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Model reactions targeted at the synthesis of carbon-14 labeled CI-996, a potent antagonist of angiotensin II receptor (1)

✍ Scribed by I. Victor Ekhato; Che C. Huang

Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
361 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A reaction sequence suitable for the preparation of an analog of 2‐propyl‐1‐[2′‐(1H‐tetrazol‐5‐yl)[1,1′‐biphenyl]‐4‐yl]methyl‐4‐[2‐(trifluoroacetyl)‐1H‐pyrrol‐1‐yl]‐1H‐imidazole‐5‐carboxylic acid, with ^14^C at the methylene bridge was developed. The would‐be labeled fragment (12) was derived from 4‐iodobenzenemethanol (6), which itself was constructed from 1,4‐dibromobenzene by the application of silicon chemistry. Pd° catalyzed coupling of TBDMS protected 6 and a tetrazole borate 10 gave the compound 12 which upon further transformation to the mesylate 13, N‐alkylated an imidazole to furnish target compound.

📜 SIMILAR VOLUMES

Carbon-11 labeling of a potent, nonpepti
Carbon-11 labeling of a potent, nonpeptide, at1-selective angiotensin-II receptor antagonist: MK-996
✍ William B. Mathews; H. Donald Burns; Robert F. Dannals; Hayden T. Ravert; Elizab 📂 Article 📅 1995 🏛 John Wiley and Sons 🌐 French ⚖ 415 KB 👁 1 views

## Abstract [α‐^11^C]Benzoyl chloride was synthesized and purified by normal phase HPLC. [^11^C]MK‐996 ([^11^C]__N__‐[[4′[(2‐ethyl‐5,7‐dimethyl‐3H‐imidazo [4,5‐b]pyridin‐3‐yl)methyl][1,1′‐biphenyl]‐2‐yl]sulfonyl]‐benzamide), a potent and selective ligand for the AT~1~ receptor, was prepared by __N_