发明授权
US3891666A 6-Phenyl-s-triazolo{8 4,3-a{9 {8 1,3,4{9 -benzotriazepines and their preparation
失效
6-苯基 - 三唑并[{4',3'{9 {8 1,3,4 {9-苯并三氮杂及其制备方法
- 专利标题: 6-Phenyl-s-triazolo{8 4,3-a{9 {8 1,3,4{9 -benzotriazepines and their preparation
- 专利标题(中): 6-苯基 - 三唑并[{4',3'{9 {8 1,3,4 {9-苯并三氮杂及其制备方法
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申请号: US39164773申请日: 1973-08-27
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公开(公告)号: US3891666A公开(公告)日: 1975-06-24
- 发明人: HESTER JR JACKSON B
- 申请人: UPJOHN CO
- 专利权人: Upjohn Co
- 当前专利权人: Upjohn Co
- 优先权: US39164773 1973-08-27
- 主分类号: A23K1/16
- IPC分类号: A23K1/16 ; A61K31/55 ; A61P21/02 ; A61P25/20 ; C07D249/08 ; C07D487/04 ; C07D55/06 ; C07D57/02
摘要:
Compounds of the formula III:
wherein R is hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, or cycloalkyl of 3 to 7 carbon atoms inclusive; wherein R1 is hydrogen and alkyl defined as above; and wherein R2, R3, R4, and R5 are hydrogen, alkyl defined as above, fluorine, chlorine, bromine, nitro or alkylthio of 1 to 3 carbon atoms inclusive, are prepared by treating a compound of the formula
WHEREIN X is chlorine or bromine, and R, R2, R3, R4, and R5 are defined as above with anhydrous hydrazine or a hydrazine mineral acid salt and a base to give the compound of formula IIIA which is like III with R1 as hydrogen. Alkylation of IIIA (R1 is hydrogen) by conventional method gives the 4-N-alkylderivatives. Compounds II are produced from non-halogenated compounds I by halogenation with N-haloacid amides. The compounds of formula III (including IIIA) are sedative compounds which can be used for tranquilization of mammals.
wherein R is hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, or cycloalkyl of 3 to 7 carbon atoms inclusive; wherein R1 is hydrogen and alkyl defined as above; and wherein R2, R3, R4, and R5 are hydrogen, alkyl defined as above, fluorine, chlorine, bromine, nitro or alkylthio of 1 to 3 carbon atoms inclusive, are prepared by treating a compound of the formula
WHEREIN X is chlorine or bromine, and R, R2, R3, R4, and R5 are defined as above with anhydrous hydrazine or a hydrazine mineral acid salt and a base to give the compound of formula IIIA which is like III with R1 as hydrogen. Alkylation of IIIA (R1 is hydrogen) by conventional method gives the 4-N-alkylderivatives. Compounds II are produced from non-halogenated compounds I by halogenation with N-haloacid amides. The compounds of formula III (including IIIA) are sedative compounds which can be used for tranquilization of mammals.