## 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 pharma
Synthesis of [2H]-labelled phase-I-metabolites using 1-[2H]-pyridinium hydrochloride
✍ Scribed by Georg Heinkele; Thomas E. Mürdter
- Publisher
- John Wiley and Sons
- Year
- 2005
- Tongue
- French
- Weight
- 81 KB
- Volume
- 48
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.941
No coin nor oath required. For personal study only.
✦ Synopsis
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.
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The preparation of deuterium labeled fexinidazole, a 5‐nitroimidazole drug candidate for the treatment of Human African Trypanosomiasis, and its two main metabolites (fexinidazole sulfoxide and fexinidazole sulfone) for use as internal standards for liquid chromatography‐mass spectrometry are report
## Abstract Sulfamethoxazole was labelled at positions 3, 5, and 4′ by H/D exchange in a mixture of 5% ^2^H~2~SO~4~ and 95% ^2^H~2~O (v/v) under reflux for 72h with good isotope incorporation and acceptable yield. Subsequently, [^2^H~3~]‐sulfamethoxazole‐__N__~1~‐glucuronide and [^2^H~3~]‐__N__~4~‐
## 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