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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 23, Number 11
BKCSDE 23(11)
November 20, 2002 

Synthesis of Tetracyclic Pyrido[2,3-b]azepine Derivatives as Analogues of Mirtazapine via N-Acyliminium Ion Cyclization
Jae Yeol Lee, Sung Hun Bang, Sook Ja Lee, Yun Seon Song, Changbae Jin, Hokoon Park, Yong Sup Lee *
Homooxacalix[4]arene, Conformation, Crystal structure
Tetracyclic pyrido[2,3-b]azepine derivatives 4a-d and 4f as analogues of mirtazapine were synthesized via N-acyliminium ion cyclization by using aromatic rings such as benzene and thiophene ring as a π-nucleophile,and evaluated for the binding affinity for α2-adrenoceptor. Among tested compounds, 2,3,9,13b-tetrahydro-1H-benzo[f]pyrrolo[2,1-a]pyrido[2,3-c]azepine (4a) was the most potent (Ki = 0.26 μM) but showed about 3-fold less binding affinity than mirtazapine (Ki = 0.08 μM) for a2-adrenoceptor.
1623 - 1628
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