Tetrahedron

Concise and highly efficient approach to three key pyrimidine precursors for rosuvastatin synthesis

D Šterk, Z Časar, M Jukič, J Košmrlj

Index: Sterk, Damjan; Casar, Zdenko; Jukic, Marko; Kosmrlj, Janez Tetrahedron, 2012 , vol. 68, # 9 p. 2155 - 2160

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Citation Number: 18

Abstract

We report the synthesis of 5-formyl-, 5-(hydroxymethyl)-, and 5-(bromomethyl) substituted N- [4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide. The presented synthetic approach is based on highly efficient three step preparation of functionalized 5- methylpyrimidine. The methyl group is selectively brominated by NBS with irradiation into the bromomethyl derivative, which is then transformed into the hydroxymethyl or formyl ...