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
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creator KIMURA KAZUHIRO
MIKI MASATAKA
FUKUOKA KOICHIRO
KAWAKAMI JUNICHI
YAMAMOTO HIROAKI
description 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.
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title METHOD FOR PRODUCING THIENOPYRIDINE DERIVATIVE
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