| 摘要 |
1501368 Triazinobenzodiazepines UPJOHN CO 13 Jan 1977 [9 Feb 1976] 01410/77 Heading C2C Compounds of the general formula (R, R 2 =H, Me; R 1 =COOH, C 2-4 alkoxycarbonyl, C n H 2n A; n = 1-3; A=F, Cl, Br, CF 3 , OH, C 1-3 alkoxy, NR<SP>11</SP>R<SP>111</SP>; R<SP>11</SP>, R<SP>111</SP>=H, C 1-3 alkyl or NR<SP>11</SP>R<SP>111</SP>=1-pyrrolidinyl, piperidino, morpholino, 4 - methyl - 1 - piperazinyl, 4 - (2- hydroxyethyl) - 1 - piperazinyl; R 3 =H, F, Cl, Br, CF 3 , NO 2 ; Ar=2-Py, Ph, o-chlorophenyl, o-fluorophenyl, 2,6-difluorophenyl) and their acid addition salts are prepared by reacting the corresponding 2-hydrazino-5-aryl-3H-1,4-benzodiazepine with R 1 COCHRY (provided that R 1 is not a basic group; Y=Cl, Br, I, OSO 2 R 4 ; R 4 = C 1-3 alkyl, Ph, tolyl), followed by ring-closure. The compounds in which R 1 is a basic group are prepared by reacting the corresponding 2-chloro or bromoalkyl compound with the appropriate amine or the corresponding 2-methyl or ethyl compound with a methylene ammonium salt, and the 2-bromomethyl compounds are alternatively prepared by brominating the corresponding 2-methyl compound. The above compounds are sedatives, hypnotics, anticonvulsants, tranquilizers and muscle relaxants, and increase growth rate and feed efficiency of livestock. They may be administered in the form of pharmaceutical or veterinary preparations containing them in association with a carrier.
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