88655-02-1Relevant academic research and scientific papers
Diastereoselective synthesis of (±)-heliotropamide by a one-pot, four-component reaction
Younai, Ashkaan,Chin, Gregory F.,Shaw, Jared T.
experimental part, p. 8333 - 8336 (2011/02/28)
The first synthesis of heliotropamide is reported. The preparation of this 2-oxopyrrolidine (γ-lactam) natural product relied on a diastereoselective one-pot, four-component reaction (4CR) for the assembly of the core structure. On the basis of chemical shift correlation and NOESY experiments, the previously unknown alkene geometry of heliotropamide is assigned as E.
Total synthesis of (±)-armepavines and (±)-nuciferines from (2-nitroethenyl)benzene derivatives
Chang, Chia-Fu,Huang, Chu-Yun,Huang, Yu-Chao,Lin, Kuan-Yu,Lee, Yean-Jang,Wang, Chau-Jong
experimental part, p. 3452 - 3466 (2011/02/22)
A concise route to armepavine 1 and nuciferine 2 and 3, which can be isolated from the leaves of Nelumbo nucifera (Nymphaceae), has been achieved in which the longest linear sequence is only six steps from commercially available benzaldehyde in 28%, 21%, and 20% overall yield, respectively. The key transformations in the synthesis are the radical cyclization of aryl bromide with Bu3SnH and the Pictet-Spengler reaction of N-substituted amine with aldehyde. Copyright Taylor & Francis Group, LLC.
3-AMIDINOBENZENESULFONAMIDE DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES IN THE PRODUCTION THEREOF
-
Page 12, (2008/06/13)
The present invention relates to 3-amidinobenzenesulfonamide derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a hydroxy group; Y represents a single bond or an oxygen atom; and R2 represents a lower alkyl group or a group represented by the general formula: (wherein n represents 1 or 2; and T represents a hydrogen atom, a lower acyl group, a halo (lower acyl) group or a group represented by the general formula:-C(=NH)-W (wherein W represents a lower alkyl group)), and pharmaceutically acceptable salts thereof, which have an excellent activated blood coagulation factor X inhibitory activity and are useful as activated blood coagulation factor X inhibitors, and to pharmaceutical compositions comprising the same and intermediates thereof.
