732199-34-7Relevant academic research and scientific papers
Radiosynthesis and in vivo evaluation of a novel σ1 selective PET ligand
Jin, Hongjun,Fan, Jinda,Zhang, Xiang,Li, Junfeng,Flores, Hubert P.,Perlmutter, Joel S.,Parsons, Stanley M.,Tu, Zhude
, p. 1669 - 1677 (2014/12/11)
The σ1 receptor is an important target for CNS disorders. We previously identified a σ1 ligand TZ3108 having highly potent (Ki-σ1 = 0.48 nM) and selective affinity for σ1versus σ2 receptors. TZ3108 wa
High regiocontrol in the nucleophilic ring opening of 1-aralkyl-3,4- epoxypiperidines with amines - A short-step synthesis of 4- fluorobenzyltrozamicol and novel anilidopiperidines
Scheunemann, Matthias,Hennig, Lothar,Funke, Uta,Steinbach, J?rg
, p. 3448 - 3456 (2011/06/20)
Nucleophilic ring-opening reactions of three 1-aralkyl-3,4-epoxypiperidines with a series of aliphatic and aromatic amines have been investigated. Reactions in protic solvents, preferably 2-propanol, gave rise to 3-amino-piperidin-4-ols in ratios up to 20:1. Accordingly, 4- fluorobenzyltrozamicol, a highly potent ligand for the vesicular acetylcholine transporter was obtained directly from an epoxide ring opening in one step, without the need of chromatographic separation. Reactions in acetonitrile assisted by Li-salts, most suitable with LiBr, led regioselectively to trans-4-amino-piperidin-3-ols in high yields. N-Phenethyl substituted anilino-piperidinols as easily obtained by this method were converted into a series of new β-hydroxy substituted anilidopiperidines.
