Lactone Pathway to Statins Utilizing the Wittig Reaction. The Synthesis of Rosuvastatin

[摘要]：The first entry to statins via lactonized side chain is reported, exemplified by the synthesis of rosuvastatin. The key step is Wittig coupling of (2S,4R)-4-(tert-butyldimethylsilyloxy)6-oxotetrahydro-2H-pyran-2-carbal dehyde and phosphonium salt of an appropriately functionalized pyrimidine heterocycle. One-pot deprotection and hydrolysis of the resulting 4-O-TBS rosuvastatin lactone provided rosuvastatin in high yield.

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