Results 121 to 130 of about 1,089 (172)

Asymmetric synthesis of 2-arylpiperazines

Bioorganic & Medicinal Chemistry Letters, 2014
An asymmetric synthesis of 2-arylpiperazines starting from phenacyl bromides, a variety of which are easily available, has been established. The synthesis features a CBS reduction of phenacyl bromide to provide optically enriched compounds, an SN2 reaction of 1,2,3-oxathiazolidine 2-oxides with an azide anion with invert of configuration, and ...
Satoshi, Yokoshima, Kazutoshi, Watanabe, Fumiaki, Uehara, Yoshihiro, Usui, Hiroshi, Tanaka   +4 more
openaire   +2 more sources

Progress in arylpiperazine synthesis by the catalytic amination reaction

Bioorganic & Medicinal Chemistry, 2002
Careful base and solvent optimization for catalytic amination is described. A Pd-catalyzed amination between some arylbromide and unprotected piperazine (1equiv) was efficiently carried out with Pd/BINAP catalyst in a toluene-DBU solvent system, which is useful for the one-pot preparation of unsymmetrical piperazine through amination and in-situ N ...
Yasuhiro, Torisawa, Takao, Nishi, Jun-ichi, Minamikawa   +2 more
openaire   +2 more sources

In-vivo metabolism of 4-substituted arylpiperazines to pharmacologically active 1-arylpiperazines.

Bollettino chimico farmaceutico, 1991
A common metabolic process of 4-substituted arylpiperazine pharmacological agents is cleavage of the side-chain to yield 1-arylpiperazines. These metabolites are a well-known class of centrally active compounds and their formation may therefore be a pharmacologically significant pathway, at least in certain species, for derivates that undergo extensive
openaire   +2 more sources

Solution phase combinatorial synthesis of arylpiperazines

Tetrahedron Letters, 1997
A solution phase combinatorial synthesis of aryl piperazines 1 and 2 is described based on the S(N)Ar reaction and Schotten-Baumann acylation. The use of excess reagent is allowed and pure arylpiperazines 1 and 2 were obtained by simple acid/base washing.
Neuville, Luc, Zhu, Jieping
openaire   +1 more source

Arylpiperazines with Affinity Toward a1-Adrenergic Receptors

Current Medicinal Chemistry, 2002
In the last years, alpha(1) adrenoceptors (alpha(1)-AR) have been the subject of intense research, in part because receptor-binding studies and molecular biology have opened up new aspects of understanding but also because of the potential to find new drugs possibly acting toward pathophysiological processes where alpha(1)-AR are involved, such as ...
MANETTI F., CORELLI F., STRAPPAGHETTI G., BOTTA M.   +3 more
openaire   +4 more sources

Arylpiperazine Derivatives Acting at 5-HT1A Receptors

Current Medicinal Chemistry, 2002
Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT(1A)R sites.
M L, López-Rodríguez, D, Ayala, B, Benhamú, M J, Morcillo, A, Viso   +4 more
openaire   +2 more sources

Soluble polymer-supported synthesis of arylpiperazines

Tetrahedron Letters, 1998
Abstract A method for soluble, inexpensive polymer-supported synthesis of piperazine and piperidine libraries on the basis of nucleophilic aryl substitution (S n Ar) and N-acylation is reported. Asymmetric N, N′-disubstituted piperazine and piperidine derivatives, that are potential drug candidates, can be synthesized in quantitative yields and ...
Pi-Chi Pan, Chung-Ming Sun
openaire   +1 more source

Spatial structure in the N-arylpiperazine series

Bulletin of the Academy of Sciences of the USSR Division of Chemical Science, 1987
In the compounds examined, the angle of rotation of the plane of the aromatic ring relative to the unshared electron pair of the nitrogen atom is close to orthogonal, but in the o-fluoro-compound it is smaller.
I. Yu. Strobykina, V. E. Kataev, A. N. Vereshchagin, I. V. Galyametdinova, V. D. Akamsin   +4 more
openaire   +1 more source

Bioactive conformation of 1-arylpiperazines at central serotonin receptors

Journal of Medicinal Chemistry, 1985
A number of 1-arylpiperazines have been characterized as direct-acting serotonin agonists. Conformational parameters of this class that may affect receptor recognition and binding have been examined through the analysis of X-ray data and synthesis of rigid analogues.
J R, Huff, S W, King, W S, Saari, J P, Springer, G E, Martin, M, Williams   +5 more
openaire   +2 more sources

Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential

Bioorganic & Medicinal Chemistry Letters, 2004
Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT(2A)/D(2) binding ratio characteristic for atypical neuroleptics (>1, pK(i) values).
Tomić, Mirko, Kundaković, Marija, Butorović, Biljana, Petković, Branka, Andrić, Deana, Roglić, Goran, Ignjatović, Đurđica, Kostić-Rajačić, Slađana   +7 more
openaire   +6 more sources