公开(公告)号：US09527822B2

公开(公告)日：2016-12-27

申请号：US15159322

申请日：2016-05-19

Applicant: E.I. du Pont de Nemours and Company

Inventor： Gary David Annis

IPC: C07D213/56 ,  C07D249/08 ,  C07D231/14 ,  C07D231/12 ,  C07D261/04 ,  C07C51/347 ,  C07C231/12 ,  C07D277/30 ,  C07C67/327 ,  C07C45/74 ,  C07C303/30 ,  C07C209/68 ,  C07C253/30 ,  C07C45/68 ,  C07C49/80 ,  C07C25/13 ,  C07C67/343 ,  C07D231/16 ,  C07C17/35 ,  C07C49/813 ,  C07C231/14 ,  C07C45/70

CPC classification number: C07D261/04 ,  C07C17/35 ,  C07C25/13 ,  C07C45/455 ,  C07C45/70 ,  C07C49/80 ,  C07C49/813 ,  C07C67/343 ,  C07C205/45 ,  C07C209/74 ,  C07C231/12 ,  C07C231/14 ,  C07C235/84 ,  C07D213/40 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D249/08 ,  C07D249/10 ,  C07D277/28 ,  C07C69/94 ,  C07C69/76 ,  C07C211/56

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is OR11 or NR12R13, and R11, R12 and R13 are as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.

Abstract translation: 公开了由式（5）和（6）的化合物制备式（2）化合物的方法，其中Z和Y在本文中定义，X表示I.还公开了新的式（2）化合物。

公开(公告)号：US09469621B2

公开(公告)日：2016-10-18

申请号：US14434556

申请日：2013-10-09

Applicant: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION ,  UBE INDUSTRIES, LTD.

Inventor： Tamao Ishida ,  Makoto Tokunaga ,  Akiyuki Hamasaki ,  Syohei Aikawa ,  Yoshiyuki Mise ,  Tetsuro Tsuji ,  Yasushi Yamamoto ,  Mitsuru Miyasaka

IPC: B01J21/06 ,  B01J23/96 ,  B01J38/56 ,  B01J38/52 ,  B01J23/89 ,  C07C67/343 ,  B01J23/68 ,  C07B37/04 ,  B01J38/50 ,  C07D307/89 ,  B01J23/66 ,  C07C2/84 ,  C07C17/269 ,  B01J23/52 ,  C07C37/11 ,  C07C67/465

CPC classification number: C07D307/89 ,  B01J21/063 ,  B01J21/066 ,  B01J23/52 ,  B01J23/66 ,  B01J23/68 ,  B01J23/688 ,  B01J23/8906 ,  B01J23/8913 ,  B01J23/892 ,  B01J23/894 ,  B01J23/96 ,  B01J38/12 ,  B01J38/50 ,  B01J38/52 ,  B01J38/56 ,  B01J2523/00 ,  C07B37/04 ,  C07C2/84 ,  C07C17/269 ,  C07C37/11 ,  C07C67/343 ,  C07C67/465 ,  C07C2523/52 ,  C07C2523/66 ,  C07C2523/68 ,  C07C2523/75 ,  C07C2523/89 ,  Y02P20/52 ,  Y02P20/584 ,  C07C69/76 ,  C07C15/14 ,  C07C22/08 ,  C07C39/15 ,  B01J2523/19 ,  B01J2523/41 ,  B01J2523/845 ,  B01J2523/3712 ,  B01J2523/48 ,  B01J2523/3706

Abstract: A method for producing a multisubstituted biphenyl compound is represented by the following formula (2), including a step of coupling a substituted benzene compound represented by the following formula (1) in the presence of a solid catalyst with gold immobilized onto a support.

公开(公告)号：US09458084B2

公开(公告)日：2016-10-04

申请号：US14400422

申请日：2013-05-07

Applicant: SOLVAY SA

Inventor： Janis Jaunzems

IPC: C07C67/343 ,  C07C69/738 ,  A01N37/06

CPC classification number: C07C67/343 ,  A01N37/06 ,  C07C69/738

Abstract: The present disclosure relates to compounds of the formula wherein R2 and A are certain substituents, Y is an ester group, a nitrile group or an amido group and Z is O, S or N+R2, and which compounds are, for example, useful as intermediates for pyrazole fungicides. The compounds of the present disclosure can be prepared by the reaction of a compound of formula R2—C(O)—CH2Y, with an orthoformate HC—(OR3)3 in the presence of a base, especially in the presence of an amine, e.g. triethylamine.

公开(公告)号：US09399210B2

公开(公告)日：2016-07-26

申请号：US13805413

申请日：2011-06-24

Applicant: Ian Andrew York ,  Sabina Ziemian

Inventor： Ian Andrew York ,  Sabina Ziemian

IPC: B01J27/24 ,  B01J23/18 ,  B01J23/20 ,  B01J27/16 ,  C07C51/353 ,  C07C67/343 ,  B01J27/18 ,  B01J37/03 ,  C01B21/097

CPC classification number: C07C67/343 ,  B01J23/18 ,  B01J23/20 ,  B01J27/16 ,  B01J27/1811 ,  B01J27/1813 ,  B01J27/24 ,  B01J37/036 ,  C01B21/0821 ,  C01B21/097 ,  C07C51/353 ,  C07C57/04 ,  C07C69/54

Abstract: The invention relates to a method of producing an ethylenically unsaturated carboxylic acid or ester, preferably an α, β ethylenically unsaturated carboxylic acid or ester. The method includes contacting formaldehyde or a suitable source thereof with a carboxylic acid or ester in the presence of a catalyst and optionally in the presence of an alcohol. The catalyst comprises a nitrided metal oxide having at least two types of metal cations, M1 and M2, wherein M1 is selected from the metals of group 2, 3, 4, 13 (called also IIIA) or 14 (called also IVA) of the periodic table and M2 is selected from the metals of groups 5 or 15 (called also VA) of the periodic table. The invention extends to a catalyst system.

Abstract translation: 本发明涉及一种制备烯属不饱和羧酸或酯，优选α，β-烯属不饱和羧酸或酯的方法。 该方法包括在催化剂存在下和任选在醇存在下使甲醛或其合适的来源与羧酸或酯接触。 催化剂包括具有至少两种金属阳离子M1和M2的氮化金属氧化物，其中M1选自第2,3,4,13族（也称为IIIA）或14（也称为IVA）的金属， 周期表和M2选自元素周期表第5或15族（也称为VA）的金属。 本发明延伸到催化剂体系。

公开(公告)号：US20160175828A1

公开(公告)日：2016-06-23

申请号：US14910456

申请日：2014-05-28

Applicant: SHANGHAI RESEARCH INSTITUTE OF CHEMICAL INDUSTRY

Inventor： An SHEN ,  Yucai CAO ,  Xiangyang WU ,  Xiaofeng YE ,  Chen NI ,  Yongqing LI

IPC: B01J31/22 ,  C07D213/16 ,  C07C67/343 ,  C07C213/08 ,  C07C1/26 ,  C07D265/30 ,  C07D333/10 ,  C07D307/36 ,  C07C45/68 ,  C07C1/32 ,  C07F15/00 ,  C07C209/10

CPC classification number: B01J31/2273 ,  B01J31/1805 ,  B01J31/2226 ,  B01J31/28 ,  B01J2231/4205 ,  B01J2231/4277 ,  B01J2531/824 ,  C07C1/26 ,  C07C1/321 ,  C07C1/325 ,  C07C1/326 ,  C07C45/68 ,  C07C49/67 ,  C07C49/784 ,  C07C67/343 ,  C07C209/10 ,  C07C213/08 ,  C07C2531/22 ,  C07C2601/14 ,  C07D213/16 ,  C07D265/30 ,  C07D295/096 ,  C07D307/36 ,  C07D333/10 ,  C07D333/16 ,  C07F15/006 ,  C07C69/734 ,  C07C69/618

Abstract: The present invention relates to an n-heterocyclic carbene (NHC) type palladium catalyst and its preparation method as well as applications. Its preparation process is as below: select glyoxal as the raw material to synthesize glyoxaldiimine in the presence of Lewis acid or Bronsted acid, and then react with paraformaldehyde to get the NHC type ligand. Use palladium(II) to react with the compound containing carbon-nitrogen double bonds to get palladium(II) cyclic dimer; make the palladium cyclic dimer and the NHC type ligand coordinated to get the NHC type palladium catalyst. The palladium catalyst with a brand new structure according to the present invention, boasts high activity and multi-purpose. In addition, it shows excellent reaction activity in a lot of catalytic-coupling reactions including Suzuki-Miyaura, Heck, Buchwald-Hartwig, Kumada-Tamao-Corriu, Sonogashira, Negishi and α-ketone arylation reactions, and some reactions even can be carried out with the presence of an extremely low concentration of catalyst, exhibiting favorable industrialization prospect.

Abstract translation: 本发明涉及一种N-杂环卡宾（NHC）型钯催化剂及其制备方法以及应用。 其制备方法如下：选择乙二醛作为原料，在路易斯酸或布朗斯台德酸存在下合成乙二醛，然后与多聚甲醛反应得到NHC型配体。 使用钯（II）与含有碳 - 氮双键的化合物反应得到钯（II）环状二聚体; 使钯环二聚体和NHC型配体配位得到NHC型钯催化剂。 本发明具有全新结构的钯催化剂具有活性高，多用途。 另外，在Suzuki-Miyaura，Heck，Buchwald-Hartwig，Kumada-Tamao-Corriu，Sonogashira，Negishi和α-酮芳基化反应等大量的催化偶合反应中显示出优异的反应活性，甚至可以进行一些反应 出现催化剂浓度极低的情况，表现出良好的工业化前景。

公开(公告)号：US09328061B2

公开(公告)日：2016-05-03

申请号：US14382053

申请日：2013-03-01

Applicant: Trustees of Boston College

Inventor： Amir H. Hoveyda ,  Daniel L. Silverio ,  Tatiana Pilyugina ,  Sebastian Torker ,  Daniel Robbins

IPC: C07C237/06 ,  C07C229/04 ,  C07D295/185 ,  C07C227/10 ,  C07C229/14 ,  C07C251/24 ,  C07F9/6539 ,  C07F9/36 ,  C07C41/30 ,  C07C29/38 ,  C07C67/343 ,  C07F7/08 ,  C07C229/08 ,  C07D207/06 ,  C07F9/50

CPC classification number: C07C237/06 ,  C07B2200/07 ,  C07C29/38 ,  C07C41/30 ,  C07C67/343 ,  C07C227/10 ,  C07C229/04 ,  C07C229/08 ,  C07C229/14 ,  C07C251/24 ,  C07D207/06 ,  C07D295/185 ,  C07F7/081 ,  C07F7/0812 ,  C07F9/36 ,  C07F9/5022 ,  C07F9/6539 ,  C07C229/30 ,  C07C43/23 ,  C07C33/30 ,  C07C33/28 ,  C07C33/483 ,  C07C69/76

Abstract: The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.

Abstract translation: 本发明提供有机分子及其有机硼试剂和双键之间的反应的方法，例如亚胺或羰基，以立体选择性提供包括胺和醇的手性产物，可用于制备生物活性分子的实体。

公开(公告)号：US20160107980A1

公开(公告)日：2016-04-21

申请号：US14782699

申请日：2014-04-09

Applicant: MATERIA INC.

Inventor： Adam M. JOHNS ,  Richard L. PEDERSON ,  Rosemary Conrad KISER ,  Andrew NICKEL

IPC: C07C67/283 ,  C07C303/06 ,  C07C67/475 ,  C07C5/03 ,  C07C41/26 ,  C07C67/347 ,  C07C2/32 ,  C07C2/02 ,  C07C303/24 ,  C07C29/147

CPC classification number: C07C67/283 ,  C07C2/02 ,  C07C2/32 ,  C07C5/03 ,  C07C6/04 ,  C07C29/147 ,  C07C41/26 ,  C07C67/343 ,  C07C67/347 ,  C07C67/475 ,  C07C303/06 ,  C07C303/24 ,  C07C2521/18 ,  C07C2523/44 ,  C07C2531/22 ,  C07C2531/24 ,  C07F11/00 ,  C07F15/0046 ,  C07C11/21 ,  C07C15/44 ,  C07C15/107 ,  C07C309/31 ,  C07C305/04 ,  C07C69/587 ,  C07C69/145

Abstract: This invention describes processes to make products by cross metathesis of functionalized or non-functionalized olefins with poly-branched poly-olefins such as terpenes (e.g., farnesene(s), α-farnesene, β-farnesene, β-myrcene, etc.) and compositions made by such methods. More particularly, the present invention relates to methods of making (i) cross metathesis products by a cross metathesis reaction between at least one hydrovinylated olefinic substrate and at least one hydrovinylated cross metathesis substrate in the presence of at least one olefin metathesis catalyst; (ii) cross metathesis products by a cross metathesis reaction between at least one hydrovinylated olefinic substrate and at least one cross metathesis substrate in the presence of at least one olefin metathesis catalyst; and (iii) cross metathesis products by a cross metathesis reaction between at least one olefinic substrate and at least one hydrovinylated cross metathesis substrate in the presence of at least one olefin metathesis catalyst; as well as compositions made by such methods.

Abstract translation: 本发明描述了通过官能化或非官能化烯烃与多支链聚烯烃如萜烯（例如法呢烯，α-法呢烯，＆ - 法呢烯，二茂铁等）的交叉复分解来制备产品的方法 ）和通过这些方法制成的组合物。 更具体地说，本发明涉及制备（i）在至少一种烯烃复分解催化剂存在下，通过至少一个加氢乙烯化的烯属基材与至少一个加氢的交联复分解基材之间的交叉复分解反应来交叉复分解产物的方法; （ii）在至少一种烯烃复分解催化剂存在下，通过至少一个加氢乙烯化的烯属基材与至少一个交叉复分解基材之间的交叉复分解反应进行交叉复分解产物; 和（iii）在至少一种烯烃复分解催化剂存在下，通过至少一种烯属基质和至少一个加氢的交联复分解基质之间的交叉复分解反应进行交叉复分解产物; 以及通过这些方法制成的组合物。

公开(公告)号：US20160039737A1

公开(公告)日：2016-02-11

申请号：US14775173

申请日：2014-03-14

Applicant: MATERIA, INC.

Inventor： Timothy M. CHAMPAGNE ,  Thay A. UNG

IPC: C07C67/333 ,  C07C5/54 ,  C07C67/60

CPC classification number: C07C67/333 ,  C07C5/54 ,  C07C6/04 ,  C07C6/06 ,  C07C7/173 ,  C07C67/343 ,  C07C67/475 ,  C07C67/60 ,  C10G29/06 ,  C10G29/205 ,  C10G2300/1088 ,  C10G2300/1092 ,  C10G2300/202 ,  C10G2400/20 ,  C10G2400/22 ,  C11B3/10 ,  C07C11/02 ,  C07C13/44 ,  C07C13/61 ,  C07C69/533 ,  C07C69/593 ,  C07C69/58

Abstract: The present invention describes the use of soluble metal salts to reduce impurities and metathesis catalysts poisons from olefinic feedstocks to improve olefin metathesis efficiency. The soluble metal salts were added to the olefinic feedstocks to prevent peroxides and catalyst poisons from inhibiting the metathesis catalyst. The soluble metal salts remain in the olefinic feedstocks and are used without further purification in the olefin metathesis reactions. The key to this invention is the soluble metal salt compounds do not inhibit the olefin metathesis catalysts but unexpectedly increase olefin metathesis catalyst efficiency while prior art heterogeneous metal complexes sequester the olefin metathesis catalyst, preventing olefin metathesis.

Abstract translation: 本发明描述了可溶性金属盐用于减少烯烃原料中杂质和易位催化剂毒物以改善烯烃复分解效率的用途。 将可溶性金属盐加入到烯烃原料中以防止过氧化物和催化剂毒物抑制复分解催化剂。 可溶性金属盐保留在烯烃原料中，无需进一步纯化即可在烯烃复分解反应中使用。 本发明的关键是可溶性金属盐化合物不会抑制烯烃复分解催化剂，但出人意料地增加了烯烃复分解催化剂效率，而现有技术的异相金属络合物螯合了烯烃复分解催化剂，从而阻止烯烃复分解。

公开(公告)号：US20150329566A1

公开(公告)日：2015-11-19

申请号：US14651832

申请日：2013-12-12

Applicant: DIVERCHIM

Inventor： Peter OOSTING ,  Emmanuel THOMAS ,  Rukiye PAMUK ,  Benoit FOLLEAS ,  Jean-Louis BRAYER ,  Benoit DE CARNE CARNAVALET ,  Christophe MEYER ,  Janine COSSY

IPC: C07F5/02 ,  C07D239/26 ,  C07D213/61 ,  C07D213/55 ,  C07D317/46 ,  C07D215/14 ,  C07D217/16 ,  C07D333/24 ,  C07D307/54 ,  C07C67/343 ,  C07D213/85

CPC classification number: C07C67/343 ,  C07B2200/09 ,  C07C41/30 ,  C07C69/743 ,  C07C69/753 ,  C07C69/757 ,  C07C269/06 ,  C07C2602/02 ,  C07D213/55 ,  C07D213/61 ,  C07D213/85 ,  C07D215/14 ,  C07D217/16 ,  C07D231/12 ,  C07D239/26 ,  C07D307/46 ,  C07D307/54 ,  C07D307/79 ,  C07D317/46 ,  C07D333/16 ,  C07D333/24 ,  C07F5/02 ,  C07F5/025 ,  C07C43/188 ,  C07C271/16 ,  C07C271/14 ,  C07C271/18

Abstract: Cyclopropylboronic compounds, the preparation process thereof and the use thereof.

Abstract translation: 环丙基硼化合物，其制备方法及其用途。

公开(公告)号：US09181298B2

公开(公告)日：2015-11-10

申请号：US12273638

申请日：2008-11-19

Applicant: Eric Marsault ,  Kamel Benakli ,  Hamid Hoveyda ,  Mark Peterson ,  Sylvie Beaubien ,  Luc Oullet ,  Carl St-Louis ,  Sophie Beauchemin

Inventor： Eric Marsault ,  Kamel Benakli ,  Hamid Hoveyda ,  Mark Peterson ,  Sylvie Beaubien ,  Luc Oullet ,  Carl St-Louis ,  Sophie Beauchemin

IPC: C07C49/84 ,  C07C45/46 ,  A61K31/122 ,  C07K5/08 ,  A61K38/12 ,  A61K38/22 ,  C07D273/00 ,  C07D413/06 ,  C07D498/04 ,  C07K5/087 ,  C07K5/097

CPC classification number: C07C213/08 ,  A61K38/12 ,  A61K38/2214 ,  C07C41/18 ,  C07C67/343 ,  C07D273/00 ,  C07D413/06 ,  C07D498/04 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/0827

Abstract: The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

Abstract translation: 本发明涉及式（I）的新型大环化合物及其药学上可接受的盐，水合物或溶剂化物：其中R1，R2，R3，R4，R5，R6，n1，m，pZ1，Z2和Z3为 在规范中描述。 本发明还涉及作为胃动素受体的拮抗剂的式（I）化合物，并且可用于治疗与该受体相关并伴有或具有运动功能障碍的病症。