期刊
ORGANIC LETTERS
卷 14, 期 12, 页码 3222-3225出版社
AMER CHEMICAL SOC
DOI: 10.1021/ol301332f
关键词
-
资金
- NSERC (Canada)
- FQRNT (Quebec)
A new approach to the synthesis of Tekturna, a recently marketed drug for hypertension, takes advantage of a modified protocol of the Stoltz palladium-catalyzed asymmetric allylation with a f-BuPHOX ligand for the synthesis of allylated acyclic alkyl aryl ketones. The method led to an alpha-isopropyl alpha-allyl aryl ketone in 90% yield and 88 to 91% ee, which was used in the synthesis of an advanced intermediate toward Tekturna. A beneficial effect of protic additives, such as BHT (2,6-di-tert-butyl-p-cresol), on the time and enantioselectivity of the reaction was discovered.
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