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公开(公告)号:US12084402B2
公开(公告)日:2024-09-10
申请号:US17611712
申请日:2019-05-21
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD.
Inventor: Hao Hong , Jiangping Lu , Enxuan Zhang , Wei Shen , Honglei Yan , Zhen Zhang
IPC: C07C245/16
CPC classification number: C07C245/16
Abstract: Provided is a preparation process of diazomethane. The preparation process includes: step S1, taking N-methylurea as a raw material to continuously prepare, in a continuous reactor, a first product system containing N-methyl-N-nitrosourea: step S2, performing continuous extraction and continuous back-extraction on the first product system to obtain an N-methyl-N-nitrosourea solution; step S3, enabling the N-methyl-N-nitrosourea solution to continuously react with an alkaline solution in a continuous reactor to obtain a second product system containing the diazomethane; and step S4, performing continuously liquid separation, water freezing and removal on the second product system, to obtain the diazomethane.
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公开(公告)号:US20230227797A1
公开(公告)日:2023-07-20
申请号:US17769204
申请日:2019-10-28
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD.
Inventor: Hao HONG , Gage JAMES , Yi XIAO , Yulei MA , Na ZHANG , Xuecheng JIAO , Huiyan MU , Yibing CHENG , Shan CAO
CPC classification number: C12N9/1096 , C12P13/001
Abstract: Provided are a transaminase mutant and use thereof. The transaminase mutant has an amino acid sequence obtained by mutation of an amino acid sequence shown in SEQ ID NO:1, the mutation at least includes one of the following mutation site combinations: T7C+S47C, Q78C+A330C, V137C+G313C, A217C+Y252C and L295C+C328C; or the transaminase mutant has an amino acid sequence which has the mutation sites in the mutated amino acid sequence and has 80% or more identity with the mutated amino acid sequence. The transaminase mutant realizes the change of protein structure and functions, reduces the enzyme amount, increases the enantiomeric excess (ee) value of a product, and reduces the difficulty of post-processing, so that the transaminase mutant may be suitable for industrial production.
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公开(公告)号:US20230151396A1
公开(公告)日:2023-05-18
申请号:US17905092
申请日:2020-03-31
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD.
Inventor: Hao HONG , Gage JAMES , Yi XIAO , Na ZHANG , Xiang LI , Xiangjun JIANG , Tong ZHAO
CPC classification number: C12P13/001 , C12P17/04 , C12P17/12 , C12Y206/01
Abstract: Provided is a method for synthesizing a chiral diamine compound. The synthesizing method includes: converting a substrate represented by Formula I into a chiral diamine compound in Formula I by using a transaminase, herein n=1˜10, an R group represents an alkyl, a cycloalkyl, a heteroatom-containing alkyl, a heteroatom-containing cycloalkyl, a heteroatom-containing aryl, an amide compound residue, or an ether compound residue, and a hetero atom is at least one from among O, S and N; R1 and R2 are the same or not the same, the R1 and R2 are respectively and independently hydrogen, a C1-C3 alkyl, or an amino protecting group; and the transaminases are derived from a plurality of strains.
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公开(公告)号:US20220242805A1
公开(公告)日:2022-08-04
申请号:US17622294
申请日:2019-07-02
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD.
Inventor: Hao HONG , Jiangping LU , Xichun FENG , Xingfang SUN , Feng ZHANG
Abstract: The present disclosure discloses a method and a device for continuously synthesizing cyclopropane compounds. The method includes the following steps: continuously performing a synthetic reaction of a diazomethane precursor in a first reactor, the reaction product of the first reactor flowing into a separator for stratification, the organic phase obtained by stratification overflowing into a second reactor, continuously consuming the diazomethane precursor in a second reactor to prepare diazomethane and performing an electron-rich monoolefin cyclopropanation reaction in situ so as to obtain the cyclopropane compound. The technical solution of the present disclosure may be applied to achieve automatic control, decrease the transfer of high-risk materials, and prevent the risk of pipeline transfer of diazomethane solution, and effectively improve production safety. Moreover, the present disclosure provides a simple device to save equipment investment, and may safely and quantitatively achieve the production of diazomethane and the cyclopropanation reaction of olefins simultaneously.
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公开(公告)号:US20200055807A1
公开(公告)日:2020-02-20
申请号:US16609237
申请日:2017-05-08
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD
Inventor: Jiangping LU , Qinglan PEI , Jinquan YU , Enxuan ZHANG
IPC: C07C67/20
Abstract: Provided is a method for the alcoholysis of an amide. The method comprises subjecting an amide-containing compound to alcoholysis under alkaline conditions using an epoxy compound as an accelerant of alcoholysis.
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公开(公告)号:US09926283B2
公开(公告)日:2018-03-27
申请号:US15124083
申请日:2014-03-07
Applicant: Asymchem Laboratories (Tianjin) Co., Ltd. , Asymchem Life Science (Tianjin) Co., Ltd. , Tianjin Asymchem Pharmaceutical Co., Ltd. , Asymchem Laboratories (Fuxin) Co., Ltd. , Jilin Asymchem Laboratories Co., Ltd.
Inventor: Hao Hong , James Gage , Jiuyuan Li , Litao Shen , Lei Zhang , Changming Dong
IPC: C07D239/42 , C07F9/6512
CPC classification number: C07D239/42 , C07B2200/13 , C07F9/6512 , Y02P20/55
Abstract: Provided are an intermediate compound for preparing rosuvastatin calcium and a preparation method of the rosuvastatin calcium. The method comprises: using the foregoing intermediate compound as a raw material, and subjecting the raw material to a step of Wittig reaction, a step of protecting group removal and hydrolysis and a step of calcium salt formation, so as to obtain the rosuvastatin calcium. The product, which is prepared from the intermediate compound, can be substantially enhanced in stereoselectivity and also notably improved in purity and yield; in addition, the method for preparing rosuvastatin calcium from the intermediate compound is simple, convenient and low in cost.
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7.
公开(公告)号:US20150119573A1
公开(公告)日:2015-04-30
申请号:US14394079
申请日:2012-12-27
Applicant: ASYMCHEM LABORATORIES (TIANJIN)CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD. , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO. LTD.
Inventor: Hao Hong , James Gage , Chaoyong Chen , Jiangping Lu , Yan Zhou , Shuangyong Liu
IPC: C07D475/04 , C07D317/32 , C07D317/26 , C07C221/00 , C07D239/50 , C07C209/62 , C07D317/28 , C07D303/48 , C07C225/06
CPC classification number: C07D475/04 , C07C209/62 , C07C221/00 , C07C225/06 , C07D239/50 , C07D303/48 , C07D317/26 , C07D317/28 , C07D317/32
Abstract: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
Abstract translation: 披露了一种合成沙rop in二盐酸盐的方法。 本公开内容减少了沙棘蛋白二盐酸盐的合成途径,并且通过使用手性拆分试剂拆分外消旋体中间体或具有低antimer异构值的中间体,从而获得具有高antimer异构值的中间体。 原材料便宜,易于获得,成本显着降低,为大规模工业生产四氢叶酸二盐酸盐提供了有效的方案。
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8.
公开(公告)号:US20240182884A1
公开(公告)日:2024-06-06
申请号:US18551160
申请日:2021-04-12
Applicant: Asymchem Laboratories (Tianjin) Co., Ltd.
Inventor: Hao HONG , Yi XIAO , Na ZHANG , Han LIN , Pong PAN , Williams VYASA , Liteng MA , Yuxia CUI , Yanyan GAO
IPC: C12N11/084 , C12N9/02 , C12N9/04 , C12N9/06 , C12N9/10
CPC classification number: C12N11/084 , C12N9/0006 , C12N9/0016 , C12N9/0073 , C12N9/1096 , C12Y101/01 , C12Y104/01009 , C12Y114/13022 , C12Y206/01
Abstract: The application provides an enzyme immobilization carrier and a preparation method thereof, an immobilized enzyme and a preparation method thereof. The above enzyme immobilization carrier is obtained by an amino modification or a cyanuric chloride modification of super-crosslinked polyvinyl alcohol. The use of the enzyme immobilization carrier provided by the application may effectively improve the stability and reusability of the immobilized enzyme. Moreover, due to the use of the form of enzyme covalent linkage, compared with an embedding method, the preparation method is no need for chemical reagent immersion and the like, it is beneficial to maintain the own activity of the enzyme, and promote the immobilized enzyme to have the better activity while the stability and reusability are kept.
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公开(公告)号:US20240117395A1
公开(公告)日:2024-04-11
申请号:US18275833
申请日:2021-07-06
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD
Inventor: Hao Hong , Gage James , Yi Xiao , Na Zhang , Xuecheng Jiao , Yulei Ma , Huiyan Mou , Zujian Wang , Kaihua Sun , Ru Jia , Fang Liu , Wenjing Liu
CPC classification number: C12P17/14 , C12N9/1096 , C12P13/001 , C12P17/12 , C12Y206/01
Abstract: Provided is a method for synthesizing a chiral amine compound. A transaminase is used to transaminate a ketone substrate under the action of an amino donor, to obtain the chiral amine compound; and the conserved amino acid sequence region of the transaminase at least includes a region 1 (MAGLWCVN) and a region 2 (YNTFFKT). With the transaminase with the specific conserved amino acid sequence region to synthesize a large sterically hindered chiral amine, the enzyme catalytic reaction volume is small, the synthesizing route is short, the product yield is high, a high-cost noble metal is not required for catalysis under the synthesizing conditions, three wastes are reduced, and the production cost is saved.
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公开(公告)号:US20230235300A1
公开(公告)日:2023-07-27
申请号:US17997419
申请日:2020-05-29
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD.
Inventor: Hao HONG , Gage JAMES , Yi XIAO , Na ZHANG , Xuecheng JIAO , Yulei MA , Huiyan MU , Shan CAO
CPC classification number: C12N9/1096 , C12N15/52 , C12N15/70 , C12P13/001 , C12Y206/01
Abstract: Provided are a transaminase mutant and an application thereof. Compared with an amino acid sequence shown in SEQ ID NO:1, an amino acid sequence of the transaminase mutant includes at least one of the following mutation sites: L166, K149, K146, A168, H73, F133, H82, E24, V194, T294, A295, G235 and F236. The mutant of the present invention has the improved catalytic activity for a transammonization reaction of ketone substrates, and is suitable for industrial production of chiral amines.
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