Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl) ethyl]-2H-pyran 2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing …

BD Roth, CJ Blankley, AW Chucholowski…

文献索引：Roth, B. D.; Blankley, C. J.; Chucholowski, A. W.; Ferguson, E.; Hoefle, M. L.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 357 - 366

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被引用次数: 145

摘要

19 (a) LiAlH,, ether-dichloromethane, reflux;(b) Et3SiH, TFA-CHpC12, 0 OC;(c) p-TSA, acetone-water. lactone stereoisomers 3 by (1) Weiler dianion condensation with ethyl acetoacetate,(2) stereoselective reduction to the syn-l, &diol with tributylborane and sodium borohydride,(3) base hydrolysis, and (4) lactonization by refluxing in toluene with azeotropic removal of water (Scheme I). The requisite propionaldehydes 2 were prepared by several ...