公开(公告)号：EP2885282A1

公开(公告)日：2015-06-24

申请号：EP13845790.8

申请日：2013-10-10

Applicant: Okinawa Institute of Science and Technology Graduate University

Inventor： CHOUTHAIWALE, Pandurang V. ,  TANAKA, Fujie

IPC: C07D309/30 ,  A61K31/215 ,  A61K31/351 ,  A61K31/357 ,  A61K31/498 ,  A61K31/551 ,  A61P35/00 ,  C07C201/14 ,  C07C205/55 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/28 ,  C07D317/30 ,  C07D407/04

CPC classification number: C07D309/28 ,  C07C201/14 ,  C07C205/55 ,  C07C2601/14 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/30 ,  C07D317/30 ,  C07D407/04

Abstract: Disclosed is a process for preparing dihydro-2H-pyran derivatives of formula I: wherein R
1 and R
2 are defined herein. The process of the invention provides the compound of formula I in concise cascade reactions and in one pot. The compound of formulae I prepared by the process of the invention and its further transformed derivatives are useful for making pharmaceutical composition for the treatment of proliferative diseases.

公开(公告)号：EP1987880A1

公开(公告)日：2008-11-05

申请号：EP07714975.5

申请日：2007-02-27

Applicant: Japan Science and Technology Agency

Inventor： KOBAYASHI, Shu ,  OYAMADA, Hidekazu ,  AKIYAMA, Ryo ,  NAITO, Takeshi

IPC: B01J31/28 ,  B01J31/26 ,  B01J31/38 ,  B01J37/03 ,  B01J37/08 ,  B01J37/34 ,  C07C2/86 ,  C07C5/03 ,  C07C5/08 ,  C07C15/12 ,  C07C15/18 ,  C07C15/54 ,  C07C67/303 ,  C07C67/343 ,  C07C69/612 ,  C07C69/618 ,  C07C201/14 ,  C07C205/19 ,  C07F7/08 ,  C07F7/18 ,  C07B61/00

CPC classification number: C07C67/303 ,  B01J23/40 ,  B01J23/70 ,  B01J31/124 ,  B01J31/127 ,  B01J31/165 ,  B01J31/26 ,  B01J31/28 ,  B01J35/006 ,  B01J37/0219 ,  B01J2231/4261 ,  B01J2231/641 ,  B01J2531/824 ,  B01J2531/828 ,  C07B2200/11 ,  C07C2/861 ,  C07C5/03 ,  C07C5/08 ,  C07C67/343 ,  C07C205/19 ,  C07C2523/42 ,  C07C2523/44 ,  C07C2523/72 ,  C07F15/0066 ,  C07F15/0086 ,  C07F15/0093 ,  C07C15/54 ,  C07C15/18 ,  C07C69/612 ,  C07C69/618

Abstract: The present invention provides a polysilane-supported transition metal catalysts or a polysilane/inorganic compound-supported transition metal catalysts, wherein various types of transition metals are supported by polysilane compounds, or combination of polysilanes and inorganic compounds. The catalysts of the present invention are hardly soluble in hydrocarbons and alcohols and are useful as catalysts in heterogeneous system for various organic synthetic reactions using the above solvents. Polysilanes supporting transition metals are easily crosslinkable by thermal treatment, microwave irradiation, UV irradiation or chemical methods such as hydrosilylation reaction and are changed to be insoluble in various solvents keeping high catalytic activity. Moreover, the stability and operability of polysilane-supported transition metal catalysts will be improved by the support thereof on inorganic compounds. These polysilane-supported transition metal catalysts show a high catalytic activity in hydrogenation reaction, hydrosilylation reaction, Heck reaction, Suzuki-Miyaura coupling reactions and the like. The catalyst is easily recoverable and reusable and the leakage of metals is extremely few.

Abstract translation: 本发明提供一种聚硅烷负载的过渡金属催化剂或聚硅烷/无机化合物负载的过渡金属催化剂，其中各种类型的过渡金属由聚硅烷化合物或聚硅烷和无机化合物的组合负载。 本发明的催化剂几乎不溶于烃和醇，并且可用作用于使用上述溶剂的各种有机合成反应的异相体系中的催化剂。 支撑过渡金属的聚硅烷通过热处理，微波照射，UV照射或氢化硅烷化反应等化学方法易于交联，并且改变为不溶于保持高催化活性的各种溶剂中。 此外，通过其对无机化合物的支持，聚硅烷负载的过渡金属催化剂的稳定性和可操作性将得到改善。 这些聚硅烷负载的过渡金属催化剂在氢化反应，氢化硅烷化反应，Heck反应，Suzuki-Miyaura偶联反应等中显示出高的催化活性。 催化剂易于回收和再利用，金属的泄漏极少。

公开(公告)号：US12247011B2

公开(公告)日：2025-03-11

申请号：US16635374

申请日：2018-07-31

Applicant: NodThera Limited

Inventor： Mark G. Bock ,  David Harrison ,  Alan Paul Watt ,  Roderick Alan Porter ,  Nicolas Felix Pierre Boutard ,  Charles-Henry Robert Yves Fabritius ,  Grzegorz Witold Topolnicki ,  Oleksandr Levenets

IPC: C07D231/12 ,  A61P37/06 ,  C07C45/68 ,  C07C201/14 ,  C07C209/36 ,  C07C263/10 ,  C07C271/28 ,  C07C271/30 ,  C07D213/55 ,  C07D231/14 ,  C07D233/60 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D241/24 ,  C07D249/08 ,  C07D307/79 ,  C07D309/12 ,  C07D409/12 ,  C07D493/04

Abstract: The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as autoinflammatory and autoimmune diseases and cancers.

公开(公告)号：US20230092143A1

公开(公告)日：2023-03-23

申请号：US17814815

申请日：2022-07-25

Applicant: MOEHS IBERICA, S.L.

Inventor： Abdeslam AKHATOU ,  Alicia DOBARRO RODRÍGUEZ

IPC: C07D401/12 ,  C07C201/14 ,  C07D239/34 ,  C07D239/36

Abstract: A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

公开(公告)号：US11168037B2

公开(公告)日：2021-11-09

申请号：US16757326

申请日：2018-10-17

Applicant: UNIVERSITA' DEGLI STUDI DI CAGLIARI ,  UNIVERSITA' DEGLI STUDI DI SASSARI

Inventor： Lidia Vera Giovanna De Luca ,  Silvia Gaspa ,  Antonio Valentoni ,  Gabriele Mulas ,  Andrea Porcheddu

IPC: C07B39/00 ,  C07C17/06 ,  C07C253/30 ,  C07C201/14 ,  C07D213/26 ,  C07D215/12 ,  C07D217/14 ,  C07C45/41

Abstract: A process that allows halogenation at the alpha-H position of alkylarenes, optionally further substituted on the aromatic or heteroaromatic ring, is described.

公开(公告)号：US20200347087A1

公开(公告)日：2020-11-05

申请号：US16724654

申请日：2019-12-23

Applicant: President and Fellows of Harvard College

Inventor： Andrew G. Myers ,  Ziyang Zhang

IPC: C07H15/12 ,  C07H17/02 ,  C07H11/02 ,  C07H15/18 ,  C07C201/12 ,  C07C201/14 ,  C07H1/00

Abstract: The present invention provides desosamine and mycaminose analogs and nitro sugars and methods for their preparation. The invention also provides methods of cyclizing a compound of Formula (A′) with glyoxal to give a nitro sugar of Formula (B). Methods for the preparation of compound of Formula (D′) are provided comprising cyclization of a nitro alcohol to give a nitro sugar and reduction and alkylation of the nitro sugar to give a desosamine, mycaminose, or an analog thereof.

公开(公告)号：US10195599B2

公开(公告)日：2019-02-05

申请号：US15911018

申请日：2018-03-02

Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

Inventor： Ankush Venkatrao Biradar ,  Shubhangi Bhalchandra Umbarkar ,  Mohan Keraba Dongare

IPC: C07D301/12 ,  C07C205/09 ,  C07C205/00 ,  B01J31/02 ,  B01J21/18 ,  B01J35/00 ,  B01J35/08 ,  B01J37/02 ,  B01J31/08 ,  B01J31/10 ,  B01J37/08 ,  C07C201/14 ,  C01B32/05

Abstract: Disclosed herein is a simple process for functionalization/grafting of carbon microspheres obtained from bagasse with various active functional groups onto it and use of the same as catalyst for various organic reactions, having very high selectivity and conversion rate.

公开(公告)号：US20160167031A1

公开(公告)日：2016-06-16

申请号：US14901456

申请日：2014-06-25

Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

Inventor： Ankush Venkatrao BIRADAR ,  Shubhangi Bhalchandra UMBARKAR ,  Mohan Keraba DONGARE

IPC: B01J31/02 ,  C07D301/12 ,  C07C201/14 ,  B01J37/08

CPC classification number: B01J31/0237 ,  B01J21/18 ,  B01J31/0205 ,  B01J31/0225 ,  B01J31/08 ,  B01J31/10 ,  B01J35/002 ,  B01J35/08 ,  B01J37/0209 ,  B01J37/084 ,  B01J2231/342 ,  B01J2231/4205 ,  B01J2231/72 ,  C01B32/05 ,  C07C201/14 ,  C07D301/12

Abstract: Disclosed herein is a simple process for functionalization/grafting of carbon microspheres obtained from bagasse with various active functional groups onto it and use of the same as catalyst for various organic reactions, having very high selectivity and conversion rate.

Abstract translation: 本文公开了一种简单的方法，用于将从具有各种活性官能团的蔗渣获得的碳微球官能化/接枝到其上，并将其用作各种有机反应的催化剂，具有非常高的选择性和转化率。

公开(公告)号：US4533776A

公开(公告)日：1985-08-06

申请号：US575649

申请日：1984-02-01

Applicant: Bernd Baasner ,  Hermann Hagemann ,  Erich Klauke

Inventor： Bernd Baasner ,  Hermann Hagemann ,  Erich Klauke

IPC: C07C67/00 ,  C07C201/00 ,  C07C201/14 ,  C07C205/08 ,  C07C205/10 ,  C07C79/12

CPC classification number: C07C205/08 ,  C07C201/14 ,  C07C205/10 ,  C07C2101/14

Abstract: In the preparation of an .alpha.-fluorinated nitroalkane of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and individually represent hydrogen, fluorine, chlorine, bromine, alkyl, halogenoalkyl or cycloalkyl, orR.sup.1 and R.sup.3 have the meaning indicated andR.sup.2 and R.sup.4 together represent an alkylene group having 3-6 carbon atoms,by conjugated nitrofluorination of the corresponding olefin of the formula ##STR2## the improvement which comprises employing about 1.1 mols of hydrogen fluoride and 1 to 2 mols of nitric acid per mol of olefin and carrying out the reaction in the presence of an agent which binds water, e.g. chlorosulphonic acid, fluorosulphonic acid, sulphur trioxide, sulphur dioxide, thionyl chloride, thionyl fluoride, sulfuryl chloride or sulfuryl fluoride. The end products, some of which are known, are useful as intermediates in synthesizing herbicides.

Abstract translation: 在制备其中R 1，R 2，R 3和R 4相同或不同并且各自表示氢，氟，氯，溴，烷基，卤代烷基或环烷基的式（Ia）的α-氟化硝基烷烃或R1和R3具有 所表示的含义，R2和R4一起表示具有3-6个碳原子的亚烷基，通过共轭硝基氟化相应的式“烯烃”烯烃，其改进包括使用约1.1摩尔氟化氢和1至2摩尔硝酸 酸/每摩尔烯烃，并在结合水的试剂存在下进行反应，例如 氯磺酸，氟磺酸，三氧化硫，二氧化硫，亚硫酰氯，亚硫酰氟，磺酰氯或硫酰氟。 其中一些已知的最终产物可用作合成除草剂的中间体。

公开(公告)号：WO2016079759A1

公开(公告)日：2016-05-26

申请号：PCT/IN2015050161

申请日：2015-11-10

Applicant: COUNCIL SCIENT IND RES

Inventor： SUDALAI ARUMUGAM ,  DEY SOUMEN

IPC: C07D213/80 ,  C07C67/39 ,  C07C201/14 ,  C07C253/30 ,  C07C319/20 ,  C07D211/94 ,  C07D307/88 ,  C07D317/12 ,  C07D333/38

CPC classification number: C07D333/38 ,  C07C67/39 ,  C07C201/14 ,  C07C253/30 ,  C07C319/20 ,  C07C2601/14 ,  C07C2602/42 ,  C07D211/94 ,  C07D213/80 ,  C07D307/88 ,  C07D317/12 ,  C07C69/76 ,  C07C69/80 ,  C07C69/92 ,  C07C69/82 ,  C07C69/618 ,  C07C69/24 ,  C07C69/56 ,  C07C69/54 ,  C07C69/78 ,  C07C205/57 ,  C07C205/42 ,  C07C323/62 ,  C07C255/57

Abstract: The present invention relates to a novel simple, efficient and single-step process for esterification of aldehydes using a heterogeneous catalyst with high yields. More particularly, the present invention relates to a novel simple, efficient and single-step process for esterification of aldehydes using Titanium superoxide with greater than 80% yields.

Abstract translation: 本发明涉及使用高产率的多相催化剂酯化醛的新型简单，有效和单步方法。 更具体地说，本发明涉及使用超过80％产率的超氧化钛来酯化醛的新型简单，有效和单步方法。