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ChemInform Abstract: An Alternative Synthesis of Piritrexim, a Lipophilic Inhibitor of Human Dihydrofolate-Reductase.

✍ Scribed by Reinhard Troschuetz; Mario Zink; Rainer Gnibl


Publisher
John Wiley and Sons
Year
2010
Weight
32 KB
Volume
30
Category
Article
ISSN
0931-7597

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An alternative synthesis of piritrexim,
✍ Reinhard TroschΓΌtz; Mario Zink; Rainer Gnibl πŸ“‚ Article πŸ“… 1999 πŸ› Journal of Heterocyclic Chemistry 🌐 English βš– 308 KB

## Abstract An alternative synthesis of the lipophilic antifolate piritrexim (1) is outlined. Starting from ketone 2, treatment with phosphorus oxychloride and dimethylformamide gave the β‐chlorocrotonaldehydes 3__E/Z__, which were reacted with cyanoacetamide (6) in the presence of sodium hydride t