申请人:Aventis Pharmaceuticals Products Inc.
公开号:US06307054B1
公开(公告)日:2001-10-23
The present invention is directed to a process for preparing 2,4-dihydroxy-pyridine comprising heating a compound of the formula A
wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed to a process for preparing 2,4-dihydroxy-3-nitropyridine comprising reacting 2,4-dihydroxypyridine with nitric acid.
The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischemia, ameliorating ischenic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.
本发明涉及一种制备2,4-二羟基吡啶的方法,包括加热化合物A,其中R为H、烷基或芳基烷基,以及磷酸,其中磷酸与水的比例不少于27:1重量%。本发明还涉及一种制备2,4-二羟基-3-硝基吡啶的方法,包括将2,4-二羟基吡啶与硝酸反应。本发明的过程制备的中间体可用于制备用于治疗高血压或心肌缺血的心血管疾病,改善缺血性损伤或心肌梗死大小,或治疗高脂血症或高胆固醇血症的化合物。