| abstract |
Processes for mass-producing on an industrial scale intermediates for the preparation of thienopyrimidine derivatives exhibiting GnRH antagonism, and so on. Specifically, a process for the production of compounds of the general formula (III) or salts thereof (wherein R1 is hydrogen, nitro, halogeno, phthalimido, mono- or di-(alkylcarbonyl)amino, or alkoxy; and R2 is alkyl or aryl), which comprises converting a compound of the general formula (I) or a salt thereof: into an acid halide corresponding thereto, reacting this acid halide with a malonic ester and a magnesium alkoxide, treating the obtained product with an acid, and reacting the resulting product with sulfur and a compound of the general formula: NCCH¿2COOR?2 or a salt thereof in the presence of a primary amine. The processes make it possible to mass-produce thienopyrimidine derivatives exhibiting GnRH antagonism in high yield at high efficiency on an industrial scale by simple means. |