期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 75, 期 19, 页码 6681-6684出版社
AMER CHEMICAL SOC
DOI: 10.1021/jo101050z
关键词
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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-carbaldehyde 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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