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公开(公告)号：EP2480523A1
公开(公告)日：2012-08-01
申请号：EP10818263.5
申请日：2010-03-23
发明人： ZHU, Guoliang , SHI, Desong , WEI, Junhui , TAO, Fengfeng
IPC分类号： C07C231/12 , C07C233/47 , C07C233/51 , C07D263/18
CPC分类号： C07C233/47 , C07C233/51 , C07C233/83 , C07C233/87 , C07D263/20
摘要： A novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.
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公开(公告)号：EP2272853A1
公开(公告)日：2011-01-12
申请号：EP09734964.1
申请日：2009-01-20
发明人： ZHOU, Qilin , ZHU, Shoufei , LI, Shen , WANG, Lixin , SONG, Song
CPC分类号： C07F9/653 , B01J31/189 , B01J2231/645 , B01J2531/827 , C07B2200/07 , C07C51/36 , C07F15/0033 , C07F15/0046 , C07C59/68 , C07C57/30
摘要： The present invention belongs to a spiro phosphine-oxazoline and preparation method and application thereof, particularly, publishes a novel spiro phosphine-oxazoline and the preparation method of its iridium complex. The substituted 7-diaryl phosphino-7'-carboxy-1,1'-Lo-dihydro-indene is used as the starting raw material to synthesize the novel spiro phosphine-oxazoline of the present invention through a two-step reaction. The novel spiro phosphine-oxazoline and the iridium precursor are complexed to become a complex, and then through ion exchange, an iridium/phosphine spiro-oxazoline complex with different anions can be obtained. The present invention overcomes the shortcomings of the existing technology. The cheap readily available amino alcohol is used as the raw material to synthesize the novel spiro phosphine-oxazoline, on the fourth position of the oxazoline ring of which there is no substituent. The iridium complex of this novel spiro phosphine-oxazoline can catalyze the asymmetric hydrogenation of α-substituted acrylic acid, and shows very high activity and enantioselectivity, therefore has a vey high research value and an industrialization prospect.
摘要翻译： 本发明属于螺环膦 - 恶唑啉及其制备方法和应用，特别公开了一种新型螺环膦 - 恶唑啉及其铱配合物的制备方法。 取代的7-二芳基膦基-7'-羧基-1,1'-O-二氢茚被用作起始原料，通过两步反应合成本发明的新型螺环膦 - 恶唑啉。 新型螺环膦 - 恶唑啉与铱前体络合形成配合物，然后通过离子交换获得具有不同阴离子的铱/膦螺恶唑啉配合物。 本发明克服了现有技术的缺点。 廉价易得的氨基醇用作合成新型螺环膦 - 恶唑啉的原料，在其没有取代基的恶唑啉环的第四位上。 该新型螺环膦 - 恶唑啉的铱配合物催化α-取代丙烯酸的不对称氢化反应，具有很高的活性和对映选择性，具有很高的研究价值和工业化前景。
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公开(公告)号：EP4008712A1
公开(公告)日：2022-06-08
申请号：EP20848133.3
申请日：2020-06-08
发明人： LI, Hongliang , ZHANG, Xianyi , GAO, Zhaobo , MEI, Yijiang
IPC分类号： C07C227/36 , C07C231/12 , C07D241/08 , C07D295/185 , C07D471/04 , C07D487/04 , C07C229/34 , C07C233/47 , C07C229/12 , C07C229/18 , C07B55/00
摘要： The present disclosure relates to the field of medicine synthesis, and relates to a method for a racemic preparation of chiral β -amino acids and derivatives thereof, and in particular to a method for racemizing sitagliptin intermediates.
where R 1 is hydrogen, alkyl or aryl; R 2 is hydrogen, alkyl or aryl; R 3 is hydrogen, alkyl, aryl or acyl; R 4 is alkyl, aryl, OR', SR', NHR' or NR'R", wherein R', R" are hydrogen, alkyl or aryl.-
公开(公告)号：EP2752419B1
公开(公告)日：2019-01-02
申请号：EP12828043.5
申请日：2012-07-27
发明人： ZHOU, Qilin , ZHU, Shoufei , YU, Yanbo , LI, Kun , WANG, Lixin
IPC分类号： C07F9/50 , C07F19/00 , B01J31/24 , C07B35/02 , C07C51/36 , C07C57/30 , C07C59/64 , C07C57/58 , C07C53/128 , C07C67/303 , C07C69/42 , C07C59/13 , C07C59/125
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25.发明公开PREPARATION METHOD FOR PYRROLIDINE-2-CARBOXYLIC ACID DERIVATIVES 审中-公开VERFAHREN ZUR HERSTELLUNG VON PYRRIDIDIN-2-CARBONSAUREDERIVATEN
公开(公告)号：EP3015456A1
公开(公告)日：2016-05-04
申请号：EP14816731.5
申请日：2014-06-23
发明人： ZHANG, Bin , LI, Yuanqiang , CHE, Daqing , QIAN, Lingfeng , ZHU, Guoliang , YE, Wenfa
IPC分类号： C07D207/22 , C07D207/46 , C07D207/16
CPC分类号： C07D207/22 , C07D207/16 , Y02P20/55
摘要： The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R 1 or R2, R1 is C1-C6 an alkyl, benzyl, p-methoxybenzyl, or p-nitrobenzyl group, and R2 is hydrogen; R3 is a protecting group of the carboxyl group; and P1 is a protecting group on nitrogen.
摘要翻译： 本发明涉及医药合成领域，特别涉及吡咯烷-2-羧酸衍生物的制备方法。 本发明采用以下技术方案：提供具有式（E）结构的化合物，其中R为R 1或R 2，R 1为C 1 -C 6烷基，苄基，对甲氧基苄基或对硝基苄基， R2是氢; R3是羧基的保护基; P1是氮的保护基。
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26.发明授权
公开(公告)号：EP2275398B1
公开(公告)日：2016-05-04
申请号：EP09733969.1
申请日：2009-01-20
发明人： ZHOU, Qilin , LI, Shen , ZHU, Shoufei , ZHANG, Canming , WANG, Lixin
IPC分类号： C07C51/347 , C07C57/04 , C07F9/653 , B01J31/18 , B01J31/22 , B01J31/24 , C07B53/00 , C07C51/36 , C07C201/12 , C07D263/12 , C07D307/54 , C07F15/00 , C07F17/02
CPC分类号： C07F9/653 , B01J31/189 , B01J31/2295 , B01J2231/645 , B01J2531/827 , C07B53/00 , C07B2200/07 , C07C51/36 , C07D263/12 , C07D307/54 , C07F15/0033 , C07F17/02 , C07C57/30 , C07C59/64
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27.发明公开SPIROBENZYLAMINE-PHOSPHINE, PREPARATION METHOD THEREFOR AND USE THEREOF 审中-公开维生素Z- U IN ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON ON
公开(公告)号：EP2752419A1
公开(公告)日：2014-07-09
申请号：EP12828043.5
申请日：2012-07-27
发明人： ZHOU, Qilin , ZHU, Shoufei , YU, Yanbo , LI, Kun , WANG, Lixin
IPC分类号： C07F9/50 , C07F19/00 , B01J31/24 , C07B35/02 , C07C51/36 , C07C57/30 , C07C59/64 , C07C57/58 , C07C53/128 , C07C67/303 , C07C69/42 , C07C59/13 , C07C59/125
CPC分类号： C07F15/004 , B01J31/189 , B01J2231/645 , B01J2531/827 , C07B35/02 , C07B53/00 , C07B2200/07 , C07C51/36 , C07F9/5022 , C07F9/505 , C07F15/0033 , C07C53/128 , C07C57/30 , C07C57/58 , C07C59/125 , C07C59/13 , C07C59/64
摘要： The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 having a value as defined in claim 1. Starting from the substituted 7-trifluoromesyloxy-7'-diarylphosphino-1, 1'-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization.
摘要翻译： 本发明涉及螺苄胺 - 膦，其制备方法及其用途。 该化合物具有由式（I）表示的结构，其中n = 0至3; R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9具有如权利要求1所定义的值。从取代的7-三氟甲氧基-7'-二芳基膦基-1， 1'-螺二氢茚，该化合物以两步或三步反应合成。 新的螺苄胺 - 膦与铱前体络合并进行离子交换，得到包含各种阴离子的铱/螺苄基胺 - 膦配合物。 根据本发明的螺苄胺 - 膦/铱络合物可用于催化各种α-取代的丙烯酸的不对称氢化，具有高活性和对映选择性，并具有良好的工业化前景。
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28.发明公开
公开(公告)号：EP2275398A1
公开(公告)日：2011-01-19
申请号：EP09733969.1
申请日：2009-01-20
发明人： ZHOU, Qilin , LI, Shen , ZHU, Shoufei , ZHANG, Canming , WANG, Lixin
IPC分类号： C07C51/347 , C07C57/04 , C07F9/653 , B01J31/24
CPC分类号： C07F9/653 , B01J31/189 , B01J31/2295 , B01J2231/645 , B01J2531/827 , C07B53/00 , C07B2200/07 , C07C51/36 , C07D263/12 , C07D307/54 , C07F15/0033 , C07F17/02 , C07C57/30 , C07C59/64
摘要： The present invention relates to a preparation method of carboxylic acids with optical activity, particularly, publishes that very useful chiral carboxylic acids can be obtained by the asymmetric catalytic hydrogenation of tri-substituted α,β-unsaturated carboxylic acids, with the complexes of the chiral phosphor nitrogen ligands and iridium used as the catalysts which show high activity and enantioselectivity (up to 99.8% ee), thus provides a more efficient method with higher enantioselectivity for asymmetric catalytic hydrogenation of chiral carboxylic acid-like compounds, and has important application value to asymmetric hydrogenation of chiral carboxylic acids.
摘要翻译： 本发明涉及羧酸与光学活性的制备方法，具体地，发布并非常有用的手性羧酸可以通过三substituiertem±，²不饱和羧酸的不对称催化氢化而获得，与手性的复合物 磷 - 氮的配体和用作其显示高的活性和对映选择性（高达99.8％ee）的催化剂铱，因此提供具有用于手性羧酸类化合物的不对称催化氢化高对映选择性的更有效的方法，具有重要的应用价值 的手性羧酸的不对称氢化。
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