Synthesis of the potent immunosuppressive agent, mycophenolate mofetil (I) labelled with carbon-14 is described. Methoxyethoxymethyl (MEM) protected mycophenolate norbromide (2) was prepared from unlabelled mycophenolic acid (2) using a modified Hunsdiecker reaction. A three step synthesis furnished
Synthesis of the antiinflammatory prodrug RS-42169-14C
β Scribed by Howard Parnes; Glenn T. Huang
- Publisher
- John Wiley and Sons
- Year
- 1995
- Tongue
- French
- Weight
- 281 KB
- Volume
- 36
- Category
- Article
- ISSN
- 0022-2135
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β¦ Synopsis
A facile synthesis of the antiinflammatory agent RS-42169-14C, based on a carbonation/cycloaddition sequence is described. The product was obtained in 36% yield from Ba14CO3 at a specific activity of 52 mCilmmole. The design of the six step sequence was such that pure intermediates were isolated by extractive workup, and only a single chromatographic purification was required.
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The Hantzsch synthesis has been applied to the general prepararion of 4-aryl-dihydropyridines labelled in the metabolically stable 4-position of the dihydropyridine ring. The synthesis is based on the preparation of a key common intermediate, m-nirr~benzaldehyde-[formyl-~~C], in high yield from Ba14
Two isotopic isomers of tenidap, a novel antiinflammatory agent, were prepared. Compound 6 (specific activity = 10.24 rnCi/rnmol), having 1% in the indole ring, was prepared in three steps (52% overall yield) starting from 1 H-[14C]indole-2,3-dione. Compound 11 (specific activity = 57.1 6 mCi/mmol,
We report here a facile synthesis of (RS) methyl-2-([2 0 -14 C]4,6-dimethoxypyrimidin-2 0yloxy)-2-phenyl [1-14 C]ethanoate under microwave irradiation.