The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Feb. 01, 2005
Filed:
Feb. 27, 2001
Koichiro Fukuoka, Osaka, JP;
Hiroaki Yamamoto, Kawanishi, JP;
Kazuhiro Kimura, Suita, JP;
Junichi Kawakami, Ikoma, JP;
Shokyo Miki, Toyonaka, JP;
Koichiro Fukuoka, Osaka, JP;
Hiroaki Yamamoto, Kawanishi, JP;
Kazuhiro Kimura, Suita, JP;
Junichi Kawakami, Ikoma, JP;
Shokyo Miki, Toyonaka, JP;
Takeda Chemical Industries, Ltd., Osaka, JP;
Abstract
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 Rdenotes 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: NCCHCOOR[wherein Rdenotes 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.