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Synthesis of a (+)-anatoxin-a analogue for monoclonal antibodies production |
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| Authors: | Mickael Marc Pierre-Yves Renard Xavier Franck |
| Affiliation: | a UMR-CNRS6014 & FR3038 COBRA, Université de Rouen, INSA de Rouen, IRCOF, 1 rue Tesnière, 76130 Mont Saint Aignan, France b CEA iBiTecS, Service de Pharmacologie et d’Immunoanalyse, Gif sur Yvette F-91191, France |
| Abstract: | Anatoxin-a analogue was prepared by resolution of aminoacid 1 using chiral (R)-4-phenyl-oxazolidin-2-thione as derivatizing agent. X-ray diffraction of a diastereomer allowed us to determine its absolute configuration. The synthesis could then be completed in few steps followed by introduction of an amide linker bearing a terminal alkyne in order to attach a carrier protein for monoclonal antibodies production. |
| Keywords: | Anatoxin Aminoacid resolution Monoclonal antibodies Toxin analogue |
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