20011-11-4Relevant articles and documents
N-heterocyclic carbene-Pd(II)-2-methyl-4,5-dihydrooxazole complex-catalyzed highly chemoselective mono-amination of dichlorobenzenes
He, Qian-Wei,Lu, Jian-Mei,Shao, Li-Xiong,Sun, Kai-Xin,Zhou, Jin-Hui
, (2020/01/22)
The palladium-catalyzed chemoselective mono-amination of dichlorobenzenes was reported in this paper. Under the suitable conditions, all reactions involving the three isomers of dichlorobenzenes with various secondary and primary amines in the presence of
Nickel-catalysed synthesis of 3-chloroanilines and chloro aminopyridines via cross-coupling reactions of aryl and heteroaryl dichlorides with amines
Desmarets, Christophe,Schneider, Rapha?l,Fort, Yves
, p. 247 - 250 (2007/10/03)
Selective monoamination of aryl and heteroaryl dichlorides has been carried out using a catalyst combination of Ni(0) associated to 2,2′-bipyridine. The synthesis of novel 3-chloroanilines and chloro aminopyridines in good to excellent yields is allowed u
Structure-affinity relationships of a unique nicotinic ligand: N1-dimethyl-N4-phenylpiperazinium iodide (DMPP)
Romanelli,Manetti,Scapecchi,Borea,Dei,Bartolini,Ghelardini,Gualtieri,Guandalini,Varani
, p. 3946 - 3955 (2007/10/03)
DMPP is a well-known nicotinic agonist that does not fit any proposed pharmacophore for nicotinic binding and represents a unique ligand among the hundreds of nicotinic agonists studied in the past decades. A systematic modulation of the chemical structure of DMPP, aimed to establish its structure-affinity relationships, is reported. The research has allowed to identify molecules such as 11c, 13c, 14c, and 28c, with affinities for α4β2 receptors in the low nanomolar range, some 2 orders of magnitude lower than the lead compound. The agonistic properties of the most interesting compounds have been assessed by measuring their analgesic activity on mice (hot-plate test). Another result of the research was the identification of DMPP analogues, such as 3a (Ki = 90 nM) and 14b (Ki = 180 nM), that maintain affinity for the central nicotinic receptor when the ammonium function is changed into an aminic one and are therefore possible leads for drug development in neurodegenerative diseases.
Nickel-catalysed couplings of aryl chlorides with secondary amines and piperazines
Brenner, Eric,Schneider, Raphael,Fort, Yves
, p. 12829 - 12842 (2007/10/03)
The reaction of aryl chlorides with secondary amines or piperazines in the presence of an in situ generated liganded nickel catalyst gives arylamines in good yields. Our process provides a mild, convenient and cheap method of arylamination starting from readily available substrates.
Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3- chlorophenyl)piperazines for 5-HT(1A) receptor site
Mokrosz,Pietrasiewicz,Duszynska,Cegla
, p. 2369 - 2374 (2007/10/02)
The effect of the hydrocarbon chain of the model 4-substituted 1-(3- chlorophenyl)piperazines 12-31 on their affinity for 5-HT(1A) receptor sites was investigated. It was found that elongation of the 4-n-alkyl chain strongly increases the 5-HT(1A) affinit