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Synthesis of a tumor‐growth inhibitor‐dihydrochloride of 1‐nitro‐9‐/dimethylamino‐propylamino/‐acridine/C‐283/tritium labelled in the acridine ring and 14 C‐labelled in the side chain
Author(s) -
Kołodziejczyk A.,
Arendt A.
Publication year - 1975
Publication title -
journal of labelled compounds
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0022-2135
DOI - 10.1002/jlcr.2590110313
Subject(s) - acridine , tritium , chemistry , nitro , pyridinium , aniline , ring (chemistry) , tritiated water , stereochemistry , medicinal chemistry , organic chemistry , alkyl , physics , nuclear physics
1‐Nitro‐9/dimethylaminopropylamino/‐acridine dihydro‐chloride /C‐283, ‘Ledaarin’/ is used as an anti‐twnor drug, In view of the studies on its mechanism of action. the syntheses of two specimens of this compound labelled with radioisotopes have been carried out. One of them contained C 14 in the side chain and the other tritiwn in the acridine ring. 3‐Dimethylaminopropylamine /1‐C 14 / prepared on the basis of K 14 was used as the initial substrate for the synthesis of C‐283 labelled with 14 C. It was condensed with pyridinium salt of 1‐nitro‐9‐chloroacridine. In order to introduce tritium to the acridine ring, m‐nitro‐aniline was tritiated in the aaidia solution of tritiated water. Thus obtained tritiated m‐nitroaniline was condensed by Ullman's method with o‐ahlorobenzoia acid. The N‐/3′‐nitrophenyl/anthranilia acid was then converted to the derivative of 1‐nitro‐9‐chloroacridine /2,3,4‐T 3 /. The specific activity of C‐283 14 C labelled was 5.5 mCi/mmole and that of C‐283 tritium labelled 103 mCi/mmole.