𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis of [14C]-labelled tolrestat(N-[[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]-[14C]thioxomethyl]-N-methylglycine; AY-27, 773)

✍ Scribed by D. R. Hicks

Publisher
John Wiley and Sons
Year
1984
Tongue
French
Weight
265 KB
Volume
21
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

[^14^C]‐Tolrestat(N‐[[5‐(trifluoromethyl)‐6‐methoxy‐1‐naphthalenyl]‐[^14^C]‐thioxomethyl]‐N‐methylglycine; [14C]AY‐27, 773), a new aldose reductase inhibitor, was prepared by incorporating [14C]carbon dioxide. The intermediate, 6‐methoxy‐5‐trifluoromethyl‐[1–14C]‐naphthoic acid, prepared by carbonation of the corresponding lithiated derivative, was condensed with sarcosine methyl ester hydrochloride, converted to the thioamide and hydrolyzed. [14C]Tolrestat, having a specific activity of 52.7 μCi/mg was obtained in 26% overall yield from [14C]barium carbonate and had a radiochemical purity of 97%.

📜 SIMILAR VOLUMES

Synthesis of [14C]-labelled 3-[N-(4-brom
Synthesis of [14C]-labelled 3-[N-(4-bromophenyl)carbamoyl]-7-chloro-4-hydroxycoumarin and 3-[N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]carbamoyl]-7-chloro-4-hydroxycoumarin
✍ Byung H. Lee; Michael F. Clothier 📂 Article 📅 1993 🏛 John Wiley and Sons 🌐 French ⚖ 196 KB 👁 1 views

## Abstract The novel [^14^C]‐labelled 3‐carbamoyl‐4‐hydroxycoumarins were prepared in two steps from 4‐chloro‐acetylsalicyloyl chloride (3). The isotope was incorporated by the reaction of diethyl malonate‐1,3‐^14^C with 4‐chloro‐acetylsalicyloyl chloride (3). Subsequent condensation of the result

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-

Synthesis of [carbonyl-14C]- and (methox
Synthesis of [carbonyl-14C]- and (methoxy-d3)-labeled N-[(2RS, 3RS)-1-benzyl-2-methyl-3-pyrrolidinyl] −5-chloro-2-methoxy-4-(methylamino) benzamide (YM-09151-2). A new potent neuroleptic agent
✍ Kazuharu Tamazawa; Hideki Arima 📂 Article 📅 1984 🏛 John Wiley and Sons 🌐 French ⚖ 485 KB

## Abstract A new potent neuroleptic agent YM‐09151‐2, N‐[(2RS, 3RS)‐1‐benzyl‐2‐methyl‐3‐pyrrolidinyl]‐5‐chloro‐2‐methoxy‐4‐ (methylamino) benzamide (**10c**), was labeled with carbon‐14 and deuterium for biochemical studies such as metabolism and 14 pharmacokinetics. The synthesis of [carbonyl‐^14