Simultaneous O-demethylation and hydrogen/deuterium exchange of aryl-methylethers can be obtained using 1-[ 2 H]-pyridinium hydrochloride as reagent at 2208C for 6 h. This reaction was applied to dextromethorphan and various non-steroidal antiinflammatory drugs.
Synthesis of 2H- and 3H-labelled iptakalim hydrochloride
✍ Scribed by Cheng Zhang; Rifang Yang; Lanfu Chen; Bohua Zhong; Liuhong Yun; Hai Wang
- Publisher
- John Wiley and Sons
- Year
- 2004
- Tongue
- French
- Weight
- 110 KB
- Volume
- 47
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.844
No coin nor oath required. For personal study only.
✦ Synopsis
Abstract
Iptakalim hydrochloride (N‐(1‐methylethyl)‐1,1,2‐trimethyl‐propylamine hydrochloride) is a promising antihypertensive drug discovered and developed by Beijing Institute of Pharmacology and Toxicology. Deuterium‐ and tritium‐labelled compounds were designed and synthesized for pharmacokinetic and pharmacological mechanism studies. A derivatization method has been employed in the synthesis procedure. Copyright © 2004 John Wiley & Sons, Ltd.
📜 SIMILAR VOLUMES
## Abstract Tritium‐labeled [1,2‐^3^H]ethylamine hydrochloride was prepared through a multiple‐step sequence in high radioactive specificity. The labeled amine was isolated in high purity following cartridge filtration and used subsequently in the synthesis of [__N__‐ethyl‐1,2‐^3^H]apadenoson, an a
Commercially available [3Hl-camptothecin, labeled mainly at the C-5 position, had partially lost the tritium label after recovery from the plasma of a patient injected with this drug or after incubation in plasma at 38OC for 72 h. Carnptothecin dissolved in CH302H/2Hz0, incorporated deuterium at the
The first, involving a reversible ene reaction yielded 10-deuteriocarvone with some substitution at other reactive centres, An improverent to this route involved the decomposition of an organozinc reagent of 10-chlorocarvone which gave a better yield of product substituted only at C-10, As a prelini
## Abstract ^2^H and ^3^H labelled Sch 40120 were prepared by Pt catalysed exchange with isotopic water. D7‐Sch 40120 was obtained in two exchanges in 53% yield and ^3^H‐Sch 40120 was prepared by a single exchange at a specific activity of 19.8 Ci/mmole. ^14^C‐Sch 40120 was prepared in 4 steps from