𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis of 3H and 14C labeled (S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indol-2-one, maxipost™. An agent for post-stroke neuroprotection

✍ Scribed by Douglas D. Dischino; Valentin K. Gribkoff; Piyasena Hewawasam; George M. Luke; J. Kent Rinehart; Tony L. Spears; John E. Starrett Jr

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
113 KB
Volume
46
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

The syntheses of tritium labeled (S)‐3‐(5‐chloro‐2‐[OC^3^H~3~]methoxyphenyl‐1,3‐dihydro‐3‐fluoro‐6‐(trifluoromethyl)‐1H‐indol‐2‐one, and carbon‐14 (S)‐3‐(5‐chloro‐2‐methoxyphenyl)‐1,3‐dihydro‐3‐fluoro‐6‐(trifluoromethyl)‐2H‐[2,3‐^14^C~2~] indol‐2‐one are reported. The ^3^H‐labeled compound was prepared in a two‐step synthesis from C^3^H~3~I. The final product was purified via chiral HPLC to yield the desired enantiomer in a 4% radiochemical yield and a specific activity of 60 Ci/mmol. The ^14^C‐labeled compound was prepared in a four‐step synthesis from diethyl [carboxylate‐^14^C~1~,~2~] oxalate. The final product was purified via chiral HPLC to yield the desired enantiomer in a 20% radiochemical yield and a specific activity of 28.4 μCi/mg. Copyright © 2002 John Wiley & Sons, Ltd.

📜 SIMILAR VOLUMES

Synthesis of 14C- and 2H-labeled 1,3-dih
Synthesis of 14C- and 2H-labeled 1,3-dihydro-3,3-dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2H-indol-2-one (LY195115), an orally effective positive inotrope
✍ David W. Robertson; Joseph H. Krushinski; Don Kau 📂 Article 📅 1986 🏛 John Wiley and Sons 🌐 French ⚖ 437 KB 👁 1 views

We have synthesized 14C-and 2H-labeled 1,3-dihydro-3,3dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2H\_-indol-2one (LY195115), an extremely potent, orally-effective cardiotonic with inotropic and vasodilator activities. '\*C-label was introduced in the antepenultimate step by reaction of a B-

Synthesis of isotopically labelled [3-14
Synthesis of isotopically labelled [3-14C]- and [3,3-2H2]-5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), a new antifungal agent for the potential treatment of onychomycosis
✍ Stephen J. Baker; Yong-Kang Zhang; Tsutomu Akama; Conrad Wheeler; Jacob J. Platt 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 French ⚖ 113 KB

## Abstract 5‐Fluoro‐1,3‐dihydro‐1‐hydroxy‐2,1‐benzoxaborole (AN2690) is a new antifungal agent for the potential treatment of onychomycosis. During the preclinical development phase, it was necessary to synthesize the radioisotope [3‐^14^C]‐5‐fluoro‐1,3‐dihydro‐1‐hydroxy‐2,1‐benzoxaborole and the

The synthesis of 7-chloro-1-methyl-5-phe
The synthesis of 7-chloro-1-methyl-5-phenyl-1, 3-dihydro-2H-1,4-benzodiazepin-2-one-5-14C and 7-nitro-1-methyl-5-(2′-fluorophenyl)-1, 3-dihydro-2H-1,4-benzodiazepin-2-one-5-14C
✍ H. H. Kaegi; W. Burger; C. J. Bader 📂 Article 📅 1982 🏛 John Wiley and Sons 🌐 French ⚖ 393 KB 👁 1 views

## Abstract Two benzodiazepines, Diazepam and Flunitrazepam, labeled with carbon‐14 in position 5 of the diazepine ring have been synthesized. Use of a condensation between iminochlorides and ^14^C‐benzonitriles, followed by exhaustive methylation of the resulting quinazolines and hydrolyses is des

Synthesis of carbon-14 labeled 1,4-benzo
Synthesis of carbon-14 labeled 1,4-benzodiazepines. III. 2-allyloxy-amino-7-chloro-5-(2-chlorophenyl)-3h-l,4-benzodiazepine-2-14C, 8-chloro-1-dimethylamino-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-3a-14C, and 8-chloro-2,4-dihydro-2-methyl-6-phenyl-1H-s-triazolo[4,3-a] [1,4]benzodiazepin-l-one-3a-14
✍ Richard S. P. Hsi; Tommy D. Johnson 📂 Article 📅 1976 🏛 John Wiley and Sons 🌐 French ⚖ 281 KB 👁 1 views

## Abstract A group of radioactive 1,4‐benzodiazepine derivatives have been synthesized from glycine‐1‐^14^C. The subject compounds are labeled with carbon‐14 in the 2‐position of the 1,4‐benzodiazepine ring system.

Synthesis of 13C, 14C and 2H13C labeled
Synthesis of 13C, 14C and 2H13C labeled adrenoceptor antagonists: 6-chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine hydrochloride and its N-desmethyl analog
✍ A. J. Villani; F. Etzkorn; G. A. Rotert; J. R. Heys 📂 Article 📅 1988 🏛 John Wiley and Sons 🌐 French ⚖ 428 KB 👁 1 views

The compound 6-chloro-2,3,4,5-tetrahydroi~-methyl-l &3-t#nzazepine (SK&F 86466) was prepared in phenyl-U-C and phenyl-C , labeled forms in a six step sequence beginning with the appropriately labeled benzenes. In addition, the N-desmeJhyl analog of the carbon-1 4 labeled isotopomer and the N-methyl-