piperidines and ethyl-trifluoropyruvate

piperidines has been researched along with ethyl-trifluoropyruvate* in 1 studies

Other Studies

1 other study(ies) available for piperidines and ethyl-trifluoropyruvate

Article	Year
Asymmetric synthesis of the carbon-14-labeled selective glucocorticoid receptor modulator using cinchona alkaloid catalyzed addition of 6-bromoindole to ethyl trifluoropyruvate. Molecules (Basel, Switzerland), 2012, May-30, Volume: 17, Issue:6 We describe in this study the asymmetric synthesis of radioisotope (RI)-labeled selective glucocorticoid receptor modulator. This synthesis is based on optimization of the cinchona alkaloid catalyzed addition of 6-bromoindole to ethyl trifluoropyruvate and Negishi coupling of zinc cyanide to the 6-bromoindole moiety. [¹⁴C] Labeled (-)-{4-[(1-{2-[6-cyano-1-(cyclohexylmethyl)-1H-indol-3-yl]-3,3,3-trifluoro-2-hydroxypropyl}piperidin-4-yl)oxy]-3-methoxyphenyl}acetic acid (-)-1 was synthesized successfully with high enantioselectivity (>99% ee) and sufficient radiochemical purity. Topics: Carbon Radioisotopes; Catalysis; Cinchona Alkaloids; Indoles; Piperidines; Pyruvic Acid; Receptors, Glucocorticoid; Temperature	2012

Article

Year

Asymmetric synthesis of the carbon-14-labeled selective glucocorticoid receptor modulator using cinchona alkaloid catalyzed addition of 6-bromoindole to ethyl trifluoropyruvate.

Molecules (Basel, Switzerland), 2012, May-30, Volume: 17, Issue:6

We describe in this study the asymmetric synthesis of radioisotope (RI)-labeled selective glucocorticoid receptor modulator. This synthesis is based on optimization of the cinchona alkaloid catalyzed addition of 6-bromoindole to ethyl trifluoropyruvate and Negishi coupling of zinc cyanide to the 6-bromoindole moiety. [¹⁴C] Labeled (-)-{4-[(1-{2-[6-cyano-1-(cyclohexylmethyl)-1H-indol-3-yl]-3,3,3-trifluoro-2-hydroxypropyl}piperidin-4-yl)oxy]-3-methoxyphenyl}acetic acid (-)-1 was synthesized successfully with high enantioselectivity (>99% ee) and sufficient radiochemical purity.

Topics: Carbon Radioisotopes; Catalysis; Cinchona Alkaloids; Indoles; Piperidines; Pyruvic Acid; Receptors, Glucocorticoid; Temperature

2012