发明名称 A new method of preparing 3-(2-hydroxy-2-arylethyl)-2-iminothiazolidines.
摘要 A new method of preparing 3-(2-hydroxy-2-arylethyl)-2-iminothiazolidines of the formula <CHEM> and acid addition salts thereof, wherein Ar is phenyl, halophenyl, nitrophenyl or (trifluormethyl)phenyl, by protonating a starting material of the formula <CHEM> wherein Ar is as defined above, R<1> is chloro or bromo and R<2> is lower alkyloxy, aryloxy or optionally substituted phenyl, or, R<1> and R<2> taken together, represent an -O-radical, and subsequently reacting the thus obtained protonated intermediate with thiourea, ammonium isothiocyanate or an alkali- or earth alkaline metal isothiocyanate. The compounds of formula I are used as starting materials in the preparation of anthelmintic 2,3,5,6-tetrahydro-6-arylimidazo[2,1-b]thiazoles, in particular tetramisole and levamisole. The starting materials of formula (II) are obtained by hydrolyzing the corresponding halides of the formula <CHEM> wherein R<1>, R<2>, and Ar are as defined in formula (II) and X is chloro, bromo, or iodo. The starting materials of formula (II) and the halides of formula (III) are novel compounds.
申请公布号 EP0047546(A2) 申请公布日期 1982.03.17
申请号 EP19810200903 申请日期 1981.08.13
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 ALBERT, RUDOLF WILLEM HORTENSE;DE KNAEP, ALFONS GASTON MARIA;DOCKX, JOZEF CAROLUS JOANNES
分类号 C07D263/20;C07D263/22;C07D277/18;(IPC1-7):C07D277/40 主分类号 C07D263/20
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