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1,4‐Benzodiazepines. Chemistry and Some Aspects of the Structure‐Activity Relationship
Author(s) -
Sternbach Leo H.
Publication year - 1971
Publication title -
angewandte chemie international edition in english
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 0570-0833
DOI - 10.1002/anie.197100341
Subject(s) - ring (chemistry) , chemistry , benzodiazepine , quinazoline , stereochemistry , contraction (grammar) , combinatorial chemistry , organic chemistry , medicine , biochemistry , receptor
Numerous clinically used compounds having favorable tranquilizing and toxic properties possess the 1,4‐benzodiazepine skeleton. This group of active substances is readily accessible, e.g. by ring enlargement of quinazoline derivatives, by ring contraction of benzoxadiazocines, and by synthesis from aminobenzophenones, constructing the seven‐membered ring in many cases in one step. The relationships between type and position of substituents and the pharmacological properties are illustrated using 1,3‐dihydro‐5‐phenyl‐1,4‐benzodiazepin‐2‐ones as examples.