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Asymmetric syntheses of (-)-lentiginosine and an original pyrrolizidinic analogue thereof from a versatile epoxyamine intermediate
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Asymmetric syntheses of (-)-lentiginosine and an original pyrrolizidinic analogue thereof from a versatile epoxyamine intermediate

Tahar Ayad, Yves Génisson et Michel Baltas
Organic & biomolecular chemistry, Vol.3(14), pp.2626-2631
21/07/2005
PMID: 15999197

Résumé

Alkaloids - chemical synthesis Alkaloids - chemistry Amines - chemistry Aspergillus niger - enzymology Epoxy Compounds - chemistry Glucan 1,4-alpha-Glucosidase - chemistry Glucan 1,4-alpha-Glucosidase - drug effects Pyrrolizidine Alkaloids - chemical synthesis Pyrrolizidine Alkaloids - chemistry Pyrrolizidine Alkaloids - pharmacology Stereoisomerism
Ready access to natural (-)-lentiginosine and its pyrrolizidinic analogue from a chiral vinylic epoxyamine in a straightforward five-step sequence is presented. Careful use of the RCM reaction on aminotriols and constitutes the key feature of the synthetic pathway. The alpha-amyloglucosidase inhibitory activities of the target compounds were evaluated and showed that the more easily accessible pyrrolizidinic analogue possesses an inhibitory activity quite similar to that of (-)-lentiginosine.

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