PIPERIDYLPROPIONAMIDE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS INCLUDING DEPRESSION AND PANIC DISORDER
申请人:Peters Dan
公开号:US20110218217A1
公开(公告)日:2011-09-08
This invention relates to novel piperidine-4-propionamide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
α-alkylation of unactivated amides with alcohols is described. Using a NCP-type pincer Ir complex as the precatalyst and KOtBu as the base, the reactions of secondary or tertiary acetamides with benzyl or nonbenzyl primary alcohols occur at 80 °C, furnishing the alkylation products in good yields. This method represents a practical and green means of α-alkylation of amides in a relatively mild, efficient
描述了未活化酰胺与醇的α-烷基化。使用NCP型夹钳Ir络合物作为前催化剂,并使用KO t Bu作为碱,仲或叔乙酰胺与苄基或非苄基伯醇的反应在80°C发生,提供了高收率的烷基化产物。该方法代表了以相对温和,有效和选择性的方式以低催化剂负载量(0.5mol%)进行酰胺的α-烷基化的实用和绿色手段。