Highly Efficient Synthesis of a Staphylococcus aureus Targeting Payload to Enable the First Antibody-Antibiotic Conjugate was written by Linghu, Xin;Segraves, Nathaniel L.;Abramovich, Ifat;Wong, Nicholas;Mueller, Barbara;Neubauer, Nadja;Fantasia, Serena;Rieth, Sebastian;Bachmann, Stephan;Jansen, Michael;Sowell, C. Gregory;Askin, David;Koenig, Stefan G.;Gosselin, Francis. And the article was included in Chemistry – A European Journal in 2018.Application In Synthesis of N,N-Dimethylpiperidin-4-amine This article mentions the following:
A practical synthesis of the complex payload for an anti-Staphylococcus aureus THIOMABTM antibody-antibiotic conjugate (TAC) is described. The route takes advantage of a delicate oxidative condensation, achieved using a semi-continuous flow procedure. It allows for the generation of kilogram quantities of a key intermediate to enable a mild nucleophilic aromatic substitution to the tertiary amine free drug. The linker component is introduced as a benzylic chloride, which allows formation of the quaternary ammonium salt linker-drug. This chem. process surmounts numerous synthetic challenges and navigates deeply colored and unstable compounds to support clin. studies to counter S. aureus bacterial infections. In the experiment, the researchers used many compounds, for example, N,N-Dimethylpiperidin-4-amine (cas: 50533-97-6Application In Synthesis of N,N-Dimethylpiperidin-4-amine).
N,N-Dimethylpiperidin-4-amine (cas: 50533-97-6) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application In Synthesis of N,N-Dimethylpiperidin-4-amine
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem