252353-90-5Relevant articles and documents
A straightforward and efficient method for the synthesis of diversely substituted β-aminoketones and γ-aminoalcohols from 3-(N,N-dimethylamino)propiophenones as starting materials
Abonia, Rodrigo,Arteaga, Danny,Castillo, Juan,Insuasty, Braulio,Quiroga, Jairo,Orti?z, Alejandro
, p. 1396 - 1402 (2013/09/24)
Bibliotecas de novos β-aminocetonas e γ-aminoa?lcoois que mostram uma grande diversidade estrutural foram facilmente obtidas a partir de uma abordagem simple, utilizando os derivados da 3-(N,N-dimetilamino) propiofenona como material de partida chave. O p
Transformation of α-substituted propanols into γ-amino alcohols through nickel-catalyzed amination on the terminal γ-carbon of propanols
Ueno, Satoshi,Usui, Kazumi,Kuwano, Ryoichi
supporting information; experimental part, p. 1303 - 1307 (2011/07/08)
A nickel-phosphine complex was found to be effective as the catalyst for the transformation of alcohols into β-enaminones, which was successively converted into γ-amino alcohols by a conventional reductant. The sequential transformation is equivalent to the carbon-nitrogen bond formation at the γ-position of saturated alcohols. Georg Thieme Verlag Stuttgart · New York.
Synthesis and appetite suppressant activity of 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes as conformationally rigid analogues of fluoxetine
Bhandari, Kalpana,Srivastava, Shipra,Shankar, Girija,Nath, Chandishwar
, p. 2535 - 2544 (2007/10/03)
Several 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes (7-21) as conformationally rigid analogues of fluoxetine were synthesized and evaluated for their anorexigenic and antidepressant activities. For SAR studies the related acyclic analogues (
Structure - Immunosuppressive activity relationships of new analogues of 15-deoxyspergualin. 2. Structural modifications of the spermidine moiety
Lebreton, Luc,Jost, Eric,Carboni, Bertrand,Annat, Jocelyne,Vaultier, Michel,Dutartre, Patrick,Renaut, Patrice
, p. 4749 - 4763 (2007/10/03)
A series of new analogues of 15-deoxyspergualin (DSG), an immunosuppressive agent commercialized in Japan, was synthesized and tested in a graft-versus-host disease (GVHD) model in mice. Various substitutions of the spermidine 'D' region were made in order to determine its optimum structure in terms of in vivo immunosuppressive activity. Various positions of methylation were first investigated leading to the discovery of the monomethylated malonic derivative 56h in which the pro-R hydrogen of the methylene α to the primary amine of the spermidine moiety has been replaced by a methyl group. Synthesis of the similarly methylated analogue of the previously reported glycolic derivative LF 08-0299 afforded 60c which demonstrated a powerful activity at a dose as low as 0.3 mg/kg in the GVHD model and was much more potent than DSG in the demanding heart allotransplantation model in rats. The improvement of in vivo activity was supposed to be related to an increase of the metabolic stability of the methylated analogues compared to the parent molecules. Due to its very low active dose, compatible with a subcutaneous administration in humans, and its favorable pharmacological and toxicological profile, 60e was selected as a candidate for clinical evaluation.
