Relevant articles and documents
All total 11 Articles be found
All total 11 Articles be foundSNAr reaction in aqueous medium in the presence of mixed organic and inorganic bases
Shelke, Nilesh B.,Ghorpade, Ramrao,Pratap, Ajay,Tak, Vijay,Acharya
, p. 31226 - 31230 (2015/04/22)
N-Arylation of amines with fluorobenzonitriles in aqueous medium is described. A mixture of N,N-diisopropylethyl amine and Na2CO3 (1:1) is found to achieve maximum conversion by refluxing for 3 hours in water. The product can be easily isolated by solvent extraction.
Rhodium(iii)-catalyzed olefinic C-H alkynylation of enamides at room temperature
Feng, Chao,Feng, Daming,Loh, Teck-Peng
supporting information, p. 9865 - 9868 (2014/08/18)
Rh(iii)-catalyzed C-H olefinic alkynylation of enamides for the stereospecific construction of synthetically useful Z-type enynamides is reported. This protocol displays good functionality tolerance and operational simplicity thus providing an alternative synthetic opportunity for the ease of access to specific 1,3-enyne derivatives.
Efficient construction of C=N double bonds via acceptorless dehydrogenative coupling
Sun, Xiang,Hu, Yu,Nie, Shao-Zhen,Yan, Yun-Yun,Zhang, Xue-Jing,Yan, Ming
supporting information, p. 2179 - 2184 (2013/10/01)
The efficient construction of C=N double bonds has been achieved by the Ir-catalyzed intramolecular acceptorless dehydrogenative cross-coupling of tertiary amines and amides. An iridium/2-hydroxypyridine complex was identified as the highly efficient catalyst. A number of quinazolinone derivatives was prepared in excellent yields. An iridium-mediated C-H activation mechanism is proposed. This finding provides an unprecedented strategy for the direct imidation of sp3 C-H bonds.
Design and synthesis of 6-fluoro-2-naphthyl derivatives as novel CCR3 antagonists with reduced CYP2D6 inhibition
Sato, Ippei,Morihira, Koichiro,Inami, Hiroshi,Kubota, Hirokazu,Morokata, Tatsuaki,Suzuki, Keiko,Iura, Yosuke,Nitta, Aiko,Imaoka, Takayuki,Takahashi, Toshiya,Takeuchi, Makoto,Ohta, Mitsuaki,Tsukamoto, Shin-ichi
, p. 8607 - 8618 (2008/12/23)
In our previous study on discovering novel types of CCR3 antagonists, we found a fluoronaphthalene derivative (1) that exhibited potent CCR3 inhibitory activity with an IC50 value of 20 nM. However, compound 1 also inhibited human cytochrome P450 2D6 (CYP2D6) with an IC50 value of 400 nM. In order to reduce its CYP2D6 inhibitory activity, we performed further systematic structural modifications on 1. In particular, we focused on reducing the number of lipophilic moieties in the biphenyl part of 1, using C log D7.4 values as the reference index of lipophilicity. This research led to the identification of N-{(3-exo)-8-[(6-fluoro-2-naphthyl)methyl]-8-azabicyclo[3.2.1]oct-3-yl}-3-(piperidin-1-ylcarbonyl)isonicotinamide 1-oxide (30) which showed comparable CCR3 inhibitory activity (IC50 = 23 nM) with much reduced CYP2D6 inhibitory activity (IC50 = 29,000 nM) compared with 1.
Substituted compounds derived from N-(benzyl)phenylacetamide, preparation and uses
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Page/Page column 32, (2010/10/20)
This invention relates to poly-substituted derivatives of the N-(benzyl)phenylacetamide type, pharmaceutical compositions comprising same, therapeutic uses thereof, more particularly in the fields of human and animal health. This invention also relates to a process for the preparation of such derivatives.
