PRODUCTION OF PIPERIDINE COMPOUND AND SYNTHETIC INTERMEDIATE COMPOUND THEREOF

PURPOSE:To obtain the title compound from a phenyl derivative and piperidine derivative containing a novel substance via three kind of novel intermediates by condensation, reduction, intramolecular ring closure, condensation and deesterification and/or denitrogen protecting group reaction. CONSTITUT...

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Hauptverfasser: IKEBE TSUGIO, KITAJIMA HIROSHI, MURAKAMI OSAMU
Format: Patent
Sprache:eng
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Zusammenfassung:PURPOSE:To obtain the title compound from a phenyl derivative and piperidine derivative containing a novel substance via three kind of novel intermediates by condensation, reduction, intramolecular ring closure, condensation and deesterification and/or denitrogen protecting group reaction. CONSTITUTION:A novel substance expressed by formula 1 (A is CH2, O or S; R is ester residue; R is alkyl capable of having halogen, phenyl or substituted phenyl) is condensed with a compound expressed by formula II (R is ester residue; R is nitrogen protecting group; B is O or S; m is 1 or 2; n is integer of 0-3) or a compound expressed by formula III is condensed with a compound expressed by formula VI to give a novel substance, which is then reduced to give a novel substance expressed by formula VI. Then the novel substance expressed by formula VI is subjected to intramolecular ring closure to afford a novel substance expressed by formula VII, which is then condensed with a compound expressed by the formula XCH2CO2R (R is ester residue; X is halogen) and the condensed product is subjected to deester and/or denitrogen-protecting group reaction to provide the compound expressed by formula VIII useful as angiotensin conversion enzyme-preventing agent, ester thereof or salt thereof.