期刊
ORGANIC LETTERS
卷 18, 期 5, 页码 1028-1031出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b00155
关键词
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资金
- 863 Hi-Tech Program of China [2014AA020525]
- National Basic Research Program of China [2014CB541800]
- Shanghai ShuGuang Project [14SG33]
An organocatalytic enantioselective Michael Michael cascade reaction is developed for the synthesis of chiral spirotetrahydrothiopyrans. This highly functionalized scaffold was assembled in moderate to good yield (55-74%) and excellent diastereo- and enantioselectivities (>30:1 dr, >= 99% ee) with the creation of four consecutive stereogenic centers. The novel spiro-oxindole scaffold is validated as a new class of p53-MDM2 protein-protein interaction inhibitors with good antitumor activity.
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