Autor: |
Norie Tsuboya, Masanori Tobe, Tomoko Nakajima, Kazumi Niidome, Masato Sakamoto, Kengo Tojo, Daisuke Urabe, Takaaki Sumiyoshi |
Jazyk: |
angličtina |
Rok vydání: |
2012 |
Předmět: |
|
Zdroj: |
Molecules, Vol 17, Iss 6, Pp 6507-6518 (2012) |
Druh dokumentu: |
article |
ISSN: |
1420-3049 |
DOI: |
10.3390/molecules17066507 |
Popis: |
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. |
Databáze: |
Directory of Open Access Journals |
Externí odkaz: |
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