Tricyclo[4.2.2.02,5]dec-9-ene-3,4,7,8-tetracarboxlic acid diimide: Formulation and stability studies
β Scribed by B. Rao Vishnuvajjala; James C. Cradock
- Publisher
- John Wiley and Sons
- Year
- 1986
- Tongue
- English
- Weight
- 344 KB
- Volume
- 75
- Category
- Article
- ISSN
- 0022-3549
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β¦ Synopsis
The experimental antitumor drug, tricycl0[4.2.2.0~~~]dec-9ene-3,4,7,8-tetracarboxylic acid diimide, NSC 284356, was formulated as the disodium salt in a stable freeze-dried form suitable for parenteral administration. The stability of the drug was determined in buffers at various temperatures using liquid chromatography. The drug was found to undergo hydrolysis in aqueous solutions. The rate of hydrolysis followed pseudo-first-order kinetics and is accelerated by increases in temperature and pH of the solutions. The hydrolysis product was isolated, and its structure was determined by unambiguous chemical methods.
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## Abstract 4β[3β[4β(2βMethoxyphenyl)piperazinβ1βyl]propoxy]β4βazaβtricyclo[5.2.1.02,6]decβ8βeneβ3,5βdione (4), a potent and selective 5βHT~1A~ agonist, was labeled by ^11^Cβmethylation of the corresponding desmethyl analogue 3 with ^11^Cβmethyl triflate. The precursor molecule 3 was synthesized fr