Improved and Scalable Preparation of 6-Bromo-4-Chlorothieno[2,3-d]Pyrimidine

Improved and Scalable Preparation of 6-Bromo-4-Chlorothieno[2,3-d]Pyrimidine

A practical, robust and scalable synthesis of 6-bromo-4-chlorothieno[2,3-d]pyrimidine starting from cheap bulk chemicals has been developed. The method involves four synthetic steps: Gewald reaction, pyrimidone formation, bromination, and chlorination. The process relies on standard laboratory equip...

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Veröffentlicht in:Chemistry of heterocyclic compounds (New York, N.Y. 1965) N.Y. 1965), 2014-11, Vol.50 (8), p.1177-1187
Hauptverfasser: Bugge, S., Skjønsfjell, E. M., Willumsen, F. B., Sundby, E., Hoff, B. H.
Format: Artikel
Sprache:eng
Schlagworte:
Chemistry
Chemistry and Materials Science
Organic Chemistry
Pharmacy
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Beschreibung
Zusammenfassung:A practical, robust and scalable synthesis of 6-bromo-4-chlorothieno[2,3-d]pyrimidine starting from cheap bulk chemicals has been developed. The method involves four synthetic steps: Gewald reaction, pyrimidone formation, bromination, and chlorination. The process relies on standard laboratory equipment, allowing to obtain the product in an overall yield of 49% without using chromatography for purification of the product and intermediates.
ISSN:0009-3122
1573-8353
DOI:10.1007/s10593-014-1579-z