- 1,3-bis(2-pyridyl)benzene receptor unit and indacenodipyridine diketone organic semiconductor material and application of organic semiconductor material
-
The invention discloses a 1,3-bis(2-pyridyl)benzene receptor unit and an indacenodipyridine diketone organic semiconductor material and application of the organic semiconductor material. 1,3-bis(2-pyridyl)benzene is taken as a basic skeleton, an electron
- -
-
Paragraph 0035; 0038; 0039
(2019/04/14)
-
- Synthesis and properties of novel N,C,N terdentate skeleton based on 1,3-di(pyridin-2-yl)benzene moiety—new tricks for old dogs
-
Utilization of intermolecular Friedel–Crafts and intramolecular condensation reaction, novel 1,3-di(pyridine-2-yl)benzene(N,C,N terdentate) skeleton with electro-withdrawing group in 6' position of pyridyl and a cyclization between 6' position of pyridyl and 6 position of benzyl ring were firstly designed and synthesized. The structures of these novel N,C,N terdentate were confirmed by NMR, MS and X-ray single crystalanalyses. The photophysical properties of these compounds were briefly explored.
- Tan, Shuai,Wu, Xiugang,Zheng, Yanqiong,Wang, Yafei
-
p. 1951 - 1954
(2019/09/12)
-
- A ultrasonic process for synthesizing 2 - halogenated nicotinate and intermediates thereof
-
The invention discloses a method for synthesizing 2-halogenated ester nicotinate and a 2-halogenated ester nicotinate intermediate according to an ultrasonic method. The method comprises the following steps: adding substituent amino acrolein, a catalyst and cyanacetic ester into a reactor for a reaction under ultrasonic radiation; tracing the reaction till substituent amino acrolein is disappeared, thereby obtaining a reaction solution I containing the 2-halogenated ester nicotinate intermediate; then, adding halogen hydride into the reaction solution I for another reaction to obtain a reaction solution II; tracing and monitoring the reaction till completion; adding a lye into the reaction solution II to adjust the pH value of the reaction solution II to be 5-6; carrying out standing stratification to obtain a water layer and an organic layer; conducting extraction on the water layer by utilizing an organic solvent, and then combining the extraction solution with the organic layer; carrying out refining to obtain 2-halogenated ester nicotinate. Through the adoption of the method, an organic synthesis reaction can be effectively facilitated, the reaction speed and yield can be improved, and the environmental protection can be promoted; the reaction time is short and the operation is simple, that is, the organic synthesis reaction can be finished within 2 hours in general; the product yield and quality are high; specifically, the product yield can reach 90% or higher, and exceed that achieved according to the conventional solvent heating reflux method.
- -
-
Paragraph 0065; 0067; 0068
(2018/04/21)
-
- A microwave synthesis 2 - halogenated nicotinate and intermediates thereof
-
The invention discloses a method for synthesizing 2-halogenated nicotinic acid ester and intermediates thereof through microwave method. The method comprises the following steps: adding substitute amino acrolein, a catalyst and cyan-acetic ester into a reactor, carrying out reaction under microwave radiation, and tracking the reaction till substitute amino acrolein disappears to prepare and obtain reaction liquid of the intermediates of 2-halogenated nicotinic acid ester; adding hydrogen halide into the reaction liquid, continuously carrying out reaction, and tracking and monitoring the reaction till the reaction is complete; adding alkali liquor into the reaction liquid to adjust the pH value to 5-6; carrying out standing delamination to obtain an aqueous layer and an organic layer; extracting the aqueous layer with an organic solvent, combining the extracted aqueous layer with the organic layer, and carrying out refinement to prepare and obtain 2-halogenated nicotinic acid ester. The synthesis method of 2-halogenated nicotinic acid ester related to the invention has the advantages of beingenvironment-friendly, short in reaction time, simple to operate, high in product yield and good in quality.
- -
-
Paragraph 0047; 0048
(2018/05/16)
-
- HEMOGLOBIN MODIFIER COMPOUNDS AND USES THEREOF
-
Described herein are compounds, including pharmaceutically acceptable salts thereof, methods of making such compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat, prevent or diagnose blood-based diseases, disorders or conditions.
- -
-
Paragraph 00474
(2018/02/28)
-
- Synthesis of 9,9′-Spirobifluorenes and 4,5-Diaza-9,9′-spirobifluorenes and Their Application as Affinity Materials for Quartz Crystal Microbalances
-
Two different classes of aza analogues of 9,9′-spirobifluorenes have been synthesized. These were obtained by either furnishing the spirobifluorene with additional pyridyl moieties or by installing the aza function directly into the spirobifluorene core. These structurally rigid compounds were then evaluated as affinity materials for quartz crystal microbalances and proved to be highly potent for the detection of volatile organic compounds.
- Stobe, Caroline,Pyka, Isabella,Linke, Alexander,Müller, Sarah,Schnakenburg, Gregor,Waldvogel, Siegfried R.,Lützen, Arne
-
p. 758 - 769
(2017/06/06)
-
- Method using hydrothermal method to synthesize 2-halogeneated nicotinate and 2-halogeneated nicotinic acid
-
The invention discloses a method using a hydrothermal method to synthesize 2-halogeneated nicotinate and 2-halogeneated nicotinic acid and relates to the field of chemical synthesizing. The method uses substituted amino acrolein, catalyst, catalyst assistant, water and cyanoacetate as raw materials to synthesize the 2-halogeneated nicotinate and the 2-halogeneated nicotinic acid through the hydrothermal method. Compared with the prior art, the method is environmentally friendly, easy in separation, high in product yield, good in product quality, capable of achieving large-scale industrial production favorably, and the like.
- -
-
Paragraph 0037; 0038
(2017/11/01)
-
- Scope of Successive C-H Functionalizations of the Methyl Group in 3-Picolines: Intramolecular Carbonylation of Arenes to the Metal-Free Synthesis of 4-Azafluorenones
-
A transition-metal-free, t-BuOOH mediated intramolecular carbonylation of arenes in 2-aryl-3-picolines via oxidative C-H functionalizations of the methyl group has been developed, providing an expedient synthesis of 4-azafluorenones. Distinct from the current literature wherein methylarenes have been used as acylating agents, 2-aryl-3-picolines in this study are transformed into aldehydes, which give 4-azafluorenones upon rapid intramolecular acylation. The study demonstrates the first example of intramolecular carbonylation of arenes utilizing a methyl group as latent carbonyl functionality.
- Laha, Joydev K.,Jethava, Krupal P.,Patel, Sagarkumar
-
supporting information
p. 5890 - 5893
(2015/12/11)
-
- 1-(2-PHENOXYMETHYLHETEROARYL)PIPERIDINE AND PIPERAZINE COMPOUNDS
-
The invention relates to compounds of formula I: where X, HAr, a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
- -
-
Page/Page column 26
(2011/10/10)
-
- Discovery and SAR of 5-(3-Chlorophenylamino)benzo[ c ][2,6]naphthyridine-8- carboxylic Acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the Treatment of Cancer
-
Herein we chronicle the discovery of CX-4945 (25n), a first-in-class, orally bioavailable ATP-competitive inhibitor of protein kinase CK2 in clinical trials for cancer. CK2 has long been considered a prime cancer drug target because of the roles of deregulated and overexpressed CK2 in cancer-promoting prosurvival and antiapoptotic pathways. These biological properties as well as the suitability of CK2s small ATP binding site for the design of selective inhibitors, led us to fashion novel therapeutic agents for cancer. The optimization leading to 25n (Ki = 0.38 nM) was guided by molecular modeling, suggesting a strong binding of 25n resulting from a combination of hydrophobic interactions, an ionic bridge with Lys68, and hydrogen bonding with the hinge region. 25n was found to be highly selective, orally bioavailable across species (20-51%) and efficacious in xenograft models. The discovery of 25n will allow the therapeutic targeting of CK2 in humans for the first time.
- Pierre, Fabrice,Chua, Peter C.,Obrien, Sean E.,Siddiqui-Jain, Adam,Bourbon, Pauline,Haddach, Mustapha,Michaux, Jerome,Nagasawa, Johnny,Schwaebe, Michael K.,Stefan, Eric,Vialettes, Anne,Whitten, Jeffrey P.,Chen, Ta Kung,Darjania, Levan,Stansfield, Ryan,Anderes, Kenna,Bliesath, Josh,Drygin, Denis,Ho, Caroline,Omori, May,Proffitt, Chris,Streiner, Nicole,Trent, Katy,Rice, William G.,Ryckman, David M.
-
p. 635 - 654
(2011/03/21)
-
- Iodine-mediated solvent-controlled selective electrophilic cyclization and oxidative esterification of o-alkynyl aldehydes: An easy access to pyranoquinolines, pyranoquinolinones, and isocumarins
-
Chemoselective behavior of iodine in different solvents in the electrophilic iodocyclization of o-alkynyl aldehydes is described. o-Alkynyl aldehydes 3a-t on reaction with I2 in CH2Cl2 with appropriate nucleophiles provides pyrano[4,3-b]quinolines 4a-f, via formation of cyclic iodonium intermediate Q; however, using alcohols as a solvent as well as nucleophile, o-alkynyl esters 5a-y were obtained selectively in good to excellent yields via formation of hypoiodide intermediate R. Subsequently, o-alkynyl esters were converted in to pyranoquinolinones 6a-i and isocoumarin 6j by electrophilic iodocyclization. This developed oxidative esterification provides a novel access for the chemoselective synthesis of esters 5q-u from aldehydes 3n-p without oxidizing primary alcohol present in the substrate.
- Verma, Akhilesh K.,Rustagi, Vineeta,Aggarwal, Trapti,Singh, Amit P.
-
experimental part
p. 7691 - 7703
(2010/12/29)
-
- TRICYCLIC DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
-
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion
- -
-
Page/Page column 68
(2009/10/22)
-
- INHIBITORS OF PRENYL-PROTEIN TRANSFERASE
-
The present invention comprises piperazine/piperazinone-containing compounds having multicyclic ring system substituents on one of the piperazine/piperazinone nitrogens, which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer
- -
-
Page column 51
(2010/01/21)
-
- Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core
-
The selective inhibition of coagulation factor Xa has emerged as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe highly potent benzamidine factor Xa inhibitors based on a vicinally-substituted, heterocyclic core.
- Fevig, John M.,Pinto, Donald J.,Han, Qi,Quan, Mimi L.,Pruitt, James R.,Jacobson, Irina C.,Galemmo, Jr, Robert A.,Wang, Shuaige,Orwat, Michael J.,Bostrom, Lori L.,Knabb, Robert M.,Wong, Pancras C.,Lam, Patrick Y.S.,Wexler, Ruth R.
-
p. 641 - 645
(2007/10/03)
-
- 6-membered aromatics as factor Xa inhibitors
-
The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(=NH)NH2, which are useful as inhibitors of factor Xa.
- -
-
-
- SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW HMG-COA SYNTHASE INHIBITORS: 2-OXETANONES WITH A SIDE CHAIN CONTAINING BIPHENYL, TERPHENYL OR PHENYLPYRIDINE
-
A series of 1233A analogs containing biphenylyl, terphenylyl or phenylpyridyl groups in their side chain were synthesized and tested for the inhibitory activities against 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase and inhibition for the chol
- Hashizume, Hirokazu,Ito, Hajime,Kanaya, Naoaki,Nagashima, Hajime,Usui, Hiroyuki,et al.
-
p. 1551 - 1572
(2007/10/02)
-
