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公开(公告)号：US20170334836A1
公开(公告)日：2017-11-23
申请号：US15521021
申请日：2015-10-13
发明人： Shudong Wang , Xuehai You , Wenling Zhang
IPC分类号： C07C235/12 , C07C211/27 , C01D1/04
CPC分类号： C07C235/12 , C01D1/04 , C07C211/27 , C07C231/24 , C07C233/05 , Y02P20/582
摘要： The present invention provides a method for recycling 3-carbamoymethyl-5-methylhexanoic acid from 3-carbamoymethyl-5-methylhexanoic acid chiral resolving mother liquor. The method comprises the following steps: (a) distilling 3-carbamoymethyl-5-methylhexanoic acid chiral resolving mother liquor, adding aromatic hydrocarbon, heating to dissolve, keeping the temperature and stirring; (b) after completing the reaction in step (a), cooling the reaction solution to 30-60° C., then adding alkali liquor dropwise, keeping the temperature and reacting; and (c) after completing the reaction in step (b), cooling the reactant to 20-30° C., layering, adjusting the pH of the separated water layer to 1 to 2, performing extraction by using an organic solvent, distilling an organic phase under a reduced pressure, and crystallizing at 0±5° C. to obtain 3-carbamoymethyl-5-methylhexanoic acid. The method provided in the present invention is convenient to operate, and the recycled product is high in purity (≧99.8%) and yield.
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公开(公告)号：US09656958B2
公开(公告)日：2017-05-23
申请号：US14902286
申请日：2014-07-29
发明人： Boyu Wang , Jinfeng Yao , Luning Huang , Jeannie Zhang
IPC分类号： C07D211/02 , C07D211/40 , C07D211/88 , C07D211/76
CPC分类号： C07D211/88 , C07D211/02 , C07D211/40 , C07D211/76
摘要： The invention relates to a method for synthesizing an intermediate of Apixaban comprising reacting a compound of formula I with 5-chloro-valeryl chloride in the presence of inorganic base in an inert solvent to obtain a compound of formula II, with the reaction formula of (A), wherein R is selected from nitro group and the group (B). The method is mild in reaction condition, simple in operation, easy in purification, inexpensive in production cost, environmental-friendly, and suitable for industrial production.
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33.发明申请METHOD FOR PREPARING CANAGLIFLOZIN INTERMEDIATE 2-(2-METHYL-5-BROMOBENZYL)-5-(4-FLUOROPHENYL)THIOPHENE 有权中间体2-（2-甲基-5-溴甲基）-5-（4-氟代戊基）噻吩的制备方法公开(公告)号：US20170044129A1
公开(公告)日：2017-02-16
申请号：US15308456
申请日：2015-06-19
发明人： Wenjing Liao , Xiaowen Guo , Luning Huang , Eric Gu
IPC分类号： C07D333/12
CPC分类号： C07D333/12
摘要： Provide in the present invention is a method for preparing canagliflozin intermediate 2-(2-methyl-5-bromobenzyl)-5-(4-fluorobenzene)thiophene. The method comprises a compound, shown as formula (II), of (5-bromo-2-methylphenyl)[5-(p-fluorophenyl)thiophene-2-yl]ketone being reduced under the action of a directly used borane solution or borane locally produced by reacting alkali metal borohydride with a Lewis acid in a suitable solvent and at a suitable temperature, so as to obtain the compound of formula (I) of 2-(2-methyl-5-bromobenzyl)-5-(4-fluorobenzene)thiophene. The preparation method avoids the use of expensive reductive agents and guarantees the complete conversion of raw materials, wherein the post-treatment is simple, the purity of product obtained is high, the reaction yield is high, in the preparation method is simple and convenient, and can easily be used in industry.
摘要翻译： 在本发明中提供了制备canagliflozin中间体2-（2-甲基-5-溴苄基）-5-（4-氟苯）噻吩的方法。 该方法包括在直接使用的硼烷溶液的作用下还原的（5-溴-2-甲基苯基）[5-（对氟苯基）噻吩-2-基]酮的式（II）化合物，或 硼烷在局部通过碱金属硼氢化物与路易斯酸在合适的溶剂中和在合适的温度下反应，得到2-（2-甲基-5-溴苄基）-5-（4）的式（I）化合物 - 氟苯）噻吩。 制备方法避免使用昂贵的还原剂，保证原料完全转化，其中后处理简单，得到的产物纯度高，反应收率高，制备方法简单方便， 并且可以很容易地在工业中使用。
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公开(公告)号：US11845710B2
公开(公告)日：2023-12-19
申请号：US17312635
申请日：2019-12-02
发明人： Chen Liu , Xing Li , Huaxiang Ye , Jicheng Zhang , Luning Huang , Anping Tao , Jianguo An , Hong Gu
IPC分类号： C07C253/30
CPC分类号： C07C253/30
摘要： The present application relates to a method for citalopram intermediate citalopram diol. The method comprises: first mixing two Grignard reagents required for a reaction; then mixing the mixed Grignard reagents with a raw material 5-cyanophthalide in a temperature-controllable micromixer to obtain a reaction solution; then subjecting the reaction solution to the reaction by means of a reactor to obtain a citalopram diol reaction solution; and then performing operations such as quenching, concentration, extraction, acidification, and crystallization to obtain a qualified product. The citalopram diol provided in the present invention has good selectivity, high yield, high safety, safety and reliability, and little sewage discharge, and is suitable for industrial production.
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公开(公告)号：US20230348471A1
公开(公告)日：2023-11-02
申请号：US18002133
申请日：2021-06-18
发明人： Xin Xu , Jia Chen , Guan Wang , Linli Zhang , Qingyun Jiang , Chenghao Xi , Kang Sun , Xiaojuan Zhang , Chunqiao Chen , Shuai Li , Qiang Li , Liangze Xia , Ying Wang , Xiaoer Xia
IPC分类号： C07D487/04 , C07D519/00 , A61P35/00 , A61P19/02 , A61P11/00 , A61P37/06
CPC分类号： C07D487/04 , C07D519/00 , A61P35/00 , A61P19/02 , A61P11/00 , A61P37/06
摘要： A type of Bruton's tyrosine kinase inhibitor, a preparation method therefor, and an application thereof in the field of medicine. The Bruton's tyrosine kinase inhibitor may be used for preventing and/or treating a disease related to Bruton's tyrosine kinase mediation, such as an autoimmune disease, cancer, or an inflammatory disease. Through experimental research, the provided compound has high selectivity with respect to a Bruton's tyrosine kinase target, and can exhibit a uniquely advantageous medicinal effect in an in vivo animal experiment.
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36.发明授权公开(公告)号：US11707461B2
公开(公告)日：2023-07-25
申请号：US16647847
申请日：2017-09-20
发明人： Jinsheng Lin , Tianpei Huang , Feifei Lan , Xiaoyan Xu , Libin Hu , Dan Li , Wenquan Zhu , Min Li , Zhiyun Wang
IPC分类号： A61K31/4965 , A61K47/38
CPC分类号： A61K31/4965 , A61K47/38
摘要： Disclosed is N-formyl vortioxetine, and also disclosed is a method for preparing the N-formyl vortioxetine and a stable solid preparation of vortioxetine.
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公开(公告)号：US11434210B2
公开(公告)日：2022-09-06
申请号：US17259292
申请日：2018-07-17
发明人： Xiaohui Zhou , Xiaoren Zhu , Yuanxun Zhu , Peng Dong , Peng Wang , Jinsheng Lin , Wenquan Zhu , Min Li
IPC分类号： C07D257/04
摘要： A method for synthesizing valsartan, comprising the steps of: synthesizing a valsartan methyl ester intermediate to obtain a reaction mixture of the valsartan methyl ester intermediate; diluting the reaction mixture by salt water or water, and then using a first extraction solvent to extract the valsartan methyl ester intermediate; adding alkali to an organic layer containing the valsartan methyl ester intermediate for hydrolyzing, removing the organic layer, regulating pH of a water layer to be acidic by using acid, using the first extraction solvent to extract, concentrating a part of solvent, or distilling the solvent to dryness, and then adding a new solvent; finally, crystallizing, filtering, and drying to obtain the valsartan.
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公开(公告)号：US20220098178A1
公开(公告)日：2022-03-31
申请号：US17442899
申请日：2020-03-24
发明人： Xin XU , Jia CHEN , Zhen ZHANG , Liming ZHANG , Qimei WU , Qingyun JIANG , Fengying GUO , Yuyun ZHANG , Hao YU , Ying WANG , Kang SUN , Chengxu ZANG , Chenggang QIN , Xiaobo ZHOU , Xiaojuan ZHANG , Yijin WANG , Xiaoer XIA , Yunfei LI , Jian GE
IPC分类号： C07D405/14 , A61P35/00 , C07D405/12 , C07D487/04
摘要： The present invention relates to a preparation method for an amide compound and an application thereof in the field of medicine. Specifically, provided by the present invention is an amide small molecule compound which is an inhibitor of Zeste gene enhancer homolog 2 (EZH2) and which may be used to prevent and/or treat EZH2-mediated related diseases, comprising tumors, myeloproliferative diseases or autoimmune diseases.
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公开(公告)号：US20220089526A1
公开(公告)日：2022-03-24
申请号：US17420009
申请日：2019-01-02
发明人： Guoliang Tu , Jiansheng Huang , Lu Zhang , Tao Yang , Zunjun Liang
IPC分类号： C07C269/06 , B01J31/02
摘要： A synthesis method for a candesartan cilexetil intermediate represented by formula (II) is provided. The method includes (1) dissolving a compound represented by formula (IV) to an aprotic solvent to obtain a first mixed solution, and dissolving a phase transfer catalyst and an azidation reagent to water to obtain a second mixed solution; (2) dropping the first mixed solution to the second mixed solution for azidation reaction, and after the reaction is ended, standing and layering same to obtain an organic phase containing a compound represented by formula (V); (3) dropping the obtained organic phase containing the compound represented by formula (V) to tertiary butyl alcohol for rearrangement reaction, and after the reaction is ended, concentrating same to obtain a solid or oily material, then adding a crystallizing solvent to the obtained solid or oily material for recrystallization, and separating same to obtain a crystal.
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公开(公告)号：US20210300883A1
公开(公告)日：2021-09-30
申请号：US17266955
申请日：2019-08-06
发明人： Wenjing LIAO , Jianfeng GE , Jicheng ZHANG , Luning HUANG , Anping TAO , Eric GU
IPC分类号： C07D295/135
摘要： The present application relates to a synthesis method for cariprazine, comprising performing an acylation reaction between a compound represented by formula (I) and dimethylcarbamoyl chloride in a reaction solvent in the presence of an aqueous solution of an inorganic base, so as to obtain the cariprazine compound represented by formula (II). The synthesis method overcomes defects in the prior art such as a long reaction time, large size impurities and the difficulty of purification, and provides a new method suitable for commercial production wherein the reaction is fast, impurity sizes are small, the product is easily purified, the purity of the product can reach 99.0% or more, and the yield is high.
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