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DERIVATIVES OF ISOINDOLONE AS (3 AR, 7 AR)- OR (3 ARS, 7 ARS)-FORMS OR THEIRS MIXTURES OR THEIRS HYDROCHLORIDES, WHICH ARE ANTAGONISTS OF COMPOUND P
DERIVATIVES OF ISOINDOLONE AS (3 AR, 7 AR)- OR (3 ARS, 7 ARS)-FORMS OR THEIRS MIXTURES OR THEIRS HYDROCHLORIDES, WHICH ARE ANTAGONISTS OF COMPOUND P
FIELD: organic chemistry. SUBSTANCE: derivatives of isoindolone of the general formula I, where both R - hydrogen or together form the bond; both R - phenyl, which can be substituted at position 2 or 3 with halogen or methyl; R - phenyl, which can be substituted, if necessary, with a single or several radicals, - halogen, hydroxyl, alkyl (which can be substituted with hydroxyl, dialkylamine or 4-methylpiperazine), amine, alkylamine, dialkylamine, 1-pyrrolidinyl, cyclohexanediyl, naphthyl, thienyl, dithiinyl, pyrazyl and indolyl; R - hydrogen, halogen, hydroxyl, alkyl, aminoalkyl, alkoxy, acyloxy, carboxy, alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; X - oxygen atom or radical NR5, where R5 - hydrogen atom, alkyl containing from 1 to 12 carbon atoms and, if necessary, it is substituted with one or two radicals, - carboxy, dialkylamino, acylamino, alkyloxycarbonyl, alkyloxycarbonylamino, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl (alkyl components of these radicals can have also dialkylamino or phenyl substitute), phenyl, halogen-, alkyl-, alkyloxy- or dialkylamino-substituted phenyl, naphthyl, thienyl, furyl, pyridinyl or imidazolyl, or dialkylamine of latters (alkyl and acyl radicals indicated above can be directed or branched and contain from 1 to 4 carbon atoms), as (3aR, 7aR)- or (3aRS, 7aRS)-forms or theirs mixtures, or hydrochlorides. Reagent 1: reactive derivative of the general formula R3R4CHCOOH-CHCOOH. Reagent 2: derivatives of isoindolone. Reaction condition: the following modification of synthesized compounds. Synthesized compounds are used in therapy as antagonists of substance P. EFFECT: improved method of synthesis. 2 tbl
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