07C237/22
摘要： Described is a method for the preparation of renin inhibitors such as aliskiren, and intermediates useful therein. The method introduces a nitrogen-containing intermediate such as a lactone of formula (8). with R4 being a branched C3—6 alkyl. In the preparation of the lactone, or related intermediates, a desired stereochemical configuration can be controlled by starting from a chiral aldehyde satisfying formula (10).
摘要翻译：描述了制备肾素抑制剂如阿利吉仑的方法和其中有用的中间体。该方法引入含氮中间体如式（8）的内酯。其中R4是支链C 3-6烷基。在内酯或相关中间体的制备中，可以通过从满足式（10）的手性醛开始来控制所需的立体化学构型。

3. 发明授权

US08563279B2 Convergent synthesis of renin inhibitors and intermediates useful therein 失效
标题翻译：肾素抑制剂和其中有用的中间体的收敛合成
公开(公告)号：US08563279B2
公开(公告)日：2013-10-22
申请号：US12810220
申请日：2008-12-19
申请人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Franciscus Boogers , Quirinus Bernardus Broxterman
发明人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Franciscus Boogers , Quirinus Bernardus Broxterman
IPC分类号： C07C231/18 , C07C253/16 , C07C255/20 , C07F1/02 , C07F7/18 , C07D307/32 , C07D307/33 , C12P13/00
CPC分类号： C07D307/33 , C07C231/02 , C07C231/18 , C07D307/32 , C07F1/02 , C07F7/1804 , C07C237/22
摘要： Described is a method for the preparation of renin inhibitors such as aliskiren, and intermediates useful therein. The method introduces a nitrogen-containing intermediate such as a lactone of formula (8). with R4 being a branched C3—6 alkyl. In the preparation of the lactone, or related intermediates, a desired stereochemical configuration can be controlled by starting from a chiral aldehyde satisfying formula (10).
摘要翻译：描述了制备肾素抑制剂如阿利吉仑的方法和其中有用的中间体。该方法引入含氮中间体如式（8）的内酯。其中R4是支链C 3-6烷基。在内酯或相关中间体的制备中，可以通过从满足式（10）的手性醛开始来控制所需的立体化学构型。

4. 发明授权

US09126975B2 Process for the preparation of statins in the presence of base 有权
标题翻译：在基础存在下制备他汀类药物的方法
公开(公告)号：US09126975B2
公开(公告)日：2015-09-08
申请号：US13979976
申请日：2012-01-13
申请人： Karin Henderika Maria Bessembinder , Dennis Heemskerk , Ben De Lange
发明人： Karin Henderika Maria Bessembinder , Dennis Heemskerk , Ben De Lange
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。

5. 发明授权

US08105807B2 Carbamoylglycine derivatives 失效
标题翻译：氨基甲酰甘氨酸衍生物
公开(公告)号：US08105807B2
公开(公告)日：2012-01-31
申请号：US12738736
申请日：2008-10-02
申请人： Georgios Sarakinos , Ben De Lange
发明人： Georgios Sarakinos , Ben De Lange
IPC分类号： C12P17/10 , C12P13/04 , C07C229/12
CPC分类号： C07D209/52 , C07C275/18
摘要： The present invention relates to carbamoylglycine derivatives, a process for the preparation of carbamoylglycine derivatives and the use of carbamoylglycine derivatives 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 carbamoylglycine derivatives.
摘要翻译：本发明涉及氨基甲酰基甘氨酸衍生物，氨基甲酰基甘氨酸衍生物的制备方法和氨基甲酰基甘氨酸衍生物在制备对映异构体富集的α-氨基酸中的用途。此外，本发明涉及使用新的氨基甲酰基甘氨酸衍生物制备药物活性产物如培哚普利和雷米普利。

6. 发明申请

US20100174092A1 NOVEL 5 SUBSTITUTED HYDANTOINS 失效
标题翻译：第5代替代HYDANTOINS
公开(公告)号：US20100174092A1
公开(公告)日：2010-07-08
申请号：US12601304
申请日：2008-06-03
申请人： Georgios Sarakinos , Wilhelmus Hubertus Joseph Boesten , Dennis Heemskerk , Ben De Lange
发明人： Georgios Sarakinos , Wilhelmus Hubertus Joseph Boesten , Dennis Heemskerk , Ben De Lange
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。

7. 发明授权

US07732621B2 Process for the preparation of enantiomerically enriched indoline-2-carboxylic acid 有权
标题翻译：用于制备对映体富集的二氢吲哚-2-羧酸的方法
公开(公告)号：US07732621B2
公开(公告)日：2010-06-08
申请号：US11794246
申请日：2005-12-22
申请人： Andreas Hendrikus Maria De Vries , Johannes Gerardus De Vries , Friso Bernard Jan Van Assema , Ben De Lange , Daniel Mink , David John Hyett , Peter Johannes Dominicus Maas
发明人： Andreas Hendrikus Maria De Vries , Johannes Gerardus De Vries , Friso Bernard Jan Van Assema , Ben De Lange , Daniel Mink , David John Hyett , Peter Johannes Dominicus Maas
IPC分类号： C07D209/04
CPC分类号： C07D209/42
摘要： The present invention relates to a process for the preparation of an enantiomerically enriched optionally substituted indoline-2-carboxylic acid or a salt thereof, wherein an enantiomerically enriched chiral ortho-X-substituted phenylalanine compound, wherein X is a leaving group, is subjected to cyclisation, preferably at a temperature of below about 140° C., upon formation of the enantiomerically enriched indoline-2-carboxylic acid compound.
摘要翻译：本发明涉及一种制备对映体富集的任选取代的二氢吲哚-2-羧酸或其盐的方法，其中将对映异构体富集的手性邻-X取代的苯丙氨酸化合物（其中X为离去基团）在形成对映体富集的二氢吲哚-2-羧酸化合物时，优选在低于约140℃的温度下进行环化。

8. 发明申请

US20130303779A1 PROCESS FOR THE PREPARATION OF DIOL SULFONES 有权
标题翻译：制备二氧化硅的方法
公开(公告)号：US20130303779A1
公开(公告)日：2013-11-14
申请号：US13980154
申请日：2012-01-13
申请人： Ben De Lange , Peter Hans Riebel , Michael Wolberg , Dennis Heemskerk , Daniel Mink
发明人： Ben De Lange , Peter Hans Riebel , Michael Wolberg , Dennis Heemskerk , Daniel Mink
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。

9. 发明申请

US20100221796A1 NOVEL CARBAMOYLGLYCINE DERIVATIVES 失效
标题翻译：新型卡巴醇衍生物
公开(公告)号：US20100221796A1
公开(公告)日：2010-09-02
申请号：US12738736
申请日：2008-10-02
申请人： Georgios Sarakinos , Ben De Lange
发明人： Georgios Sarakinos , Ben De Lange
IPC分类号： C12P17/10 , C07C62/00 , C12P7/40
CPC分类号： C07D209/52 , C07C275/18
摘要： The present invention relates to carbamoylglycine derivatives, a process for the preparation of carbamoylglycine derivatives and the use of carbamoylglycine derivatives 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 carbamoylglycine derivatives.
摘要翻译：本发明涉及氨基甲酰基甘氨酸衍生物，氨基甲酰基甘氨酸衍生物的制备方法和氨基甲酰基甘氨酸衍生物在制备对映异构体富集的α-氨基酸中的用途。此外，本发明涉及使用新的氨基甲酰基甘氨酸衍生物制备药物活性产物如培哚普利和雷米普利。

10. 发明申请

US20130296563A1 METHYLTETRAZOLE SULFIDES AND SULFONES 有权
标题翻译：甲基噻唑磺酸和硫磺
公开(公告)号：US20130296563A1
公开(公告)日：2013-11-07
申请号：US13979755
申请日：2012-01-13
申请人： Ben De Lange
发明人： Ben De Lange
IPC分类号： C07D405/12 , C07D405/14 , C07D405/06
CPC分类号： C07D405/12 , C07D405/06 , C07D405/14 , C07D413/12 , C07D419/12
摘要： The present invention relates to a process for the preparation of a 1-methyl-1H-tetrazole-5-thio derivative comprising reaction of a halomethyl substrate with 1-methyl-H-tetrazole-5-thiol 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1-甲基-1H-四唑-5-硫代衍生物的制备方法，其包括卤甲基底物与1-甲基-4-四唑-5-硫醇的反应，得到硫代醚化合物，并将硫代醚化合物氧化成相应的砜。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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