ChemInform Abstract: Enantioselective Synthesis of Brinzolamide (AL-4862), a New Topical Carbonic Anhydrase Inhibitor. The “DCAT Route” to Thiophenesulfonamides.

✍ Scribed by Raymond E. Conrow; W. Dennis Dean; Paul W. Zinke; Michael E. Deason; Steven J. Sproull; Anura P. Dantanarayana; Mark T. DuPriest

• Publisher: John Wiley and Sons
• Year: 2010
• Weight: 34 KB
• Volume: 30
• Category: Article
• ISSN: 0931-7597
• DOI: 10.1002/chin.199929157

✦ Synopsis

Enantioselective Synthesis of Brinzolamide (AL-4862), a New Topical Carbonic Anhydrase Inhibitor. The "DCAT Route" to Thiophenesulfonamides.

-A facile large scale synthesis of the topical carbonic anhydrase inhibitors AL-4862 (IXa) and its side chain nor-homologue AL-4623A (IXb) starting from 3-acetyl-2,5-dichlorothiophene (I) (DCAT) is described.