公开(公告)号：EP2753175A4

公开(公告)日：2015-06-17

申请号：EP12829942

申请日：2012-09-07

申请人： SCRIPPS RESEARCH INST

发明人： MICALIZIO GLENN C ,  KODADEK THOMAS ,  SARKAR MOHOSIN

IPC分类号： A01N37/00 ,  A61K31/19

CPC分类号： C07K5/08 ,  A61K31/19 ,  A61K31/192 ,  A61K38/06 ,  A61K45/06 ,  C07B53/00 ,  C07B2200/07 ,  C07B2200/11 ,  C07C51/00 ,  C07C57/52 ,  C07C57/54 ,  C07C57/60 ,  C07C57/64 ,  C07D405/10 ,  C07D405/14 ,  C07K5/0205 ,  C07K5/0804 ,  G01N33/5008 ,  G01N2800/7028

摘要： Synthesis of compounds having varying degrees of conformational rigidity is obtained via a low cost, high yield and efficient synthetic reactions. The library of compounds is structurally diverse having at least one or more chiral centers and providing large numbers of compounds having building block diversity and substantial scaffold diversity. The compounds further provide a novel method for obtaining candidate therapeutic agents for prevention, treatment or diagnosis of diseases.

摘要翻译： 通过低成本，高产率和有效的合成反应获得具有不同程度的构象刚度的化合物的合成。 化合物库在结构上不同，具有至少一个或多个手性中心并提供大量具有结构多样性和基本支架多样性的化合物。 该化合物还提供了用于获得用于预防，治疗或诊断疾病的候选治疗剂的新方法。

公开(公告)号：EP2753175A1

公开(公告)日：2014-07-16

申请号：EP12829942.7

申请日：2012-09-07

申请人： The Scripps Research Institute

发明人： MICALIZIO, Glenn, C. ,  KODADEK, Thomas ,  SARKAR, Mohosin

IPC分类号： A01N37/00 ,  A61K31/19

CPC分类号： C07K5/08 ,  A61K31/19 ,  A61K31/192 ,  A61K38/06 ,  A61K45/06 ,  C07B53/00 ,  C07B2200/07 ,  C07B2200/11 ,  C07C51/00 ,  C07C57/52 ,  C07C57/54 ,  C07C57/60 ,  C07C57/64 ,  C07D405/10 ,  C07D405/14 ,  C07K5/0205 ,  C07K5/0804 ,  G01N33/5008 ,  G01N2800/7028

摘要： Synthesis of compounds having varying degrees of conformational rigidity is obtained via a low cost, high yield and efficient synthetic reactions. The library of compounds is structurally diverse having at least one or more chiral centers and providing large numbers of compounds having building block diversity and substantial scaffold diversity. The compounds further provide a novel method for obtaining candidate therapeutic agents for prevention, treatment or diagnosis of diseases.

公开(公告)号：EP0168032A1

公开(公告)日：1986-01-15

申请号：EP85108518.3

申请日：1985-07-09

申请人： DAIKIN INDUSTRIES, LIMITED

发明人： Morita, Shigeru ,  Oka, Masahiko

IPC分类号： C07C69/653 ,  C07C103/64 ,  C08F20/22

CPC分类号： C08F20/60 ,  C07C57/54 ,  C08F20/22

摘要： A novel fluorine-containing acrylic acid derivative of the invention is represented by the formula:

wherein A is a residue derived from an organic compound having at least two active hydrogen atoms by removing at least two active hydrogen atoms, and p is an integer corresponding to the valency of the residue A, which is easily cured. Polymers comprising repeating units derived from the said acid derivative are also disclosed.

公开(公告)号：EP1760064A1

公开(公告)日：2007-03-07

申请号：EP05750962.2

申请日：2005-06-20

申请人： Wako Pure Chemical Industries, Ltd.

发明人： MAESAWA, Tsuneaki ,  ITO, Nobuhiro ,  HIROTA, Kosaku ,  SAJIKI, Hironao

IPC分类号： C07C51/347 ,  C07B59/00 ,  C07C57/54 ,  C07B61/00

CPC分类号： C07B59/001 ,  C07B2200/05 ,  C07C51/347 ,  C07C57/54

摘要： The object of the present invention is to provide a method for efficiently and industrially deuterating a haloacrylic acid or salt thereof. The present invention is an invention of a deuteration method of a compound represented by the general formula [1]:

wherein, R 1 and R 2 indicate each independently a light hydrogen atom or a heavy hydrogen atom and at least one of R 1 and R 2 indicates a light hydrogen atom; R 3 indicates a light hydrogen atom, a heavy hydrogen atom, an alkaline metal atom or an alkaline earth metal atom; X indicates a halogen atom; and n indicates 1 or 2,
which comprises reacting the compound represented by the general formula [1] with a heavy hydrogen source in the presence of a catalyst selected from a palladium catalyst, a platinum catalyst, a rhodium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst that are not subjected to activation processing; and an invention of a deuterated compound represented by the general formula [2]:

wherein, R 4 and R 5 indicate each independently a light hydrogen atom or a heavy hydrogen atom and at least one of R 4 and R 5 indicates a heavy hydrogen atom; R 3 indicates a light hydrogen atom, a heavy hydrogen atom, an alkaline metal atom or an alkaline earth metal atom; X indicates a halogen atom; and n indicates 1 or 2.

摘要翻译： 本发明的目的是提供一种有效和工业上氘化卤代丙烯酸或其盐的方法。 本发明是由通式[1]表示的化合物的氘代方法的发明：其中，R 1和R 2各自独立地表示轻氢原子或重氢原子，R 1和R 2中的至少一个 2表示轻氢原子; R 3表示轻氢原子，重氢原子，碱金属原子或碱土金属原子; X表示卤素原子; n表示1或2，其包括在催化剂存在下使通式[1]表示的化合物与重氢源反应，所述催化剂选自钯催化剂，铂催化剂，铑催化剂，钌催化剂， 镍催化剂和不经过活化处理的钴催化剂; 和由通式[2]表示的氘代化合物的发明：其中，R 4和R 5各自独立地表示轻氢原子或重氢原子，R 4和R 5中的至少一个表示重氢原子 ; R 3表示轻氢原子，重氢原子，碱金属原子或碱土金属原子; X表示卤素原子; n表示1或2。

公开(公告)号：EP1623969A4

公开(公告)日：2006-09-20

申请号：EP04723004

申请日：2004-03-24

申请人： TOSOH F TECH INC

发明人： TOKUHISA KENJI ,  MIMURA HIDEYUKI ,  KAWADA KOSUKE ,  ARAI SHOJI

IPC分类号： C07C57/54 ,  C07B61/00 ,  C07C51/10 ,  C07C51/12 ,  C07C57/52

CPC分类号： C07C57/54 ,  C07C57/52

摘要： An ±-pentafluoroethyl acrylic acid derivative represented by the general formula [I]: [wherein R represents a hydrogen atom, a non-substituted or substituted aromatic ring, or a straight or branched alkyl group having 1 to 20 carbon(s) which may have a cyclic moiety optionally substituted with at least one substituent (halogen atom, hydroxyl group, straight or branched alkoxy group having 1 to 10 carbon(s) which may have a cyclic moiety, non-substituted or substituted aromatic group)].

摘要翻译： 由通式[I]表示的α-五氟乙基丙烯酸衍生物：其中R表示氢，（未）取代的芳族环或任选具有可具有一个或多个取代基的环状部分的C1-20直链或支链烷基 在卤代，羟基，任选具有环状部分的C1-10直链或支链烷氧基和（未）取代的芳香环之中）。

公开(公告)号：EP1599436A2

公开(公告)日：2005-11-30

申请号：EP04716264.9

申请日：2004-03-02

申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) ,  Ecole Nationale Superieure de Chimie de Montpellier

发明人： AMEDURI, Bruno ,  BOUTEVIN, Bernard ,  GUIOT, Jérôme

IPC分类号： C07C51/27 ,  C07C53/21

CPC分类号： C07C51/377 ,  C07C51/27 ,  C07C67/14 ,  C07C53/21 ,  C07C57/54 ,  C07C69/653

摘要： The invention relates to a method of preparing α,β-difluoroacrylic acid and α,β-alkyl difluoroacrylates. The inventive method consists in: preparing 2,3-difluoro-2,3-dichloropropanol (I) by radical telomerisation of CFCl=CFCl with CH3OH; oxidising (I) in order to obtain 2,3-difluoro-2,3-dichloropropanoic acid (II); and treating (II) with Zn in order to dechlorinate and, optionally, esterify the acid function before or after the dechlorination step.

摘要翻译： 本发明涉及制备α，β-二氟丙烯酸和α，β-烷基二氟丙烯酸酯的方法。 本发明的方法在于：通过CFCl = CFCl与CH 3 OH的自由基聚合反应制备2,3-二氟-2,3-二氯丙醇（I） 氧化（I）以获得2,3-二氟-2,3-二氯丙酸（II）; 和用Zn处理（II）以便在脱氯步骤之前或之后脱氯并任选酯化酸官能团。

公开(公告)号：EP0203462A3

公开(公告)日：1988-06-01

申请号：EP86106573

申请日：1986-05-14

申请人： HOECHST AKTIENGESELLSCHAFT

发明人： Heumüller, Rudolf, Dr. ,  Siegemund, Günter, Dr. ,  Groh, Werner, Dr. ,  Wieners, Gerhard, Dr. ,  Herbrechtsmeier, Peter, Dr.

IPC分类号： C07C69/653 ,  C07C67/14 ,  C07C67/31 ,  C07C51/377 ,  C07C51/60 ,  C07C57/54 ,  C08F20/24

CPC分类号： C08F20/22 ,  C07C51/34 ,  C07C51/377 ,  C07C51/60 ,  C07C57/54 ,  C07C57/76

公开(公告)号：EP4376970A1

公开(公告)日：2024-06-05

申请号：EP22761052.4

申请日：2022-07-19

申请人： BASF SE

发明人： GIESHOFF, Tile ,  KRAMP, Marvin ,  DE RUITER, Cornelis Hendricus ,  SCHNEIDER, Karl-Friedrich ,  HUELSMANN, Felix ,  REIN, Christian ,  ELIXMANN, David

IPC分类号： B01D3/32 ,  C07C67/54 ,  C07C69/54

CPC分类号： B01D3/32 ,  B01D3/322 ,  C07C57/54

公开(公告)号：EP2021322A2

公开(公告)日：2009-02-11

申请号：EP07761569.8

申请日：2007-04-30

申请人： ALLERGAN, INC.

发明人： DONDE, Yariv ,  NGUYEN, Jeremiah H.

IPC分类号： C07C405/00 ,  A61K31/215

CPC分类号： C07C69/732 ,  C07B2200/07 ,  C07C57/54 ,  C07C57/62 ,  C07C57/68 ,  C07C59/56 ,  C07C59/72 ,  C07C65/19 ,  C07C65/26 ,  C07C205/56 ,  C07C255/57 ,  C07C309/10 ,  C07C309/42 ,  C07C323/17 ,  C07C323/52 ,  C07C323/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2602/08 ,  C07D277/24 ,  C07D277/56 ,  C07D307/68 ,  C07D333/16 ,  C07D333/38 ,  C07D333/40 ,  C07D335/06 ,  C07D405/10 ,  C07D409/10 ,  C07F9/3834 ,  C07F9/3882 ,  C07F9/65515

摘要： Described herein are compounds having Formula (I) and therapeutic methods, compositions, and medicaments, related thereto.

摘要翻译： 本文描述的是具有与其有关的式和治疗方法，组合物和药物的化合物。

公开(公告)号：EP1760064A4

公开(公告)日：2008-03-05

申请号：EP05750962

申请日：2005-06-20

申请人： WAKO PURE CHEM IND LTD

发明人： MAESAWA TSUNEAKI ,  ITO NOBUHIRO ,  HIROTA KOSAKU ,  SAJIKI HIRONAO

IPC分类号： C07C51/347 ,  C07B59/00 ,  C07B61/00 ,  C07C57/54

CPC分类号： C07B59/001 ,  C07B2200/05 ,  C07C51/347 ,  C07C57/54

摘要： This invention provides a method for deuterating a haloacrylic acid or its salt with high efficiency on a commercial scale. The method is characterized in that a compound represented by general formula [1] wherein R1 and R2 each independently represent a light hydrogen atom or a heavy hydrogen atom, and at least one of R1 and R2 represents a light hydrogen atom; R3 represents a light hydrogen atom, a heavy hydrogen atom, an alkali metal atom, or an alkaline earth metal atom; X represents a halogen atom; and n represents 1 or 2, is reacted with a heavy hydrogen source in the co-presence of a catalyst selected from palladium catalysts, platinum catalysts, rhodium catalysts, ruthenium catalysts, nickel catalysts, and cobalt catalysts not subjected to activation treatment. The deuterated compound is represented by general formula [2] wherein R4 and R5 each independently represent a light hydrogen atom or a heavy hydrogen atom, and at least one of R4 and R5 represents a heavy hydrogen atom; R3 represents a light hydrogen atom, a heavy hydrogen atom, an alkali metal atom, or an alkaline earth metal atom; X represents a halogen atom; and n represents 1 or 2.