Improved Synthesis and Crystal Structure of Dalcetrapib
oleh: Frank Richter, Sven Nerdinger, Herwig Schottenberger, Volker Kahlenberg, Gerhard Laus
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2012-10-01 |
Deskripsi
An improved synthesis of the Cholesteryl Ester Transfer Protein inhibitor dalcetrapib is reported. The precursor disulfide was reduced (a) by Mg/MeOH or (b) by EtSH/DBU/THF. The resulting thiol was acylated (a) by a known procedure or (b) in a one-pot process. Impurities were removed (a) by dithiothreitol (DTT) or (b) by oxidation using H2O2. Dalcetrapib crystallized in space group P21/c.