JPH05310705

PURPOSE:To provide a new 7-hydroxy-1-isoquinolinecarboxylic acid or its ester, useful as an excellent intermediate for synthesizing 1'-carboxy-7'-isoquinolyl-4- guanidinobenzoate as a protease inhibitor. CONSTITUTION:A 7-hydroxy-1-isoquinolinecarboxylic acid of formula I (R is H, a 1 to 4C...

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Bibliographic Details
Main Authors NAKAMURA HIROSHI, OKUE MASAYUKI, KAWAGUCHI NOBORU, KOYAMA TADAYOSHI, SEYA MOTOHIDE, NAKAKOSHI MASAMICHI, NOMOTO MAKOTO, TAKESHITA YASUYOSHI, ISHIGURO SHUN, SHIMADA SHINICHI, ABE NORIKO
Format Patent
LanguageEnglish
Published 22.11.1993
Edition5
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:PURPOSE:To provide a new 7-hydroxy-1-isoquinolinecarboxylic acid or its ester, useful as an excellent intermediate for synthesizing 1'-carboxy-7'-isoquinolyl-4- guanidinobenzoate as a protease inhibitor. CONSTITUTION:A 7-hydroxy-1-isoquinolinecarboxylic acid of formula I (R is H, a 1 to 4C alkyl, phenyl or benzyl), its ester or its acid adduct salt, e.g. 7- hydroxy-1-isoquinolinecarboxylic acid. A compound of formula II belonging to the compound of formula I in which R is H in that case can be obtained by hydrolyzing 7-benzoyloxy-1-cyanoisoquinoline of formula III. A compound of formula I in which R is an alkyl, a phenyl or a benzyl can be obtained by reacting 7-hydroxy-1-isoquinoline of formula II or its reactive derivative with a compound of formula IV (R is R except H).
Bibliography:Application Number: JP19920136076