𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Carbon-14 labeling of a trifluoromethoxy group: synthesis of a substance P antagonist

✍ Scribed by Conrad E. Raab; Dennis C. Dean; David G. Melillo

Publisher
John Wiley and Sons
Year
2001
Tongue
French
Weight
149 KB
Volume
44
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

Synthesis of a carbon‐14 labeled trifluoromethoxy group has been accomplished using the stepwise oxidative fluorination–desulfurization of a readily prepared [^14^C]xanthate (5). This novel labeling procedure allowed a rapid synthesis of substance P antagonist candidate 1 that avoided potentially more complex ring‐labeling procedures. Similar procedures have been used to prepare C‐14 labeled trifluoromethyl and trifluoromethylamine groups. Copyright © 2001 John Wiley & Sons, Ltd.

📜 SIMILAR VOLUMES

Synthesis of carbon-14 labeled LTD4 anta
Synthesis of carbon-14 labeled LTD4 antagonist MK-571
✍ Dennis C. Dean; David G. Melillo; Robert L. Ellsworth 📂 Article 📅 1991 🏛 John Wiley and Sons 🌐 French ⚖ 289 KB

The synthesis of (E)-5-(3-(2-(7-~hloroquinolin-2-yl)ethenyl)-phen~l)-[5-~~C]-4,6-dith~anonane dicarboxylic acid N.Ndimethylamide (I1 4C]MK-571), a high-allinity LTD4 antagonist , from sodium [ l 4C]cyanide via a five step sequence is described. Condensation of 3-[14C]cyanobenzaldehyde with 7-chloroq

Synthesis of carbon-14 labeled pyraoxyst
Synthesis of carbon-14 labeled pyraoxystrobin, a novel fungicide
✍ Xun-yue Liu; Qing-fu Ye; Deng-lei Kan; Zheng Zhang; Xing-cheng Ding 📂 Article 📅 2011 🏛 John Wiley and Sons 🌐 French ⚖ 239 KB

SYP‐3343, (__E__)‐2‐(2‐((3‐(4‐chlorophenyl)‐1‐methyl‐1H‐pyrazole‐5‐yloxy)methyl)) phenyl)‐3‐methoxyacrylate, is a novel fungicide with broad‐spectrum and high activity against fungi. In this paper, radioactive pyraoxystrobin, labeled in the pyrazole ring system was achieved from ^14^C labeled 4‐chlo

Synthesis of 14C-labelled CGS 19755, a s
Synthesis of 14C-labelled CGS 19755, a selective NMDA antagonist
✍ Alban J. Allentoff; Mahesh Desai; Bohdan Markus; Timothy Duelfer 📂 Article 📅 1996 🏛 John Wiley and Sons 🌐 French ⚖ 462 KB 👁 1 views

CGS 19755 is a selective NMDA (N-methyl-D-aspartate) antagonist presently under development as a neuronal protecting agent after stroke and head trauma. It was synthesized with 1%-labelling in the carboxylic acid side chain via the synthetic route displayed in Scheme 1. Key steps in the synthesis in

Synthesis of carbon-14 labelled xenalipi
Synthesis of carbon-14 labelled xenalipin - a potential hypolipidemic agent
✍ John A. Hill; John F. Eaddy 📂 Article 📅 1992 🏛 John Wiley and Sons 🌐 French ⚖ 288 KB 👁 1 views

## Abstract Xenalipin 1 (4′‐trifluoromethyl‐2‐biphenylcarboxylic acid) was synthesized in the [^14^C]‐labelled form with specific activity 21.0 mCi/mmol suitable for metabolism and distribution studies in animals. The synthetic sequence involved conversion of [^14^C]‐ benzoic acid to the 4,4‐dimeth

Synthesis of carbon-14 labelled piritrex
Synthesis of carbon-14 labelled piritrexim - a potential anticancer agent
✍ John A. Hill; James C. Wisowaty; Michael E. Darnofall 📂 Article 📅 1993 🏛 John Wiley and Sons 🌐 French ⚖ 493 KB 👁 1 views

## Abstract Piritrexim 1(2,4‐diamino‐6‐(2,5‐dimethoxybenzyl)‐5‐methylpyrido[2,3‐__d__]‐pyrimidine) was synthesized in the [^14^C]‐labelled form with specific activity 50.8 mCi/mmol suitable for drug metabolism, transport, dispostion and mechanism of action studies. The synthetic sequence involved s