✦ LIBER ✦
The synthesis of the carbonyl-14C analog of zatosetron maleate, a potent, long-acting, orally effective 5-HT3 receptor antagonist
✍ Scribed by Douglas D. O'Bannon; William J. Wheeler
- Publisher
- John Wiley and Sons
- Year
- 1991
- Tongue
- French
- Weight
- 319 KB
- Volume
- 29
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
Abstract
Endo‐5‐chloro‐2,3‐dihydro‐2,2‐dimethyl‐N‐(8‐methyl‐8 ‐azabicyclo‐[3.2.1.]‐oct‐3‐yl‐7‐benzofurancarboxamide‐[carbonyl‐^14^C] (Z)‐2‐butenedioate (zatosetron‐[^14^C] maleate, 1), has been prepared from 5‐chloro‐7‐bromo‐2,3‐dihydro‐2,2‐dimethylbenzofuran (5) in four radiochemical steps with the reaction of 5 with K^14^CN/CuCN as the key step. The synthesis of 5 from 2‐bromo‐4‐chlorophenol is also outlined.