178624-90-3Relevant academic research and scientific papers
Tertiary amine-promoted enone aziridination: Investigations into factors influencing enantioselective induction
Armstrong, Alan,Pullin, Robert D. C.,Jenner, Chloe R.,Foo, Klement,White, Andrew J. P.,Scutt, James N.
, p. 74 - 86 (2014/02/14)
trans-N-Unsubstituted aziridines were synthesised (up to 77% ee) via a chiral tertiary amine-promoted nucleophilic aziridination of a,b-unsaturated ketones utilising in situ generated N-N ylides (aminimines). A wide range of chiral tertiary amines were sy
Radical cyclization in heterocycle synthesis. Part 9: A novel synthesis of aminocyclitols and related compounds via stannyl radical cyclization of oxime ethers derived from sugars
Kiguchi, Toshiko,Tajiri, Kazumi,Ninomiya, Ichiya,Naito, Takeaki
, p. 5819 - 5833 (2007/10/03)
Stannyl radical addition-cyclization of oxime ethers derived from D-glucose, D-galactose, and D-xylose proceeded smoothly to afford alkoxyamino alcohols which were effectively converted into two types of glycosidase inhibitors or its candidates such as aminocyclitols, 1-deoxynojirimycin, and 1-deoxygalactostatin via reductive ring-expansion of trans alkoxyamino alcohols. (C) 2000 Elsevier Science Ltd.
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics
Bolós, Jordi,Gubert, Santiago,Anglada, Lluís,Planas, Josep M.,Burgarolas, Carme,Castelló, Josep M.,Sacristán, Aurelio,Ortiz, José A.
, p. 2962 - 2970 (2007/10/03)
Compound 1 (1-benzyl-3-methyl-4-[4-(4-fluorophenyl)-4- oxobutyl]piperazine), a synthetic intermediate identified as a potential atypical antipsychotic, was selected as the starting point for pharmacological improvement. From 1, sequential structural variations were conducted in order to improve its potency and oral bioavailability. These variations included a series of piperazine, ethanediamine, and piperidine derivatives. The piperidine series afforded some orally potent compounds in the inhibition of apomorphine-induced climbing and hyperactivity in mice, which are regarded as behavioral models predictive of antipsychotic efficacy. Further optimization of these structures led to the highly potent 7-[3-(1- piperidinyl)propoxy]chromenones. Inhibition of stereotypies and induction of catalepsy in rats at doses substantially higher than required for inhibition of climbing suggest an atypical antipsychotic profile, which is assumed to predict a reduced induction of extrapyramidal side effects in humans.
