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Synthesis of 1,3,4,14b‐tetrahydro‐2 H ,10 H ‐pyrazino[1,2‐α]‐ pyrrolo[2,1‐c][1,4]benzodiazepines
Author(s) -
OngLee Avelina,
Sylvester Leo,
Wasley Jan W. F.
Publication year - 1983
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570200626
Subject(s) - chemistry , benzodiazepine , stereochemistry , biochemistry , receptor
1,3,4,14b‐Tetrahydro‐2 H ,10 H ‐pyrazino[1,2‐α]pyrrolo[2,1‐c] [1,4]benzodiazepines (1a‐e) were synthesized to investigate their potential CNS activity. The key step in the synthesis was the formation of the 10,11‐dihydro‐5 H ‐pyrrolo[2,1‐c][1,4]benzodiazepine (13) by reduction and concomitant cyclization of the nitroketone (11). Biological evaluation of 1a‐e revealed interesting properties for 1b (CGS 7525A) [2].