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
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引用文献:
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GB1332766A|1971-06-18|1973-10-03|Upjohn Co|Triazolo-benzodiazepines|
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US4663321A|1984-06-26|1987-05-05|Merck & Co., Inc.|Triazolobenzodiazepines and pharmaceutical use|
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法律状态:
优先权:
申请号 | 申请日 | 专利标题
DE3625197|1986-07-25|
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