期刊
MOLECULES
卷 28, 期 10, 页码 -出版社
MDPI
DOI: 10.3390/molecules28104067
关键词
sclareolide; Mannich reaction; aldmine; antifungal activity
Sclareolide was developed as an efficient C-nucleophilic reagent for an asymmetric Mannich addition reaction with N-tert-butylsulfinyl aldimines. The reaction exhibited high yields and diastereoselectivities, even on a gram scale. The resulting Mannich addition products could be deprotected to obtain sclareolide derivatives with a free N-H group, which showed considerable antifungal activity against forest pathogenic fungi in vitro.
Sclareolide was developed as an efficient C-nucleophilic reagent for an asymmetric Mannich addition reaction with a series of N-tert-butylsulfinyl aldimines. The Mannich reaction was carried out under mild conditions, affording the corresponding aminoalkyl sclareolide derivatives with up to 98% yield and 98:2:0:0 diastereoselectivity. Furthermore, the reaction could be performed on a gram scale without any reduction in yield and diastereoselectivity. Additionally, deprotection of the obtained Mannich addition products to give the target sclareolide derivatives bearing a free N-H group was demonstrated. In addition, target compounds 4-6 were subjected to an antifungal assay in vitro, which showed considerable antifungal activity against forest pathogenic fungi.
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