Development of a Practical Process for the Synthesis of PDE4 Inhibitors

Development of a Practical Process for the Synthesis of PDE4 Inhibitors

A practical, safe, and efficient process for the synthesis of PDE4 (phosphodiesterase type 4) inhibitors represented by 1 and 2 was developed and demonstrated on a multi-kilogram scale. Key aspects of the process include the regioselective synthesis of dihydrothieno­[3,2-d]­pyrimidine-2,4-diol 9 and...

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Veröffentlicht in:Organic process research & development 2016-05, Vol.20 (5), p.982-988
Hauptverfasser: Frutos, Rogelio P, Tampone, Thomas G, Mulder, Jason A, Rodriguez, Sonia, Yee, Nathan K, Yang, Bing-Shiou, Senanayake, Chris H
Format: Artikel
Sprache:eng
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Zusammenfassung:A practical, safe, and efficient process for the synthesis of PDE4 (phosphodiesterase type 4) inhibitors represented by 1 and 2 was developed and demonstrated on a multi-kilogram scale. Key aspects of the process include the regioselective synthesis of dihydrothieno­[3,2-d]­pyrimidine-2,4-diol 9 and the asymmetric sulfur oxidation of intermediate 11.
ISSN:1083-6160
1520-586X
DOI:10.1021/acs.oprd.6b00104