Synthesis and characterisation of asymmetric primaquine and halogenaniline fumardiamides

Reakcija adicije nukleofila na C=C dvostruku vezu koja je susjedna karbonilnoj C=O skupini zove se konjugirana adicija, Michaelova adicija ili 1,4-adicija. Reaktanti u Michaelovoj adiciji još se nazivaju Michaelovi donori i Michaelovi akceptori. Michaelove akceptore nalazimo u sljedećim skupinama lijekova: citostatici - inhibitori EGFR-a, te inhibitori Brutonove tirozin-kinaze, potom antiparkinsonici, lijekovi za terapiju multiple skleroze (dimetil-fumarat) i diuretici (etakrinska kiselina). U ovom radu opisana je sinteza potencijalnih Michaelovih akceptora, asimetričnih fumardiamida primakina i halogenanilina 4a-d. Novi spojevi karakterizirani su uobičajenim metodama (MS, IR, 1H i 13C NMR). Ispitivanje njihovog biološkog djelovanja je u tijekuNucleophilic addition to a C=C double bond immediately adjected to the C=O group is called conjugate addition, Michael addition or 1,4-addition. The reactants in Michaels addition are commonly known as Michael acceptors and Michael donors. Michael acceptors are present in the following drug classes: cytostatics – EGFR inhibitors and Bruton′s tyrosine kinase inhibitors , antiparkinsonics , drug for the therapy of multiple sclerosis and diuretics . Here we present synthesis of potential Michael acceptors, asymmetric primaquine and halogenaniline fumardiamides 4a-d. All new compounds were characterized by standard methods (MS, IR, 1H and 13C NMR). The evaluation of their biological activity is in progress