𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Syntheses of AZ12320927 labeled with H-3, C-14, and H-2

✍ Scribed by Charles S. Elmore; Mark E. Powell; J. Richard Heys

Publisher
John Wiley and Sons
Year
2008
Tongue
French
Weight
123 KB
Volume
51
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

In support of a program to develop a treatment for depression, three isotopically labeled forms of the 5‐HT~1B~ antagonist AZ12320927 were synthesized. A tritium labeled version was synthesized for autoradiography using Ir‐catalyzed hydrogen–tritium exchange. A C‐14 labeled version was prepared for use in metabolism studies in four‐steps from [u‐^14^C]p‐nitrophenol. A stable isotope labeled version was synthesized for use as an internal standard for LC/MS/MS quantitation in two steps from chromenone 1. Copyright © 2008 John Wiley & Sons, Ltd.

📜 SIMILAR VOLUMES

Economical syntheses of 3H-2H and 14C-la
Economical syntheses of 3H-2H and 14C-labeled ethyl acetates
✍ Francisco J. Alvarez; Ildiko M. Kovach; Richard L. Schowen 📂 Article 📅 1982 🏛 John Wiley and Sons 🌐 French ⚖ 165 KB

## Abstract Tritium and ^14^C‐labeled isomers of ethyl acetate are excellent substrates for competitive dual‐labeled radioactive isotopic measurements of β‐deuterium and β‐tritium isotope effects. Methods are given for preparation of the ethyl esters of acetic acid‐2‐^3^H, acetic acid‐2‐^14^C, and

Syntheses of [2H3, 15N], [14C]Nexavar™ a
Syntheses of [2H3, 15N], [14C]Nexavar™ and its labeled metabolites
✍ U. Pleiss; M. Gerisch; D. Seidel 📂 Article 📅 2006 🏛 John Wiley and Sons 🌐 French ⚖ 150 KB 👁 1 views

Nexavar TM , Sorafenib tosylate (BAY 43-9006 tosylate) is a potent small molecule Raf kinase inhibitor for the treatment of hyperproliferative disorders such as cancer. Both radiolabeled and stable isotope labeled compounds were required for drug absorption, distribution, metabolism and excretion (A

Syntheses of 14C and 3H labelled forms o
Syntheses of 14C and 3H labelled forms of donetidine - A histamine H2-antagonist
✍ M A Armitage; M M Cashyap; D Saunders 📂 Article 📅 1987 🏛 John Wiley and Sons 🌐 French ⚖ 440 KB

Three syntheses o f r a d i o l a b e l l e d 2-[2-(2-N.N-Dlmethylarnlnomethyl-5 -f uranyl-methyl thlo)ethylamlno]-5-( 6-hydroxy-l-plcolyl ) -4pyrlmldone t r i h y d r o c h l o r l d e (donetldlne t r i h y d r o c h l o r i d e ) are described. One descrlbes the preparatlon o f the f r e e base, a

Synthesis of 14C-labeled and 2H-labeled
Synthesis of 14C-labeled and 2H-labeled dibucaine
✍ Naba K. Chaudhuri 📂 Article 📅 1985 🏛 John Wiley and Sons 🌐 French ⚖ 329 KB 👁 1 views

A synthesis of dibucaine labeled with l"C in the heterocyclic ring is described. starting with isatin and acetic anh~dride-2-~"C as shown in Scheme I. Two deutero analogs, dibucaine-d2 and dibucaine-dg, were also synthesized by the reactions shown in Scheme 11. Dibucaine-dg was synthesized by conden

Synthesis of 2H, 3H and 14C labelled Sch
Synthesis of 2H, 3H and 14C labelled Sch 40120
✍ D. Hesk; T. Duelfer; S. Hickey; D. Hochman; D. Koharski; P. McNamara; S. Saluja 📂 Article 📅 1994 🏛 John Wiley and Sons 🌐 French ⚖ 376 KB

## 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

Synthesis of 2H- and 14C-labeled fexinid
Synthesis of 2H- and 14C-labeled fexinidazole and its primary metabolites labeled with 2H
✍ E. Fontana; Alberto Pignatti; Serena Venegoni; Michael A. Bray 📂 Article 📅 2011 🏛 John Wiley and Sons 🌐 French ⚖ 419 KB

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