METHOD FOR PRODUCING THIENOPYRIDINE DERIVATIVE

PROBLEM TO BE SOLVED: To provide a method for producing an intermediate for a thienopyrimidine derivative having GnRH antagonism on an industrial large amount scale. SOLUTION: This method for producing a compound of formula (III) [R1 is hydrogen, nitro, a halogen, phthalimide, a mono- or di-(alkylca...

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Hauptverfasser: KIMURA KAZUHIRO, MIKI MASATAKA, FUKUOKA KOICHIRO, KAWAKAMI JUNICHI, YAMAMOTO HIROAKI
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To provide a method for producing an intermediate for a thienopyrimidine derivative having GnRH antagonism on an industrial large amount scale. SOLUTION: This method for producing a compound of formula (III) [R1 is hydrogen, nitro, a halogen, phthalimide, a mono- or di-(alkylcarbonyl)amino or alkoxy; R2 is an alkyl or an aryl] or its salt comprises subjecting a compound of formula (I) or its salt to an acid halogenation reaction, reacting the reaction product with a malonic ester and a magnesium alkoxide, treating the resultant substance with an acid and then reacting the resultant substance with sulfur and a compound of the formula: NCCH2COOR2 or its salt in the presence of a primary amine.