申请人:Vasopharm Biotech GmbH
公开号:EP1669355A1
公开(公告)日:2006-06-14
The present invention relates to aminotetrahydropteridines and processes for the manufacture thereof. In particular, the present invention relates to a process for the manufacture of aminotetrahydrobiopterine. Said compound is an inhibitor of NO-synthase and may therefor be a valuable agent in medical applications. The manufacturing process starts from D-ribose, which is transformed in several reaction steps into an open chain osone structure with protected hydroxyl groups. Preferred protective groups are ether forming groups, in particular benzyl groups. Subsequent reaction with tetraaminopyrimidine yields hydroxyl-protected aminopteridines, which, after reduction to aminotetrahydropteridines and cleavage of the protective groups, yield the target compound. The invention also relates to said intermediates and a process for the manufacture thereof. Another subject-matter of the present invention is the use of D-ribose in said manufacturing processes.
本发明涉及氨基四氢叶酸类化合物及其制造工艺。具体而言,本发明涉及一种制备氨基四氢生物蝶啶的工艺。该化合物是一种NO合酶抑制剂,因此可能在医学应用中是一种有价值的药剂。制造工艺从D-核糖开始,经过几个反应步骤转化为带有保护羟基的开链奥松结构。首选的保护基是醚形成基团,特别是苄基团。随后与四氨基嘧啶发生反应,生成羟基保护的氨基喹啉,经还原成氨基四氢叶酸类化合物并裂解保护基团,最终得到目标化合物。本发明还涉及上述中间体及其制造工艺。本发明的另一个内容是在上述制造工艺中使用D-核糖。