On October 1, 2013, Wang, Min; Gao, Mingzhang; Zheng, Qi-Huang published an article.Reference of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was A high-yield route to synthesize the P-glycoprotein radioligand [11C]N-desmethyl-loperamide and its parent radioligand [11C]loperamide. And the article contained the following:
N-Desmethyl-loperamide and loperamide were synthesized from α,α-diphenyl-γ-butyrolactone and 4-(4-chlorophenyl)-4-hydroxypiperidine in five and four steps with 8% and 16% overall yield, resp. The amide precursor was synthesized from 4-bromo-2,2-diphenylbutyronitrile and 4-(4-chlorophenyl)-4-hydroxypiperidine in 2 steps with 21-57% overall yield. [11C]N-Desmethyl-loperamide and [11C]loperamide were prepared from their corresponding amide precursor and N-desmethyl-loperamide with [11C]CH3OTf through N-[11C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 20-30% and 10-15% radiochem. yields, resp., based on [11C]CO2 and decay corrected to end of bombardment (EOB), with 370-740 GBq/μmol specific activity at EOB. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Reference of 4-(4-Chlorophenyl)piperidin-4-ol
The Article related to radioligand desmethylloperamide loperamide preparation, butyrolactone hydroxypiperidine ring opening, automation, brain imaging, p-glycoprotein (p-gp), positron emission tomography (pet), [(11)c]loperamide, [(11)c]n-desmethyl-loperamide ([(11)c]dlop) and other aspects.Reference of 4-(4-Chlorophenyl)piperidin-4-ol
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem