1208-76-0Relevant academic research and scientific papers
Method for the preparation of hexahydroazepinones and hexahydroazepinoles
-
, (2008/06/13)
This disclosure describes two technical procedures for the high-yield synthesis of heterocyclic seven-membered ring-systems by Dieckmann-condensation avoiding usual dilution techniques and long reaction times. Thus, it significantly increases the overall yields of the pharmaceutically active ingredients azelastine and flezelastine, whose synthesis, starting from these seven-membered heterocyclic rings, is reported elsewhere. Yields range from 80-89%, avoiding waste and increasing economics of the synthesis.
HETEROCYCLIC ETHERS DERIVED FROM 6,11-DIHYDRODIBENZOTHIEPIN-11-OLS AND 4,9-DIHYDROTHIENO-2-BENZOTHIEPIN-4-OL; A NEW SERIES OF POTENTIAL ANTIDEPRESSANTS AND ANTIHISTAMINE AGENTS
Polivka, Zdenek,Metys, Jan,Protiva, Miroslav
, p. 2034 - 2049 (2007/10/02)
Reactions of 11-chloro-6,11-dihydrodibenzothiepin and methanesulfonates of 6,11-dihydrodibenzothiepin-11-ol (I), its 2-methyl derivative II and 4,9-dihydrothieno-2-benzothiepin-4-ol (III) with 1-methylpiperidin-4-ol, 1-methylperhydroazepin-4-ol (XIX), and tropine gave the ethers V-X.Their methanesulfonates were pharmacologically tested and showed antireserpine, anticataleptic, and antihistamine activities of various degree.The most active compounds were the ethers V and VI.
