- Preparation method of 4-aryl-2-halopyridine derivatives
-
4 -aryl -2 - halopyridine derivatives are disclosed. A process for preparing γ - enamine of α-unsaturated nitrile (single-activated) using a halogen source is provided to obtain high yield and efficiency under mild conditions by using 4 - a conventional double activated (double-activated -2 -) substrate through intramolecular cyclization using a halogen source.
- -
-
Paragraph 0069-0072; 0078-0079; 0084-0086
(2021/07/27)
-
- A Dichotomy in Cross-Coupling Site Selectivity in a Dihalogenated Heteroarene: Influence of Mononuclear Pd, Pd Clusters, and Pd Nanoparticles-The Case for Exploiting Pd Catalyst Speciation
-
Site-selective dihalogenated heteroarene cross-coupling with organometallic reagents usually occurs at the halogen proximal to the heteroatom, enabled by intrinsic relative electrophilicity, particularly in strongly polarized systems. An archetypical exam
- Eyles, Anthony,Fairlamb, Ian J. S.,Ford, Mark J.,Jeddi, Neda,Scott, Neil W. J.,Simon, Lauriane,Tanner, Theo,Whitwood, Adrian C.,Willans, Charlotte E.
-
supporting information
p. 9682 - 9693
(2021/07/19)
-
- γ-Functionalization of α,β-Unsaturated Nitrile in Mild Condition: Versatile Synthesis of 4-Aryl-2-Bromopyridines
-
This report describes the synthesis of 4-aryl-2-halopyridines via γ-functionalization of α,β-unsaturated nitriles, which were obtained by the HWE reaction with the corresponding ketones. The key features of our methods involve a conjugated γ-enamine formation of α,β-unsaturated nitrile (enamino nitrile), followed by consecutive intramolecular cyclization, resulting in heteroaromatic compounds like 2-halopyridines, α-pyrone, etc.
- Sim, Jaeuk,Viji, Mayavan,Rhee, Jeongtae,Jo, Hyeju,Cho, Suk Joon,Park, Yunjeong,Seo, Seung-Yong,Jung, Kwan-Young,Lee, Heesoon,Jung, Jae-Kyung
-
supporting information
p. 5458 - 5465
(2019/11/13)
-
- A radioactive iodine labeled pyrido [1, 2-a] benzimidazole derivative compound
-
The present invention relates to a radioactive iodine labeled pyrido[1,2-a]benzimidazole derivative compound represented by a certain general formula, or the salt thereof and also relates to a radioactive medicament comprising the compound.
- -
-
Paragraph 0020; 0040
(2017/08/08)
-
- Organometallic compound and organic light emitting device including the same
-
Disclosed are an organometallic compound and an organic light emitting device comprising the same. The organometallic compound is represented by chemical formula 1. The organic light emitting device using the organometallic compound can have a low driving
- -
-
Paragraph 0304; 0309-0311
(2017/01/02)
-
- Triarylbismuthanes as threefold aryl-transfer reagents in regioselective cross-coupling reactions with bromopyridines and quinolines
-
Cross-coupling studies using bromopyridines and bromoquinolines with triarylbismuths as threefold coupling reagents in substoichiometric amounts under Pd-catalysed conditions are disclosed. The reactivity was high with both mono- and dibromopyridyl substrates, and mono- and bis-couplings were carried out regioselectively. A library of monoaryl and diaryl pyridines was formed in high yields. A one-pot strategy provided a simple and straightforward synthesis of both symmetrical and unsymmetrical diarylpyridines. Arylations of 2-bromo- and 3-bromoquinolines were achieved with triarylbismuth reagents. This study demonstrates that triarylbismuths may be used as threefold arylating reagents for the synthesis of aryl pyridines and quinolines through couplings with bromopyridines and bromoquinolines under Pd-catalysed conditions. Copyright
- Rao, Maddali L.N.,Dhanorkar, Ritesh J.
-
p. 5214 - 5228
(2014/10/15)
-
- Palladium-catalyzed highly regioselective 2-arylation of 2,x-dibromopyridines and its application in the efficient synthesis of a 17β-HSD1 inhibitor
-
2,3- and 2,5-Dibromopyridines reacted with arylboronic acids, catalyzed by Pd(OAc)2/PPh3 in the presence of K2CO 3 in CH3CN/MeOH (2:1) at 50 C for 24 h, to afford 2-arylpyridines in good to high yield
- Zhou, Qizhong,Zhang, Bin,Su, Liangjun,Jiang, Tiansheng,Chen, Rener,Du, Tieqi,Ye, Yuyuan,Shen, Jianfen,Dai, Guoliang,Han, Deman,Jiang, Huajiang
-
p. 10996 - 11003
(2014/01/06)
-
- BRAIN/NEURONAL CELL-PROTECTING AGENT, AND THERAPEUTIC AGENT FOR SLEEP DISORDER
-
A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an
- -
-
Page/Page column 43
(2008/06/13)
-
- Regioselectivity in alkenyl(aryl)-heteroaryl Suzuki cross-coupling reactions of 2,4-dibromopyridine. A?synthetic and mechanistic study
-
2,4-Dibromopyridine undergoes a regioselective Suzuki cross-coupling reaction at position 2 with several alkenyl(aryl) boronic acids to render 4-bromo-2-carbon substituted pyridines, difficult to be prepared otherwise, in good yields under palladium catal
- Sicre, Cristina,Alonso-Gómez, J.-Lorenzo,Cid, M. Magdalena
-
p. 11063 - 11072
(2007/10/03)
-
- SIX-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS
-
The present invention provides compounds of Formula (I) or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, X1, X2, X3, X4, and X5 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
- -
-
Page/Page column 77
(2010/02/15)
-
- Aminoalkoxide-mediated formation and stabilization of phenylpyridyllithium: Straightforward access to phenylpyridine derivatives
-
It is shown that lithium aggregates promoted the efficient metalation of phenylpyridines and stabilization of phenylpyridyllithium. The BuLi-LiDMAE superbase prevented dimerization or nucleophilic addition encountered with t-BuLi or n-BuLi. The reported s
- Gros, Philippe,Fort, Yves
-
p. 2028 - 2029
(2007/10/03)
-
- Directed deprotonation-transmetalation as a route to substituted pyridines
-
matrix presented Regioselective C-4 deprotonation of 3-bromopyridine, followed by Li/Zn transmetalation and Pd-mediated coupling processes, provides a flexible entry to 4-substituted and 3,4-disubstituted pyridines. Application of a similar sequence to 2-
- Karig, Gunter,Spencer, James A.,Gallagher, Timothy
-
p. 835 - 838
(2007/10/03)
-
- Process for making 2-bromopyridine
-
Disclosed is the improvement to the Craig process for producing 2-bromopyridine by the diazotization-bromination reaction of 2-aminopyridine with HBr in the presence of Br2 and a diazotization agent wherein the improvement is to conduct the reaction in the additional presence of H2 SO4 and to employ a molar ratio of HBr:2-aminopyridine in the range from about 1:1 to about 3.5:1 and to employ a molar ratio of H2 SO4 :HBr in the range from about 2:8 to about 8:2.
- -
-
-