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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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公开(公告)号：US20170088530A1
公开(公告)日：2017-03-30
申请号：US15126890
申请日：2015-03-25
发明人： Caide TANG , Gang WANG , Boyu WANG , Luning HUANG , Eric GU
IPC分类号： C07D295/096 , C07D295/185
CPC分类号： C07D295/096 , C07D295/185 , C07D295/205
摘要： The present invention provides a new intermediate II and a method for synthesizing the same. The method comprises: (a) firstly diazotizing a compound of formula I as a raw material, and then halogenating to obtain an intermediate II; and (b) reacting the intermediate II with a compound III to obtain a compound IV, hydrolyzing the obtained compound IV directly without being separated to obtain Vortioxetine represented by compound V. The intermediate II can be used for synthesizing Vortioxetine.
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公开(公告)号：US20230037151A1
公开(公告)日：2023-02-02
申请号：US17787369
申请日：2020-12-07
发明人： Yikai ZHANG , Junzheng HUANG , Hao LU , Xiaowen GUO , Yafei JIANG , Yuanhai GAO , Luning HUANG , Anping TAO , Jianguo AN , Hong GU
IPC分类号： C07D417/08
摘要： A method for preparing lurasidone hydrochloride by reacting lurasidone free alkali reacts with hydrochloric acid in a mixed solvent of an alcoholic solvent and an alkyl halide solvent.
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公开(公告)号：US10189760B2
公开(公告)日：2019-01-29
申请号：US15319370
申请日：2015-10-09
发明人： Jian Hong , Yusheng Wang , Boyu Wang , Luning Huang , Eric Gu
IPC分类号： C07C229/00 , C07C29/153 , B01J27/18 , C07C25/13 , C07D487/04 , C07C29/151
CPC分类号： C07C29/153 , B01J27/18 , B01J2231/44 , B01J2531/004 , C07C25/13 , C07C29/1514 , C07C227/32 , C07C229/34 , C07C269/04 , C07C271/22 , C07D487/04
摘要： Disclosed is a method for synthesizing a sitagliptin intermediate, the method comprising: in the presence of hydrogen and a transition metal catalyst having a chiral phosphine ligand, subjecting a compound of formula II to an asymmetric reductive amination with ammonia or ammonium salt in a proper organic solvent under the condition of adding an acidic additive to produce a compound of formula I, wherein, an R- or S-configuration of a stereocenter is represented by *; the compound of formula I of R configuration can be used to prepare sitagliptin, and a reaction formula is as follows: R1 and R2 are each independently selected from hydrogen, C1-C12 linear or branched alkyl, C3-C12 cycloalkyl, C2-C12 alkenyl, C2-C12 alkynyl and C7-C12 arylalkyl. The method has a high yield and a high ee % value, a mild reaction condition and a low production cost, and is simple to operate, convenient to purify, environmental friendly and suitable for industrial production.
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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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6.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：US20230174478A1
公开(公告)日：2023-06-08
申请号：US17922140
申请日：2020-04-30
发明人： Yipeng ZHAN , Haisheng FAN , Kai YIN , Xiang JI , Boyang LIU , Xiaowen GUO , Luning HUANG , Anping TAO , Jianguo AN , Hong GU
IPC分类号： C07D207/27
CPC分类号： C07D207/27
摘要： Disclosed is a method for preparing a brivaracetam intermediate shown in formula B-R, comprising: reacting a compound shown in formula B-P and a resolving agent to prepare a compound shown in formula B-Q; and converting the compound shown in formula B-Q into the brivaracetam intermediate shown in formula B-R, wherein the resolving agent is a (1S,2S)-(+)-1,2-diaminocyclohexane compound. Also provided is a method for preparing brivaracetam. According to the method, a mixture of two diastereoisomers of (S)-2-3-propylpyrrolidine-1-yl butyric acid can be conveniently and effectively resolved, and the use of a chiral HPLC column is avoided, thereby greatly shortening the process time, simplifying the operation, reducing the process cost, and facilitating industrial production and enviormental protection.
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8.发明申请公开(公告)号：US20180319828A1
公开(公告)日：2018-11-08
申请号：US15772521
申请日：2016-11-02
发明人： Siyuan Li , Shaoxiao Gui , Jicheng Zhang , Luning Huang , Anping Tao , Hong Gu
IPC分类号： C07F9/6558 , C07D413/14 , C07D401/04 , B01J27/122 , B01J27/055 , B01J31/02 , B01J31/30 , B01J31/28 , B01J31/22
CPC分类号： C07F9/65583 , B01J27/055 , B01J27/122 , B01J31/0212 , B01J31/0238 , B01J31/2295 , B01J31/28 , B01J31/30 , B01J2231/44 , B01J2531/824 , C07C213/00 , C07C217/40 , C07C217/48 , C07C231/10 , C07C235/78 , C07D263/20 , C07D263/24 , C07D401/04 , C07D413/14
摘要： The present invention relates to a preparation method for a tedizolid compound in Formula I. In Formula I, R is selected from hydrogen, formula A, formula B, benzyl or benzyl substituted by a substituent, the substituent is selected from a group consisting of halogen, nitryl, C1-C6 alkyl, and C1-C6 alkoxy, and R1 is C1-C6 alkyl or C1-C6 alkyl substituted by halogen. The method comprises: generating a compound having a structure as shown in Formula C and a compound having a structure as shown in Formula D by a coupled reaction under the catalysis of a metal catalyst, a substituent of R being defined as above, where X is a leaving group, the leaving group comprising chlorine, bromine, iodine, and sulfonyl oxy such as trifluoromethane sulfonic oxy, methylsulfonyl oxy and benzenesulfonyl oxy, or benzenesulfonyl oxy substituted by one or more substituents, the substituent being selected from a group consisting of halogen, C1-C6 alkyl, and C1-C6 alkoxy.
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公开(公告)号：US20170305822A1
公开(公告)日：2017-10-26
申请号：US15319370
申请日：2015-10-09
发明人： Jian Hong , Yusheng Wang , Boyu Wang , Luning Huang , Eric Gu
IPC分类号： C07C29/153 , C07C25/13 , B01J27/18 , C07D487/04 , C07C29/151
CPC分类号： C07C29/153 , B01J27/18 , B01J2231/44 , B01J2531/004 , C07C25/13 , C07C29/1514 , C07C227/32 , C07C229/34 , C07C269/04 , C07C271/22 , C07D487/04
摘要： Disclosed is a method for synthesizing a sitagliptin intermediate, the method comprising: in the presence of hydrogen and a transition metal catalyst having a chiral phosphine ligand, subjecting a compound of formula II to an asymmetric reductive amination with ammonia or ammonium salt in a proper organic solvent under the condition of adding an acidic additive to produce a compound of formula I, wherein, an R- or S-configuration of a stereocenter is represented by *; the compound of formula I of R configuration can be used to prepare sitagliptin, and a reaction formula is as follows: R1 and R2 are each independently selected from hydrogen, C1-C12 linear or branched alkyl, C3-C12 cycloalkyl, C2-C12 alkenyl, C2-C12 alkynyl and C7-C12 arylalkyl. The method has a high yield and a high ee % value, a mild reaction condition and a low production cost, and is simple to operate, convenient to purify, environmental friendly and suitable for industrial production.
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公开(公告)号：US20190263809A1
公开(公告)日：2019-08-29
申请号：US16405722
申请日：2019-05-07
发明人： Haisheng Fan , Xiaowen Guo , Luning Huang , Hong Gu
IPC分类号： C07D471/04 , B01D9/00
摘要： Disclosed is a preparation method for a Palbociclib free base crystal form A as shown in Formula I, comprising the following steps: treating a Palbociclib free base and/or a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 35 to 100′C. to obtain a Palbociclib free base crystal form A, the water solvent being water or mixed solvent obtained by water and an organic solvent capable of being mixed and disclosed in the water. Also disclosed is a preparation method for a Palbociclib free base crystal form B, comprising the following steps: treating a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 0 to 20° C. to obtain a Palbociclib free crystal form B, the water solvent being water or a mixed solvent obtained by water and an organic solvent capable of being mixed and dissolved in the water. The method is safe and convenient in operation and low in pollution, and facilitates industrial production.
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