An efficient new synthesis of racemic cetiedil and a novel route to alpha-ketocarboxylic acids utilising mild conditions

作者：Roxburgh Craig J^*; Ganellin C Robin; Thorpe Andrew J

来源：Synlett, 2007, (8): 1211-1214.

DOI：10.1055/s-2007-977414

• cetiedil
• enantiomers
• synthesis
• alpha-ketocarboxylic acids
• Swern oxidation

We describe a new efficient synthesis of the prescribed racemic drug cetiedil [(+/-)-2-cyclohexyl-2-(3-thienyl)ethanoic acid 2-(hexahydro-1H-azepin-1-yl)ethylester]. Additionally, we report herein a high yielding large scale, route to its acid precursor 7, subsequently enabling large-scale synthesis of the chiral forms of cetiedil, and detailed pharmacological investigations.
Additionally, we describe a novel route to alpha-ketocarboxylic acids, starting from readily available or easily obtainable aldehydes: The mild conditions utilised opens up its applicability for use on molecules of biological interest.

• 出版日期2007-5-16
• 单位中国人民解放军海军医学研究所