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Syntheses of 4(R)-silyloxy-6(S)-iodomethyl-tetrahydropyran-2-one and its enantiomer, building blocks for HMG-COA reductase inhibitors

✍ Scribed by E Baader; W Bartmann; G Beck; A Bergmann; H.-W Fehlhaber; H Jendralla; K Kesseler; R Saric; H Schüssler; V Teetz; M Weber; G Wess


Publisher
Elsevier Science
Year
1988
Tongue
French
Weight
176 KB
Volume
29
Category
Article
ISSN
0040-4039

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✦ Synopsis


Optically pure 4(R),6(S)-iodolactone 1 was obtained from a-D-(+)-glucose in 17 steps with 17% overall yield. Its enantiomere4(S),6(R)-iodolactone 1' was obtained from acetonedicarboxylic acid in 9 steps in 37% overall yield and witTi_70% ee. Key steps in the synthesis of 1' are enzyme (PLE)-catalyzed saponification of prochiral di-n-propyl-3-hydroxyglutarze 2 and iodolactonization of 11 -* R= (tert.-Bu)SiPh2

The enantiomeric iodolactones 1 and