Processes for the production of thienopyrimidine derivatives

Details Processes for the production of thienopyrimidine derivatives Processes for the production of thienopyrimidine derivatives

2005-02-01

2005-02-01

McKenzie, Thomas C. (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

C549S068000

Reexamination Certificate

active

06849738

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 R1denotes 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 R2denotes 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.

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Walker, et al. “Synthesis of Methyl Ketones from Diethyl Acylmalonates” J. Am. Chem. Soc. 68: 1386-1388 (1946).

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