𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis of radiolabeled racemic and enantiomeric antiarrhythmic agents

✍ Scribed by Wayne T. Stolle; Lindsay S. Stelzer; Jackson B. Hester; Salvatore C. Perricone; Richard S. P. Hsi

Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
649 KB
Volume
34
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

Ibutilide fumarate, racemic N‐[4‐[4‐(ethyl‐n‐heptylamino)‐1‐hydroxybutyl]phenyl]methanesulfonamide hemifumarate, and artilide, the R‐(+)‐enantiomer of N‐[4‐[4‐(di‐n‐butylalmino)‐1‐hydroxybutyl]‐phenyl]methanesulfonamide hemifumerate, are under clinical investigation as Class III antiarrhythmic agents. For conducting drug disposition studies, we synthesized carbon‐14 labeled ibutilide, as well as its two enantiomeric forms. In addition, high specific activity tritium labeled ibutilide was also prepared to facilitate development of a radioimmunoassay and for studying receptor site characteristics of this agent. Results of metabolism studies with [^14^C]ibutilide led us to prepare tritium labeled artilide, which is more readily accessible than the C‐14 labeled drug. The optical antipode of artilide was also labeled with tritium for comparative drug disposition investigations on the two enantiomers.

📜 SIMILAR VOLUMES

A synthesis of potential new antiarrhyth
A synthesis of potential new antiarrhythmic agents
✍ Tariq Javed; Ghassan F. Shattat 📂 Article 📅 2005 🏛 Journal of Heterocyclic Chemistry 🌐 English ⚖ 75 KB

N-Ethylation of substituted ethyl 1H-indole-2-carboxylates with iodoethane and potassium carbonate gave substituted ethyl 1-ethyl-1H-indole-2-carboxylates. The later compounds on treatment with a range of aryl amines with varying structural complexity, gave the desired ethyl 1H-indole-2-carboxamide

Racemic synthesis and enantiomeric conve
Racemic synthesis and enantiomeric conversion of [1-13C] valine
✍ Kevin J. Polach; Sapan A. Shah; John C. Laiuppa; David M. Lemaster 📂 Article 📅 1993 🏛 John Wiley and Sons 🌐 French ⚖ 314 KB

## Abstract A Strecker synthesis of isobutyraldehyde, K^13^CN and ammonia produced D,L‐[1‐^13^C] valine in 83% yield. This racemic mixtue was then converted to the L‐form via a D‐amino acid oxidase ‐ branched amino acid aminotransferase system in an overall yield of 75% based on K^13^CN. Given the

Synthesis of racemic and enantiomericall
Synthesis of racemic and enantiomerically pure 2′-thia-2′,3′-dideoxycytidine as potential anti-hepatitis B virus agents
✍ Bai-Chuan Pan; Yung-Chi Cheng; Shih-Hsi Chu 📂 Article 📅 1997 🏛 Journal of Heterocyclic Chemistry 🌐 English ⚖ 519 KB

## Abstract A novel class of nucleosides with the C~1~, atom bonded to three hetero atoms was synthesized. 2′‐Thia‐2′,3′‐dideoxycytidine was the pilot compound of this series. (±)‐β‐2′‐Thia‐1′,3′‐dideoxycytidine (6) and (±)‐α‐2′‐thia‐2′,3′‐dideoxycytidine (7) were synthesized from (±)‐3‐mercapto‐1,