IMDAZOBENSODIAZEPINES

摘要

1365455 Imidazobenzodiazepines UPJOHN CO 6 Oct 1972 [2 Nov 1971] 46278/72 Heading C2C Imidazobenzodiazepines are prepared by the following route (R = H, C 1-4 alkyl, C 3-4 alkenyl; R 1 = H, C 1-3 alkyl; R 2 = 2, 3 or 4-Py, 2-pyrimidyl, furyl, pyrryl, thienyl, C 1-3 alkyl, C 2-4 alkenyl, C 5-7 cycloalkyl or cycloalkenyl, R 3 R 4 Ph; R 3,4 = H, halogen, NO 2 , CN, CF 3 , C 1-3 alkyl, alkoxy, alkylthio; alkylsulphinyl, alkylsulphonyl or alkanoylamino, di(C 1-3 alkyl)amino; X = F, Cl, Br), optionally followed by conversion to an acid addition salt. The starting materials are prepared by heating the corresponding 1,3-dihydro-2H-1,4-benzodiazepin-2-one with phosphorus pentasulphide, and reacting the resulting 2-thione with RNH 2 . The above compounds are sedatives, hypnotics, anticonvulsants, tranquillizers and muscle relaxants, and increase growth rate, feed efficiency and milk and egg production in livestock. They may be administered in the form of pharmaceutical and veterinary preparations and feed additives containing them in association with a carrier.