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Structural Variations of Piritrexim, a Lipophilic Inhibitor of Human Dihydrofolate Reductase: Synthesis, Antitumor Activity and Molecular Modeling Investigations.

โœ Scribed by Mario Zink; Harald Lanig; Reinhard Troschuetz


Publisher
John Wiley and Sons
Year
2005
Weight
26 KB
Volume
36
Category
Article
ISSN
0931-7597

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An alternative synthesis of piritrexim,
โœ Reinhard Troschรผtz; Mario Zink; Rainer Gnibl ๐Ÿ“‚ Article ๐Ÿ“… 1999 ๐Ÿ› Journal of Heterocyclic Chemistry ๐ŸŒ English โš– 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 ฮฒโ€chlorocrotonaldehydes 3__E/Z__, which were reacted with cyanoacetamide (6) in the presence of sodium hydride t