公开(公告)号：US20220306572A1

公开(公告)日：2022-09-29

申请号：US17596494

申请日：2021-03-09

申请人： KONISHI CHEMICAL IND. CO., LTD.

发明人： Norihito IIDA

IPC分类号： C07C315/04

摘要： A diphenylsulfone compound containing 4,4′-dihydroxydiphenylsulfone is produced in good yield in a short time and at a relatively low temperature. A diphenylsulfone compound represented by formula (2) below is produced by irradiating, with microwaves, a compound represented by formula (1) below and a sulfonating agent so that a dehydration condensation reaction is carried out.

公开(公告)号：US11332442B2

公开(公告)日：2022-05-17

申请号：US16991357

申请日：2020-08-12

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： William P. Gallagher ,  John Ryan Coombs ,  Carlos A. Guerrero ,  David Marcoux ,  Qing Shi ,  Candice Lee Joe ,  Sanjeewa Rupasinghe ,  Jason J. Zhu ,  Srinivas Kalidindi ,  Sathasivam Shunmugaraj ,  Moorthy Kandasamy ,  Siva Sankar Bondigela ,  Rajappa Vaidyanathan ,  Shankar Tulsidas Tendulkar ,  Sankar Kuppusamy ,  Francisco González-Bobes

IPC分类号： C07D209/60 ,  C07C315/04 ,  C07C303/40 ,  C07C311/03 ,  C07C317/24

摘要： The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties.

公开(公告)号：US20220081407A1

公开(公告)日：2022-03-17

申请号：US17017864

申请日：2020-09-11

申请人： Peloton Therapeutics, Inc.

发明人： Peter J. Stengel ,  Rui Xu ,  Stacey Renee Spencer

IPC分类号： C07D317/72 ,  C07C319/20 ,  C07C315/04

摘要： This application discloses methods for the synthesis of substituted indane analogs that modulate HIF-2α activity, as well as key intermediates produced thereby. The synthesis of 3-(((1S,2S,3R)-2,3-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile was exemplified.

公开(公告)号：US20220002241A1

公开(公告)日：2022-01-06

申请号：US17290889

申请日：2019-11-04

申请人： Kemira Oyj

发明人： Jaakko HILTUNEN ,  Petteri SUOMINEN ,  Ivan OGIBALOV ,  Ain UUSTARE

IPC分类号： C07C315/04 ,  C07C317/32

摘要： The present invention relates to a process for the preparation of arylsulfonylpro-penenitriles. The reaction starting from arylsulfonyl halides is catalyzed by a cat-alyst compound comprising a transition metal. The process is scalable, environ-mentally benign and provides the product in good yield.

公开(公告)号：US11008315B2

公开(公告)日：2021-05-18

申请号：US16493614

申请日：2018-03-13

申请人： Assembly Biosciences, Inc.

发明人： Leping Li ,  Lee D. Arnold ,  Sreenivasa Reddy Mundla

IPC分类号： C07D417/12 ,  C07C231/10 ,  C07C231/12 ,  C07C315/02 ,  C07C315/04 ,  C07C319/14 ,  C07C319/20

摘要： The present disclosure provides, in part, a process for preparing compounds (I) having allosteric effector properties against Hepatitis B virus Cp.

公开(公告)号：US20200347014A1

公开(公告)日：2020-11-05

申请号：US16643083

申请日：2018-08-30

申请人： ARKEMA FRANCE

发明人： Jean-Alex LAFFITTE ,  Bernard MONGUILLON

IPC分类号： C07C317/04 ,  C07C315/04

摘要： The subject of the present invention is a process for producing a sulfonic acid which is sparingly corrosive, or even non-corrosive, with respect to stainless steels, said process comprising at least the steps of adding at least one nitrite to a sulfonic acid, curing, with stirring, with sparging of the mixture and recovering the low-corrosion sulfonic acid obtained.The invention also relates to the low-corrosion sulfonic acid obtained according to the process of the invention, and also to the use thereof as low-corrosion sulfonic acid.

公开(公告)号：US10697977B2

公开(公告)日：2020-06-30

申请号：US15613065

申请日：2017-06-02

申请人： The Regents of The University of California

发明人： Lan Huang ,  Scott D. Rychnovsky ,  Clinton Yu ,  Eric James Novitsky ,  Craig Bryant Gutierrez

IPC分类号： C07C317/44 ,  G01N33/68 ,  C07C315/04 ,  B01D15/34 ,  G01N30/88

摘要： Provided herein is synthesis of a novel acidic acid residue targeting sulfoxide-containing MS-cleavable homobifunctional cross-linker. The novel mass spectrometry-cleavable cross-linking agents can be used in mass spectrometry to facilitate structural analysis of intra-protein interactions in proteins and inter-protein interactions in protein complexes. Also disclosed herein are data based on the novel MS-cleavable homobifunctional cross-linker that are complimentary to amine-reactive sulfoxide-containing MS-cleavable reagents.

公开(公告)号：US10385000B2

公开(公告)日：2019-08-20

申请号：US16061880

申请日：2017-04-25

申请人： CHEN-STONE (GUANGZHOU) CO., LTD.

发明人： Yingjie Lai ,  Xuyan Wang

IPC分类号： C07C51/09 ,  C07C61/15 ,  C07C51/377 ,  C07C315/04 ,  C07C317/22

摘要： Disclosed is a new method for synthesizing 2-fluorocyclopropanecarboxylic acid comprising: 1) performing reaction of 1,1-dichloro-1-fluoroethane with thiophenol in the presence of an alkali, to produce a phenyl sulfide intermediate; 2) performing oxidation reaction of the phenyl sulfide intermediate with Oxone; 3) performing elimination reaction of the product of Step 2) in the presence of an alkali, to obtain 1-fluoro-1-benzenesulfonyl ethylene; 4) performing addition reaction of the 1-fluoro-benzenesulfonyl ethylene with ethyl diazoacetate in the presence of a catalyst, to obtain a cyclopropane intermediate; 5) performing elimination reaction of the cyclopropane intermediate in the presence of an alkali before acidification, to obtain 2-fluorocyclopropanecarboxylic acid. Herein, the synthetic route is short, used materials are bulk commodities, and raw materials are inexpensive and readily available. The process can be safely scaled up by replacing commonly used mCPBA reagents with Oxone. Further, reaction yield is improved, production cost is greatly reduced, and operation is simplified.

公开(公告)号：US10377703B2

公开(公告)日：2019-08-13

申请号：US15737492

申请日：2016-07-19

申请人： SUMITOMO CHEMICAL COMPANY, LIMITED

发明人： Yuta Honda ,  Yohei Tanaka ,  Kazuya Ueki

IPC分类号： C07C315/02 ,  C07C315/04 ,  C07C317/22 ,  C07C317/36 ,  C07C209/36 ,  C07C201/08 ,  C07C53/128

摘要： A compound represented by formula (4): can be produced by adding a heterogeneous transition metal catalyst to a solution containing a compound represented by formula (3): obtained by performing a nitration reaction by adding a nitrating agent to a solution containing a compound represented by formula (2): obtained by oxidizing a compound represented by formula (1): with hydrogen peroxide in the presence of sodium tungstate and a saturated C8 carboxylic acid, then adding water to the resultant mixture, and separating the resultant solution.

公开(公告)号：US10364208B2

公开(公告)日：2019-07-30

申请号：US15861020

申请日：2018-01-03

申请人： The Governors of the University of Alberta

发明人： Rylan Lundgren ,  Patrick Moon

IPC分类号： C07C67/32 ,  C07C69/614 ,  C07C69/38 ,  C07F5/02 ,  C07C67/343 ,  C07C303/40 ,  C07C201/12 ,  C07C315/04 ,  C07C231/12 ,  C07D295/185 ,  C07D213/55 ,  C07D213/61 ,  C07D213/64 ,  C07D307/91 ,  C07F7/08 ,  C07F9/40

摘要： Described herein are methods of oxidative coupling of aryl boron reagents with sp3-carbon nucleophiles, and ambient decarboxylative arylation of malonate half-esters via oxidative catalysis.