METHOD OF PRODUCING 1,4-DIPHENYLAZETIDINONE DERIVATIVES

FIELD: chemistry. ^ SUBSTANCE: there is described a method of producing 1,4-diphenylazetidinone derivatives from properly protected -substituted amino amides in the presence of silylation agents and at least one ring formation catalyst, where 1,4-diphenylazetidinone derivatives have general formula...

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Hauptverfasser: UILL DEHVID UILL'JAM, VOLL'MANN TEODOR ANDREAS, LINDENSHMIDT ANDREAS, BILLEN GJUNTER, RIGAL' DAVID, JENDRALLA KHAJNER, JUNKER BERND, JENE GERKHARD, FRIK VENDELIN
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry. ^ SUBSTANCE: there is described a method of producing 1,4-diphenylazetidinone derivatives from properly protected -substituted amino amides in the presence of silylation agents and at least one ring formation catalyst, where 1,4-diphenylazetidinone derivatives have general formula in which symbols, substitutes and indices assume values given in the formula of invention, where this ring formation catalyst is used as a cation in one of the following general formulae ^ where R16, R17, R18, R19 independently represent (C1-C15)alkyl, R41 represents (C1-C15) alkyl, R42 represents aryl, where the aryl can be substituted with -C(O)NH2, and as an anion of compounds with formulae or or or and symbols, substitutes and indices assume values given in the formula of invention, where residues from R20 to R32 and from R34 to R38 independently represent H, (C1-C6)alkyl, aryl and respectively two alkyl residues together can also form an aryl radical, which can be substituted again with F, O, Br, I, and where R39 and R40 together with 1,7,7-trimenylbicyclo[2.2.1]heptanyl, or a cation in that ring formation catalyst corresponds to the cation in general formula (XII), and the anion is R41O-, or the cation in that ring formation catalyst corresponds to the cation in general formula (XII), and the anion is R42COO-, where compounds of general formula in which, unless defined otherwise, symbols, substitutes and indices assume values given in the formula of invention, undergoes ring formation to obtain (pre)products of general formula from which the protection can be removed to obtain formula (I) compounds. ^ EFFECT: design of a novel method of producing target compounds. ^ 10 cl, 30 ex Описан способ получения производных 1,4-дифенилазетидинона из подходящим образом защищенных β-замещенных аминоамидов в присутствии агентов силилирования и по меньшей мере одного катализатора циклизации, причем производные 1,4-дифенилазетидинона соответствуют общей формуле (I), в которой символы, заместители и индексы имеют значения, указанные в формуле изобретения, причем этот катализатор циклизации используют как катион одной из нижеследующих общих формул (XII), причем R16, R17, R18, R19 независимо друг от друга означают (С1-С15)алкил, R41 означает (C1-C15) алкил, R42 означает арил, причем арил может быть замещен -C(O)NH2, и как анион соединения формул (VIII) или (IX) или (X) или (XI) и символы, заместители и индексы имеют указанные в формуле изобретения значения, причем остатки с