[EN] PROCESS FOR THE SYNTHESIS OF PIOGLITAZONE HYDROGEN CHLORIDE<br/>[FR] PROCEDE DE SYNTHESE DE CHLORURE D'HYDROGENE DE PIOGLITAZONE
申请人:RICHTER GEDEON VEGYESZET
公开号:WO2005058827A1
公开(公告)日:2005-06-30
The invention relates to a process for the synthesis of pioglitazone hydrogen chloride - which is an antidiabetic drug - via novel intermediates by reacting 4-[2-(5-ethyl-2-pyridinyl)-ethoxy]-benzaldehyde salt of formula (II), wherein HX is: HCI, CF3COOH, C4H4O4, (COOH)2 with a base and then thiazolidine-2,4-dione, and the obtained 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methylene]-2,4-thiazolidinedione base is treated with hydrochloric acid and the obtained 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl] methylene]-2,4-tiazolidinedione hydrogen chloride of formula(III) is hydrogenated in the presence of a catalyst. Further objects of the invention are the salts of general formula (II) and the benzylidene derivative of formula (III).
该发明涉及一种合成吡格列酮盐酸盐的过程-这是一种抗糖尿病药物-通过用碱与4-[2-(5-乙基-2-吡啶基)-乙氧基]-苯甲醛盐(式(II))的HX反应,其中HX为:HCl,CF3COOH,C4H4O4,(COOH)2,然后与噻唑烷-2,4-二酮反应,得到5-[[4-[2-(5-乙基-2-吡啶基)乙氧基]苯基]亚甲基]-2,4-噻唑烷二酮碱,然后用盐酸处理,得到5-[[4-[2-(5-乙基-2-吡啶基)乙氧基]苯基]亚甲基]-2,4-噻唑烷二酮盐酸盐(式(III)),在催化剂存在下,对其进行氢化。该发明的进一步对象是通式(II)的盐和通式(III)的苄亚甲基衍生物。