公开(公告)号：US12030854B2

公开(公告)日：2024-07-09

申请号：US17296542

申请日：2020-07-21

申请人： SOOCHOW UNIVERSITY

发明人： Xiaobing Wan ,  Pengcheng Lian ,  Wenhao Long ,  Jingjing Li ,  Yonggao Zheng

IPC分类号： C07D209/48 ,  C07B39/00 ,  C07C67/287 ,  C07C201/12 ,  C07C253/30 ,  C07C303/40 ,  C07C315/04

CPC分类号： C07D209/48 ,  C07B39/00 ,  C07C67/287 ,  C07C201/12 ,  C07C253/30 ,  C07C303/40 ,  C07C315/04

摘要： The invention provides a method for producing a dichloro addition product of an aliphatic olefin by photocatalysis under visible light. The method includes reacting an aliphatic olefin as a substrate with hydrochloric acid as a chlorine source in an organic solvent under visible light irradiation in the presence of copper chloride with visible light absorption ability as a catalyst, to obtain the dichloro addition product of the aliphatic olefin, wherein the reaction is carried out under an oxygen-containing atmosphere, the aliphatic olefin comprises a carbon-carbon double bond and a C9-C15 aliphatic chain connected to the carbon-carbon double bond by a covalent bond. In the invention, visible light is used to provide the energy and a transition metal chloride with visible light absorption ability is used to undergo light-induced electron transfer from chloride with a reaction substrate, thereby initiating an addition reaction to obtain a dichloro addition product.

公开(公告)号：US11707538B2

公开(公告)日：2023-07-25

申请号：US17150186

申请日：2021-01-15

申请人： Dong Zhou

发明人： Dong Zhou

IPC分类号： A61K49/04 ,  C07C315/04 ,  C07C315/06 ,  C07C311/48 ,  C07D487/06 ,  C07D401/12 ,  C07H3/08 ,  C07C67/317 ,  C07C67/307 ,  C07B39/00 ,  C07B59/00 ,  B01J23/92 ,  B01J27/232 ,  B01J31/02

CPC分类号： A61K49/0433 ,  B01J23/92 ,  B01J27/232 ,  B01J31/0237 ,  C07B39/00 ,  C07B59/001 ,  C07C67/307 ,  C07C67/317 ,  C07C311/48 ,  C07C315/04 ,  C07C315/06 ,  C07D401/12 ,  C07D487/06 ,  C07H3/08 ,  C07B2200/05 ,  C07C2602/10

摘要： Described herein are methods and devices that allow the generation of [F-18]triflyl fluoride and other [F-18] sulfonyl fluorides (such as [F-18]tosyl fluoride) in a manner that is suitable for radiosynthesis of F-18 labeled radiopharmaceuticals using currently available synthesis modules.

公开(公告)号：US20210276959A1

公开(公告)日：2021-09-09

申请号：US17323337

申请日：2021-05-18

申请人： BASF SE

发明人： Eric George Klauber ,  Michael Rack ,  Roland Goetz ,  Sebastian Soergel

IPC分类号： C07D237/20 ,  C07D401/12 ,  C07B31/00 ,  C07B39/00 ,  C07B43/04 ,  C07D237/12 ,  C07D403/12

摘要： Provided herein is a process for preparing a pyridazine amine compound of formula V, and a process for preparing dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof. Further, provided herein are dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof, wherein the amino group is an ethylamino group.

公开(公告)号：US10899760B2

公开(公告)日：2021-01-26

申请号：US16745418

申请日：2020-01-17

申请人： Principia Biopharma, Inc.

发明人： Jiang Zhu ,  Mohammad Masjedizadeh

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07B35/02 ,  C07B35/06 ,  C07B39/00 ,  C07B43/04 ,  C07B43/06 ,  C07B45/04

摘要： Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.

公开(公告)号：US10851060B2

公开(公告)日：2020-12-01

申请号：US16221600

申请日：2018-12-17

申请人： Zhejiang Avilive Chemical Co., Ltd.

发明人： Huiyue Li ,  Keqiang Jin ,  Jiaquan Zhu

IPC分类号： C07D213/04 ,  C07D213/61 ,  B01D3/14 ,  B01J19/12 ,  C07B39/00

摘要： The present invention relates to a method for preparing 2,6-dichloropyridine with product purity greater than or equal to 99.0% by using trifluoromethyl chlorobenzene as a solvent for reaction between pyridine and chlorine gas. The preparation process comprises the following steps: enabling pyridine and chlorine gas to continuously experience chlorination reaction under irradiation of ultraviolet light by using pyridine and chlorine gas as starting materials and using trifluoromethyl chlorobenzene as a solvent, and cooling a chlorination reaction product and the solvent to obtain pyridine chlorination solution. Advantages: firstly, it pioneers the precedent of direct and high-selectivity preparation of 2,6-dichloropyridine through liquid phase photochlorination, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be obtained, but also industrial production is facilitated; and secondly, not only can the reuse of the separated solvent in the preparation process of the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be realized, but also the purposes of low pollution, low energy consumption and low cost in the preparation process can be realized.

公开(公告)号：US10702858B2

公开(公告)日：2020-07-07

申请号：US16214793

申请日：2018-12-10

申请人： UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.

发明人： Bo Xu ,  Zhichao Lu ,  Gerald B. Hammond

IPC分类号： B01J27/055 ,  C07D277/56 ,  C07C67/287 ,  C07C303/30 ,  C07D209/50 ,  C07C303/34 ,  C07C201/12 ,  C07C213/08 ,  C07C253/30 ,  C07C45/63 ,  C07D215/227 ,  C07D307/68 ,  C07D333/38 ,  C07D207/34 ,  C01D5/00 ,  C07C17/087 ,  C07C67/307 ,  C07C51/363 ,  C07B39/00 ,  C07C29/62 ,  B01J31/00

摘要： Some embodiments of the invention include inventive catalysts (e.g., compounds of Formula (I) or (Ia)). Other embodiments include compositions comprising the inventive catalysts. Some embodiments include methods of using the inventive catalysts (e.g., in hydrofluorination of an organic compound). Further embodiments include methods for making the inventive catalysts. Additional embodiments of the invention are also discussed herein.

公开(公告)号：US10689314B2

公开(公告)日：2020-06-23

申请号：US15568017

申请日：2016-04-18

申请人： Univation Technologies, LLC

发明人： Catherine Anne Faler ,  Kevin P. Ramirez

IPC分类号： C07C15/14 ,  C07C41/01 ,  C07F5/02 ,  C07C41/30 ,  C07F7/00 ,  C07B39/00 ,  C07B51/00 ,  C07C15/20 ,  C07C43/23

摘要： New methods for preparing bridged bi-aromatic ligands are disclosed. The methods employ aryl coupling of unprotected phenols. The ligands may be used to prepare transition metal compounds useful as catalysts in olefin polymerization.

公开(公告)号：US10584102B2

公开(公告)日：2020-03-10

申请号：US15572303

申请日：2016-05-10

申请人： BASF SE

发明人： Eric George Klauber ,  Michael Rack ,  Roland Goetz ,  Sebastian Soergel

IPC分类号： C07D403/12 ,  C07D237/12 ,  C07D237/20 ,  C07B31/00 ,  C07B39/00 ,  C07B43/04

摘要： Provided herein is a process for preparing a pyridazine amine compound of formula V, and a process for preparing dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof. Further, provided herein are novel dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof, wherein the amino group is an ethylamino group.

公开(公告)号：US10577326B1

公开(公告)日：2020-03-03

申请号：US16221603

申请日：2018-12-17

申请人： Zhejiang Avilive Chemical Co., Ltd.

发明人： Huiyue Li ,  Keqiang Jin ,  Jiaquan Zhu

IPC分类号： C07D213/61 ,  C07B39/00 ,  B01D3/14 ,  B01J19/12

摘要： The present invention relates to a method for preparing 2-chloro-6-trichloromethylpyridine with product purity greater than or equal to 99.0% by using trifluoromethyl chlorobenzene as a solvent for reaction between 2-methylpyridine with chlorine gas, in which 2-methylpyridine and chlorine gas are used as starting materials, trifluoromethyl chlorobenzene is used as a solvent, 2-methylpyridine is prepared into a liquid raw material by using the solvent trifluoromethyl chlorobenzene, and the liquid raw material is continuously fed to perform liquid phase photochlorination reaction at temperature of 160-240° C. under irradiation of ultraviolet light to obtain 2-chloro-6-trichloromethylpyridine solution. Advantages: the selectivity of reaction for the production of 2-chloro-6-trichloromethylpyridine is improved, the content of components such as isomers and pentachloromethylpyridine in the crude product is decreased significantly, the crude product is easy to be purified to obtain the 2-chloro-6-trichloromethylpyridine product with purity greater than or equal to 99.0%, and the industrial production is facilitated; and secondly, not only can the reuse of the separated solvent in the preparation process of the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be realized, but also the purposes of low pollution, low energy consumption and low cost in the preparation process are realized.

公开(公告)号：US10538518B2

公开(公告)日：2020-01-21

申请号：US15748212

申请日：2016-08-10

申请人： Principia Biopharma, Inc.

发明人： Jiang Zhu ,  Mohammad Masjedizadeh

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07B35/02 ,  C07B35/06 ,  C07B39/00 ,  C07B43/04 ,  C07B43/06 ,  C07B45/04

摘要： To an appropriate reactor equipped with mechanical stirrer was charged acetic acid (12 L), tert-butyl 4-(3-(6-(3,5-dimethoxyphenyl)-2-(methylthio)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl)propyl)piperazine-1-carboxylate (2000 g) and triethylamine (639 g, 2.3 eq.). Internal temperature was adjusted to approximately 20° C. and N-chlorosuccinimide (1651 g, 4.5 eq.) was added at 20-30° C. Reaction was stirred for 2 hours. Ethyl acetate (30 L) was added. 5% aqueous NaCl solution (20 L) was added. The organic layer was separated and the aqueous layer was extracted with EtOAc. The combined organic layers were washed with 30% aqueous potassium carbonate solution (14 L). The organic layer was concentrated to ˜12 L and used for next step directly.