Synthesis of a tumor-growth inhibitor-dihydrochloride of 1-nitro-9-/dimethylamino-propylamino/-acridine/C-283/tritium labelled in the acridine ring and 14C-labelled in the side chain
✍ Scribed by A. Kołodziejczyk; A. Arendt
- Publisher
- John Wiley and Sons
- Year
- 1975
- Tongue
- French
- Weight
- 362 KB
- Volume
- 11
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
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.