✦ LIBER ✦

Synthesis of tritium labeled mazindol

✍ Scribed by Harry A. Dugger; Kenrick C. Tabot

Publisher: John Wiley and Sons
Year: 1976
Tongue: French
Weight: 326 KB
Volume: 12
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580120312

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✦ Synopsis

Abstract

Mazindol was labeled with tritium in the 6,9 positions in low yield starting with dimethyl phthalate‐3,6‐^3^H which was prepared by reduction of dimethyl 3‐chlorophthalate with tritium gas using 10% palladium on charcoal as a catalyst. The labeled dimethyl phathalate was hydrolisized with extensive loss of the label by exchange and after conversion to phthalic anhydride was condensed with chlorobenzene to give 2‐(p‐chlorobenzoyl) benzoic acid‐3,6‐^3^H. This acid was converted in two steps into 5‐hyddroxy‐54‐imidazo [2,1‐a] isoindol‐6,9‐^3^H (mazindol‐6,9‐^3^H). In a similar fashion, mazindol‐7,8‐^3^H was prepared in higher yields beginning with dimethyl 4‐chlorophthalate. There was no loss of the label during the hydrolysis of dimethyl Phthalate‐4,5‐^3^H.

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