公开(公告)号：US09975844B2

公开(公告)日：2018-05-22

申请号：US15300018

申请日：2015-04-08

Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED

Inventor： Teruki Takahashi ,  Kazuya Ueki ,  Yuta Nagashima

IPC: C07C201/12 ,  C07C209/68

CPC classification number: C07C201/12 ,  C07C209/68 ,  C07C205/11

Abstract: A compound represented by formula (1): (wherein, R1a represents an alkyl group having 1 to 6 carbon atoms or the like, R1b and R1c represent a hydrogen atom or the like, and X represents a chlorine atom, a bromine atom or an iodine atom) can be produced by: a step wherein a compound represented by formula (2): is reacted with a compound represented by formula (3): (wherein, each of R2 and R3 independently represents an alkyl group having 1 to 3 carbon atoms or the like, and each of R6 and R7 independently represents an alkoxy group having 1 to 3 carbon atoms or the like), thereby obtaining a compound represented by formula (4): a step wherein a compound represented by formula (4) is oxidized; a step wherein the product in the oxidation step is reduced; and a step wherein the product in the reduction reaction is halogenated.

公开(公告)号：US09895454B2

公开(公告)日：2018-02-20

申请号：US15323046

申请日：2015-07-02

Applicant: The Regents of the University of California

Inventor： Maxim Sergeev ,  Federica Morgia ,  Robert Michael Van Dam ,  Mark Lazari

IPC: A61K51/04 ,  C07B59/00 ,  C07D207/09 ,  C07C17/361 ,  C07H19/052 ,  C07D207/16 ,  C07D405/06 ,  C07C67/333 ,  C07C201/12 ,  C07C253/30 ,  C07D217/22 ,  C07D241/16 ,  C07D213/61 ,  B01J21/06

CPC classification number: A61K51/04 ,  A61K51/0446 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0491 ,  B01J21/063 ,  C07B59/00 ,  C07B59/001 ,  C07B59/002 ,  C07B59/005 ,  C07B2200/05 ,  C07C17/361 ,  C07C67/307 ,  C07C67/333 ,  C07C201/12 ,  C07C253/30 ,  C07C2601/14 ,  C07D207/09 ,  C07D207/16 ,  C07D213/61 ,  C07D215/18 ,  C07D217/22 ,  C07D241/16 ,  C07D405/04 ,  C07D405/06 ,  C07H19/052 ,  C07C69/76 ,  C07C205/12 ,  C07C255/50 ,  C07C25/13 ,  C07C22/08 ,  C07C25/22 ,  C07C19/08 ,  C07C23/10

Abstract: Inter alia, the first titania-catalyzed [18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.

公开(公告)号：US09890177B2

公开(公告)日：2018-02-13

申请号：US14920156

申请日：2015-10-22

Applicant: ANGUS Chemical Company

Inventor： Daniel M. Trauth ,  George D. Green ,  Raymond J. Swedo ,  Richard L. James ,  Ian A. Tomlinson

IPC: C07D498/10 ,  A01N43/76 ,  A01N43/90 ,  C07C201/08 ,  C07C201/12 ,  C07C205/02 ,  C07C205/06 ,  C07C205/18 ,  C07C215/08 ,  C07C215/42 ,  C07C239/10 ,  C07D263/04 ,  C07D263/52 ,  C07D498/04 ,  C08G18/32 ,  C07C205/04 ,  C07C205/05 ,  C07C205/15 ,  C07C205/16 ,  C07C215/20 ,  C07C215/28

CPC classification number: C07D498/10 ,  A01N43/76 ,  A01N43/90 ,  C07C201/08 ,  C07C201/12 ,  C07C205/02 ,  C07C205/04 ,  C07C205/05 ,  C07C205/06 ,  C07C205/15 ,  C07C205/16 ,  C07C205/18 ,  C07C215/08 ,  C07C215/20 ,  C07C215/28 ,  C07C215/42 ,  C07C239/10 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/10 ,  C07D263/04 ,  C07D263/52 ,  C07D498/04 ,  C08G18/3271 ,  Y02P20/582

Abstract: Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications.

公开(公告)号：US09856282B2

公开(公告)日：2018-01-02

申请号：US15183490

申请日：2016-06-15

Applicant: Kanto Kagaku Kabushiki Kaisha

Inventor： Ryohei Yamaguchi ,  Ken-ichi Fujita

IPC: C07F17/02 ,  C07C45/00 ,  C07C201/12 ,  B01J7/02 ,  C07C51/16 ,  B01J31/22 ,  C01B3/06 ,  C01B3/32 ,  C01B3/00 ,  C01B3/22 ,  C07B41/06 ,  C07B41/08 ,  C07J13/00

CPC classification number: C07F17/02 ,  B01J7/02 ,  B01J31/2295 ,  B01J2231/763 ,  B01J2231/766 ,  B01J2531/827 ,  C01B3/0015 ,  C01B3/06 ,  C01B3/22 ,  C01B3/326 ,  C01B2203/02 ,  C01B2203/0227 ,  C01B2203/0277 ,  C01B2203/1041 ,  C01B2203/1064 ,  C01B2203/1205 ,  C01B2203/1211 ,  C01B2203/1217 ,  C01B2203/1223 ,  C01B2203/1229 ,  C07B41/06 ,  C07B41/08 ,  C07C45/002 ,  C07C51/16 ,  C07C201/12 ,  C07C2601/08 ,  C07C2601/14 ,  C07J13/007 ,  Y02E60/328 ,  Y02E60/36 ,  Y02P20/132 ,  C07C47/02 ,  C07C47/06 ,  C07C47/32 ,  C07C47/52 ,  C07C49/04 ,  C07C49/213 ,  C07C49/395 ,  C07C49/403

Abstract: Objects of the present invention are to provide a novel dehydrogenation reaction catalyst, to provide a method that can produce a ketone, an aldehyde, and a carboxylic acid with high efficiency from an alcohol, and to provide a method for efficiently producing hydrogen from an alcohol, formic acid, or a formate, and they are accomplished by a catalyst containing an organometallic compound of Formula (1).

公开(公告)号：US20170369417A1

公开(公告)日：2017-12-28

申请号：US15694982

申请日：2017-09-04

Applicant: Emory University

Inventor： Huw M. L. Davies ,  Spandan Chennamadhavuni ,  Andrei Bakin

IPC: C07C69/73 ,  A61K31/194 ,  C07D317/60 ,  C07D307/80 ,  C07D307/79 ,  C07D209/34 ,  C07D209/26 ,  C07D209/24 ,  C07C259/06 ,  C07C205/56 ,  C07C201/12 ,  C07C69/738 ,  C07C69/736 ,  C07C69/734 ,  C07C69/732 ,  C07C69/65 ,  C07C69/618 ,  C07C69/604 ,  C07C67/31 ,  C07C57/42 ,  C07C51/00 ,  A61K31/405 ,  A61K31/36 ,  A61K31/357 ,  A61K31/343 ,  A61K31/216 ,  C07D317/68 ,  C07D319/18

CPC classification number: C07C69/73 ,  A61K31/194 ,  A61K31/216 ,  A61K31/343 ,  A61K31/357 ,  A61K31/36 ,  A61K31/405 ,  C07C51/00 ,  C07C57/42 ,  C07C67/31 ,  C07C69/604 ,  C07C69/618 ,  C07C69/65 ,  C07C69/732 ,  C07C69/734 ,  C07C69/736 ,  C07C69/738 ,  C07C201/12 ,  C07C205/56 ,  C07C259/06 ,  C07D209/24 ,  C07D209/26 ,  C07D209/34 ,  C07D307/79 ,  C07D307/80 ,  C07D317/60 ,  C07D317/68 ,  C07D319/18

Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I, pharmaceutical compositions having a compound of formula I, and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula I to a subject in need thereof.

公开(公告)号：US20170326520A1

公开(公告)日：2017-11-16

申请号：US15533839

申请日：2015-12-09

Applicant: Lonza Ltd

Inventor： Dominique ROBERGE ,  Patrick PLOUFFE ,  Arturo MACCHI

IPC: B01J10/00 ,  C07C51/41 ,  B01F5/06 ,  B01F13/00 ,  C07C201/12 ,  B01J19/02

CPC classification number: B01J10/00 ,  B01F5/064 ,  B01F5/0647 ,  B01F13/0059 ,  B01J19/02 ,  B01J2219/0277 ,  B01L3/502746 ,  B01L2400/086 ,  C07C51/412 ,  C07C201/12

Abstract: A fluid mixing structure (10) for mixing at least two fluidic components has a flow inlet port and a flow outlet port and comprises a contraction zone (12), an expansion zone (14), and a retention zone (16), arranged in this order in an inflow direction (IFD) of a fluid flow to flow through said fluid mixing structure (10) and being composed of said at least two fluidic components, and a flow splitter (32) arranged In a space (30) formed by said expansion zone (14) and said retention zone (16) to split said fluid flow in a first sub fluid flow and a second sub fluid flow flowing in a first flow path and a second flow path, respectively, formed in the fluid mixing structure, and to mix said first and second sub fluid flows within said space (30) to generate and discharge a homogenized fluid flow, wherein said flow splitter (32) is arranged and configured to let any flow element of each of said first and second sub fluid flows prior to their mixing have a non-zero average flow component in said inflow direction (IFD).

公开(公告)号：US09815768B2

公开(公告)日：2017-11-14

申请号：US15112617

申请日：2015-02-16

Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED

Inventor： Satoru Ujita ,  Takashi Miyamoto

IPC: C07C205/11 ,  C07C201/12 ,  B01J23/44

CPC classification number: C07C205/11 ,  B01J21/18 ,  B01J23/44 ,  C07C201/12

Abstract: Position-1 halogen can be selectively reduced by reacting a compound represented by formula (3): [wherein X represents a chlorine atom, a bromine atom, or an iodine atom] with halogen in the presence of a heterogeneous transition metal catalyst to produce 2-(halogenomethyl)-1-methyl-3-nitrobenzene represented by formula (1): [wherein the symbol is as defined above].

公开(公告)号：US20170291876A1

公开(公告)日：2017-10-12

申请号：US15511243

申请日：2015-06-12

Applicant: Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

Inventor： Xiaoming FENG ,  Qian YAO ,  Xiaohua LIU ,  Lili LIN ,  Yuheng ZHANG

IPC: C07D231/12 ,  C07C201/12

CPC classification number: C07D211/88 ,  C07C201/12 ,  C07C205/53 ,  C07D207/267 ,  C07D231/12 ,  C07D231/16 ,  C07D405/06 ,  C07D409/06

Abstract: A synthesis method of γ-nitropyrazole amide compound through asymmetrical catalyzing technique is provided, a nitroalkane and an α,β-unsaturated pyrazole amide are applied as the raw material, a complex formed by a chiral amine oxide with a rare earth metal compound is served as the catalyst, a 4 Å molecular sieve is served as an additive, the γ-nitropyrazole amide compound can be obtained with a yield more than 99% and enantiomeric excess more than 99% ee. The catalytic system not only has the advantages of simple operation, mild reaction conditions, requiring no acid/base additives, convenient product purification, high yield and enatioselectivity, compliance with green atomic economy, and promising prospects for industrial application, but also allows the obtained γ-nitropyrazole amide compound to undergo some simple chemical conversions to produce some molecules having physiological activities.

公开(公告)号：US20170275318A1

公开(公告)日：2017-09-28

申请号：US15362997

申请日：2016-11-29

Applicant: KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS

Inventor： Bassam EL ALI ,  Rami Khalid SULEIMAN ,  Mansur Bala IBRAHIM

IPC: C07F15/00 ,  C07C2/86 ,  C07C41/32 ,  C07C45/68 ,  C07C201/12 ,  C07D317/50 ,  C07C1/32 ,  B01J31/18

CPC classification number: C07F15/0066 ,  B01J31/183 ,  B01J2231/4211 ,  B01J2231/4261 ,  B01J2231/4266 ,  B01J2531/824 ,  C07C1/321 ,  C07C2/861 ,  C07C17/269 ,  C07C41/30 ,  C07C41/32 ,  C07C45/68 ,  C07C201/12 ,  C07C209/68 ,  C07C253/30 ,  C07D317/50 ,  C07C255/34 ,  C07C211/45 ,  C07C205/06 ,  C07C49/784 ,  C07C43/205 ,  C07C15/14 ,  C07C47/546 ,  C07C43/215 ,  C07C15/52 ,  C07C49/796 ,  C07C49/84 ,  C07C15/54 ,  C07C22/04

Abstract: A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be recycled without significantly losing any catalytic activity in a variety of chemical transformations, a method for producing the solid-supported catalyst ligand and a method for catalyzing a palladium cross-coupling reaction, such as the Suzuki-Miyaura, Mizoroki-Heck, and Sonagashira reactions.

公开(公告)号：US09676795B2

公开(公告)日：2017-06-13

申请号：US14000116

申请日：2012-02-17

Applicant: Vladimir Grushin ,  Alessandro Zanardi

Inventor： Vladimir Grushin ,  Alessandro Zanardi

IPC: C07F1/08 ,  C07B39/00 ,  C07C17/32 ,  C07C201/12 ,  C07F1/00 ,  C07C41/30 ,  C07C45/45 ,  C07C45/68

CPC classification number: C07F1/08 ,  C07B39/00 ,  C07C17/32 ,  C07C41/30 ,  C07C45/455 ,  C07C45/68 ,  C07C201/12 ,  C07F1/005 ,  C07C22/08 ,  C07C205/11 ,  C07C43/225 ,  C07C49/80

Abstract: Process to obtain a trifluoromethylating composition which comprises the reaction between a copper (I) source and a base in the presence of a solvent and between the resulting cuprating reagent with fluoroform.