PROCESS FOR PREPARING CYSTEIN DERIVATIVES

摘要

The title compds. (I; R = benzyloxycarbonyl or tosyl) were obtd. by reacting an N,N'-protected cystyl dichloride with 2,4dibromo-6-(N- methyl-N-cyclohexylamino-methyl)aniline(II). (I) have good expectorant, antitissue and respiratory tract fluid fluidifying activities with low toxicity. LD 50 (mouse, rat; i.p. and p.o.) is over 3000 mg/kg. Expectorant ED 50 in a rabbit is 100 mg/kg (R is benzoyloxycarbonyl) and 3.7 mg/kg (R is tosyl). (I) (R is benzoyloxycarbonyl) is active as an antitussive at 30 mg/kg i.p.