728918-75-0Relevant articles and documents
Syntheses of a flobufen metabolite and dapoxetine based on enantioselective allylation of aromatic aldehydes
Hessler, Filip,Korotvicka, Ales,Necas, David,Valterova, Irena,Kotora, Martin
supporting information, p. 2543 - 2548 (2014/05/06)
The enantioselective allylation of an aromatic aldehyde to give a chiral homoallylic alcohol was employed as the key step in the syntheses of a flobufen metabolite and dapoxetine. In the former case, the homoallylic alcohol moiety (99 % ee) was converted into a five-membered lactone ring with good preservation of the optical purity, and the target compound, a flobufen metabolite, was obtained in 95 % ee. In the latter case, the homoallylic alcohol moiety (97 % ee) was transformed over several steps into a 3-aminopropanol moiety. During the course of the synthesis, the gradual loss of optical purity was observed, and the target compound, dapoxetine, was obtained in 85 % ee. The enantioselective allylation of an aromatic aldehyde to give the corresponding homoallylic alcohol was the key step in the syntheses of a flobufen metabolite and dapoxetine. In the first case, the homoallylic moiety was converted into a chiral five-membered lactone ring. In the second case, it was transformed into a chiral 1,3-amino alcohol moiety. Copyright
Phosphonosulfonates are potent, selective inhibitors of dehydrosqualene synthase and staphyloxanthin biosynthesis in staphylococcus aureus
Song, Yongcheng,Lin, Fu-Yang,Yin, Fenglin,Hensler, Mary,Poveda, Carlos A. Rodrígues,Mukkamala, Dushyant,Cao, Rong,Wang, Hong,Morita, Craig T.,Pacanowska, Dolores González,Nizet, Victor,Oldfield, Eric
experimental part, p. 976 - 988 (2009/12/04)
Staphylococcus aureus produces a golden carotenoid virulence factor called staphyloxanthin (STX), and we report here the inhibition of the enzyme, dehydrosqualene synthase (CrtM), responsible for the first committed step in STX biosynthesis. The most acti
