Synthesis of two series of pyrazolic analogues of the marine alkaloids granulatimide and isogranulatimide as potent Checkpoint 1 kinase inhibitors
✍ Scribed by Sébastien Deslandes; Stefan Chassaing; Evelyne Delfourne
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- French
- Weight
- 171 KB
- Volume
- 51
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
Two series of regioisomeric pyrazolic analogues of the marine alkaloids granulatimide and isogranulatimide were prepared. The synthesis of the first series was based on the condensation reaction of diversely 5-substituted 3-bromoindoles with pyrazole followed by addition of the intermediates on dibromomaleimide, the so-obtained acyclic adducts being finally photochemically cyclised to the desired analogues. Compounds of the second series were obtained by reacting different 5-substituted-indole-3-glyoxylates with N-Boc-pyrazole-3-acetamide and subsequent photochemical cyclisation of the adducts.