𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis of [14C]-radiolabelled entecavir

✍ Scribed by Marc D. Ogan; David J. Kucera; Yadagiri R. Pendri; J. Kent Rinehart

Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
138 KB
Volume
48
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

Radiolabelled [^14^C]entecavir, (1), was prepared in 12 steps from (1S,2R,3S,5R)‐3‐(benzyloxy)‐2‐(benzyloxymethyl)‐6‐oxa‐bicyclo[3.1.0]hexane 2. The chemical yield of [^14^C]entecavir was 14% from the epoxide 2. Introduction of [^14^C] radiolabel was achieved by elaboration of 4,5‐diaminopyrimidine 8 with triethyl[^14^C]orthoformate to purine derivative 9. The radiochemical yield of [^14^C]entecavir from triethyl[^14^C]orthoformate was 11.3%. Radiochemical purity of [^14^C]entecavir determined by HPLC was 99.8%. The specific activity of [^14^C]entecavir was 108 µCi/mg (29.9 mCi/mmol). Copyright © 2005 John Wiley & Sons, Ltd.

📜 SIMILAR VOLUMES

Radiolabeled antimalarials: Synthesis of
Radiolabeled antimalarials: Synthesis of 14C-artemisinin
✍ Mitchell A. Avery; Jason D. Bonk; James Bupp 📂 Article 📅 1996 🏛 John Wiley and Sons 🌐 French ⚖ 194 KB

The stereoselective total synthesis of the antimalarial agent 14C-(+)-artemisinin (l), incorporating I4C at C-16 (C-9 methyl) is reported, in 18% radiochemical yield from acid 3.

Synthesis of 14C-radiolabeled ractopamin
Synthesis of 14C-radiolabeled ractopamine hydrochloride
✍ Norman H. Terando 📂 Article 📅 1992 🏛 John Wiley and Sons 🌐 French ⚖ 311 KB 👁 1 views

## Abstract Ractopamine HCl was uniformly labeled with carbon‐14 in one of two phenyl rings as a requirement for animal metabolism studies. The six‐step synthesis was completed in a 14% yield. Product instability on silica gel complicated purification, but development of a chromatographic method af

Synthesis and biodistribution of 14C-rad
Synthesis and biodistribution of 14C-radiolabelled hypocrellin B
✍ Jixiang Liu; Gerald G. Miller; Liren Huang; Zhenjun Diwu; J. William Lown; Kevin 📂 Article 📅 1995 🏛 John Wiley and Sons 🌐 French ⚖ 395 KB

## Abstract Our research group is currently exploring the use of hypocrellins as potential photosensitizers for photodynamic therapy (PDT). The purpose of this study is to investigate the synthesis and biodistribution of ^14^C‐labelled Hypocrellin B. Radiolabelled hypocrellin‐B (HB) with the ^14^C

Synthesis of [13C4]Baraclude® (entecavir
Synthesis of [13C4]Baraclude® (entecavir)
✍ Scott B. Tran; Ihoezo V. Ekhato; J. Kent Rinehart 📂 Article 📅 2009 🏛 John Wiley and Sons 🌐 French ⚖ 132 KB

## Abstract Entecavir, labeled as 1H‐[^13^C~4~]purin‐6(9H)‐one, was prepared from commercially available [^13^C]guanidine HCl, 1 and diethyl [1,2,3‐^13^C~3~]malonate, 2. The reagents were condensed together to give 2‐amino‐4,6‐dichloro[2,4,5,6‐^13^C~4~]pyrimidine 3, which in turn was coupled to an

Synthesis of [8-14C]-2,6-dichloro-9H-pur
Synthesis of [8-14C]-2,6-dichloro-9H-purine, a radiolabelled precursor for 14C-nucleosides
✍ Jacob S. Valsborg; Lars J. S. Knutsen; Inge Lundt; Christian Foged 📂 Article 📅 1995 🏛 John Wiley and Sons 🌐 French ⚖ 321 KB

The synthesis of [8-'4C]-2,6-dichloro-9H-purine (z), a radiolabelled precursor for preparing ''C-labelled nucleosides, is described. Triethyl ['4C]orthoformate was reacted with 4,5-diamino-2,6-dichloropyrimidine (1) in acetonitrile at 90°C with methanesutfonic acid as catalyst to generate 2 in 84% r