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2. 发明授权

US06849738B2 Processes for the production of thienopyrimidine derivatives 失效
标题翻译：噻吩并嘧啶衍生物的制备方法
公开(公告)号：US06849738B2
公开(公告)日：2005-02-01
申请号：US10220233
申请日：2001-02-27
申请人： Koichiro Fukuoka , Hiroaki Yamamoto , Kazuhiro Kimura , Junichi Kawakami , Shokyo Miki
发明人： Koichiro Fukuoka , Hiroaki Yamamoto , Kazuhiro Kimura , Junichi Kawakami , Shokyo Miki
IPC分类号： C07D333/38 , C07D495/04
CPC分类号： C07D495/04 , C07D333/38
摘要： The present invention provides a process for producing an intermediate for thienopyrimidine derivatives having the GnRH antagonistic activity at an industrial large scale.The process for production of the present invention relates to a process for producing a compound represented by the formula (III): wherein respective symbols have the same meanings as those described below, or a salt thereof, which comprises subjecting a compound represented by the formula (I): wherein R1 denotes hydrogen, nitro, halogen, phthalimido, mono- or di-(alkylcarbonyl)amino or alkoxy, or a salt thereof, to an acid halogenating reaction, which is successively reacted with malonic acid ester and magnesium alkoxide, treated with an acid, and reacted with sulfur and a compound represented by the formula: NCCH2COOR2 [wherein R2 denotes alkyl or aryl], or a salt thereof, in the presence of primary amine. According to the process of production of the present invention, thienopyrimidine derivatives having the GnRH antagonistic activity can be produced effectively and at an industrial large scale by a high yield and simple method.
摘要翻译：本发明提供了一种在工业上大规模生产具有GnRH拮抗活性的噻吩并嘧啶衍生物的中间体的方法。本发明的制备方法涉及一种由式（III）表示的化合物的制备方法：其中各自符号具有与下述相同的含义或其盐，其包括使由式（I）表示的化合物：其中R 1表示氢，硝基，卤素，苯二甲酰亚氨基，单 - 或二 - （烷基羰基）氨基或烷氧基或其盐与酸卤化反应反应，该酸卤化反应与丙酸和烷氧基镁连续反应，用酸处理，并与硫和式NCCH 2 COOR 2表示的化合物反应[其中 R 2表示烷基或芳基]或其盐，在伯胺的存在下。根据本发明的制造方法，可以通过高产率和简单的方法有效地以工业规模生产具有GnRH拮抗活性的噻吩并嘧啶衍生物。

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