476014-77-4Relevant academic research and scientific papers
OXAZOLIDONE COMPOUND, PREPARING METHOD AND APPLICATION THEREOF
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Paragraph 0241; 0242; 0243, (2015/12/08)
The present invention relates to the field of a pharmaceutical compound, and more specifically, relates to a new oxazolidone compound, an enantiomer, a diastereoisomer and a raceme thereof, and a mixture thereof, and a pharmaceutically acceptable salt thereof, a preparation method thereof, an application thereof as a bioactive substance in a drug. The compound in the present invention has strong anticoagulant activity, does not affect the activity of thrombin, and can reduce the risk of hemorrhage. A pharmacokinetics experiment shows that the compound in the present invention further has good metabolic characteristics, and has a far better oral bioavailability than a positive contrastive agent rivaroxaban.
PIPERIDINYL INDOLE DERIVATIVES AND THEIR USE AS COMPLEMENT FACTOR B INHIBITORS
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Page/Page column 105, (2015/02/02)
The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitors of the complement alternative pathway, in particular of Factor B. The present invention further p
Stereoselective synthesis of (2S,4R)-4-hydroxypipecolic acid
Occhiato, Ernesto G.,Scarpi, Dina,Guarna, Antonio
, p. 524 - 531 (2008/09/18)
A new synthetic route to enantiopure (2S,4R)-4-hydroxypipecolic acid from commercial ethyl (3S)-4-chloro-3-hydroxybutanoate is reported. The synthesis is based on the Pd-catalyzed methoxycarbonylation of a 4-alkoxy-substituted δ-valerolactam-derived vinyl triflate followed by the stereocontrolled hydrogenation of the enamine double bond. The final product was obtained after exhaustive hydrolysis in 20 % yield over 10 steps. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
A stereodivergent approach to substituted 4-hydroxypiperidines
Vink, Mandy K. S.,Schortinghuis, Christien A.,Luten, Jordy,Van Maarseveen, Jan H.,Schoemaker, Hans E.,Hiemstra, Henk,Rutjes, Floris P. J. T.
, p. 7869 - 7871 (2007/10/03)
A stereodivergent route toward both diastereomeric forms of functionalized 4-hydroxypiperidines has been successfully developed. This route involves biocatalytic generation of the enantiopure starting materials followed by functionalization via N-acyliminium ion-mediated CC-bond formation.
