![]() Method for preparation of 1,4-benzodiazepine derivatives
专利摘要:
The novel 1,4-benzodiazepines of the formula Ia or Ib which are shown in the description can be prepared by customary methods and are suitable as active substances for medicaments. 公开号:SU1681729A3 申请号:SU874202929 申请日:1987-07-20 公开日:1991-09-30 发明作者:Вальтер Герхард;Харреус Альбрехт;Вебер Карл-Гейнц;Странски Вернер;Муацевич Гойко;Казальс-Штенцель Иорге;Бехтель Вольф-Дитрих 申请人:Берингер Ингельгейм Кг (Фирма); IPC主号:
专利说明:
Table 3
权利要求:
Claims (1) [1] Formula and Method for the preparation of 1,4-benzodiazepine derivatives of the general formula (la) or where A is a group of CH or N: R is a group —O — X — CO — OR3. — O — X — CO — OR4, —O — J — R5, or —0 — X / Hl) 35 where R3 is a Ci — Sb — al kil; R4 is the group —NRsRt, where Re and Rz are independently hydrogen, CiCe alkyl, and if R6 is hydrogen, then. 40 Rz is the group / N-Re, where Re is a C1-Cd alkip, or the group ~ - {CH2) 2b / p: Rs are groups wherein Rg and Rio are the same and mean Cs-Cb alkyl; X is Ci-Ce alkylene; Y - Cr-Ce-alkylene: Ri is St-C4 alkyl; R 2 ~ phenyl unsubstituted or singly substituted by halogen, characterized in that the compound of formula II wherein A, Ri and R 2 have the indicated meanings, are reacted with a compound of formula III Hal - R11 where Hal is a halogen; R11 is the group —X — CO — OR3, —X — CO — R4, —J — RsnnH — X—, where K3, R4. Rs, X and Y have the indicated meanings, or with its hydrochloride in an inert organic solvent in the presence of a base at the boiling point of the reaction mixture, followed by, if necessary, reduction of the target product (la) to compound (16). Table 1 Compounds of formula (1a) Example A R Ri R2 T.pl 1 CH -O-CH 2 -CH 2 -NQO SNZ SbN5 4 A/ -O-SNG-S " FROMZ 0[1 SNZ SW 51'-7 V -O- (CH2) s <o SNZ CeH5 187-188 ° P0 table 2 Table 3 CompoundMr. A R a b N N -O * (CH 2 ) 3 - coax 2 n 5 0-CH Z -COONH-L- Cit H 9 in N o-ch 2 -coonh- <3n-ch 3 g N 0 “CH 2 -CM 2 -a / ' D N with e N N - z CH 3 о-sn 2 - ^ Г СНз well N 0-CH 2 - C00NH- (CHg) 2 -Nf } 3 N -O-CH 2 -COON (C2H5) 2
类似技术:
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同族专利:
公开号 | 公开日 PL266932A1|1988-09-01| HUT44788A|1988-04-28| KR880001657A|1988-04-25| EP0255028A2|1988-02-03| HU197011B|1989-02-28| FI873243A0|1987-07-24| PT85396A|1987-08-01| YU136287A|1990-06-30| DK387587A|1988-01-26| JPS6335574A|1988-02-16| AU603591B2|1990-11-22| EP0255028A3|1990-03-21| NZ221189A|1990-09-26| IL83318D0|1987-12-31| FI873243A|1988-01-26| DK387587D0|1987-07-24| DD266355A5|1989-03-29| AU7610387A|1988-01-28| NO873108L|1988-01-26| PT85396B|1989-10-26| NO873108D0|1987-07-24| ZA875446B|1989-03-29|
引用文献:
公开号 | 申请日 | 公开日 | 申请人 | 专利标题 GB1332766A|1971-06-18|1973-10-03|Upjohn Co|Triazolo-benzodiazepines| FR2183716B1|1972-05-05|1976-12-03|Centre Etd Ind Pharma| US3880876A|1972-11-03|1975-04-29|American Home Prod|Process for the preparation of 6-aryl-4H-s-triazolo-{8 4,3-a{9 {8 1,4{9 benzodiazepines| US4663321A|1984-06-26|1987-05-05|Merck & Co., Inc.|Triazolobenzodiazepines and pharmaceutical use| DE3610848A1|1986-04-01|1987-10-15|Boehringer Ingelheim Kg|NEW 1,4-DIAZEPINE| US4735941A|1986-12-23|1988-04-05|Merck & Co., Inc.|1,4-benzodiazepines with 5- and 6-membered heterocyclic rings, useful as gastrointestinal and CNS agents|GB8720414D0|1987-08-28|1987-10-07|Roussel Lab Ltd|Chemical compounds| US5895785A|1987-10-20|1999-04-20|Ruth Korth|Treatment and prevention of disorders mediated by LA-paf or endothelial cells| DE3808283A1|1988-03-12|1989-09-21|Boehringer Ingelheim Kg|NEW 3,4,5-SUBSTITUTED 4H-1,2,4-TRIAZOLE, THEIR PREPARATION AND USE| DE3810848A1|1988-03-30|1989-10-19|Boehringer Ingelheim Kg|NEW 2,3,4-SUBSTITUTED IMIDAZOLE AND 3,4,5-SUBSTITUTED 1,2,4-TRIAZOLE, THEIR PREPARATION AND USE| IL91386D0|1988-08-24|1990-04-29|Boehringer Ingelheim Kg|Method for treating autoimmune diseases by using a paf antagonist and pharmaceutical compositions comprising it| GR900100619A|1989-08-19|1991-12-30|Boehringer Ingelheim Kg|Substituted n-heterocyclic preparation process and use thereof| JP2733708B2|1990-09-22|1998-03-30|カースル産業株式会社|Exhaust port filter device| JP2520577Y2|1991-05-28|1996-12-18|住友重機械工業株式会社|Slaked lime dissolution injection device| ES2181665T3|1991-11-04|2003-03-01|Ruth-Maria Korth|TREATMENT AND PREVENTION OF MENTAL DISEASES, ACCOMPANIED BY ELEVATED LEVELS OF LISO PAF, WITH PAF ANTAGONISTS.| DE4244265C2|1992-12-28|1999-08-12|Korth Ruth Maria|Use of Paf antagonists against the new formation of Paf binding sites on endothelial cells for the treatment or prevention of hyperinsulinism| JP3719324B2|1997-12-24|2005-11-24|豊田工機株式会社|Machining method using cold air cooling| JPH11188570A|1997-12-24|1999-07-13|Toyoda Mach Works Ltd|Device and method for machining using cool air cooling|
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