| The modification of purine heterocyclic compounds as the parent by coupling different side chains is an important direction in the synthesis of small molecular kinase inhibitors.In this paper,based on 2,6-dichloro-7-azapurine,various pyrimidine purine derivatives were synthesized by the catalytic coupling reaction of ferrocene cyclopyridine palladium imide with different activity at different sites in the mother nucleus.At the same time,the reaction conditions were optimized,and the step-by-step reaction was crosslinked by the coordination of ferrocene cyclopyridine palladium compounds and carbene ligands in a "one-pot" way,which greatly reduced the amount of catalyst used and the amount of work needed for synthesis.It also provided a green,environmentally friendly and high atomic utilization catalytic design concept for industrial operation and application and a new method for green chemistry.β-hydroxybutyric acid exists widely and is one of the most important ketones in animals,including humans.At the same time,it is also the most common microbial degradation product.Beta-hydroxybutyric acid derivatives are widely used in the field of medicine.Amino acid is the basic structural unit of human body.In recent decades,with the rapid development of research on polypeptide drugs,several polypeptide drugs have been successfully marketed.Most of these polypeptide drugs are composed of natural amino acids.It can be said that the treatment of a considerable part of modern medical diseases can not be separated from the participation of amino acid drugs.A series of compounds of beta-hydroxybutyryl amino acids were designed and synthesized,and their toxicological,metabolic and biological properties were systematically studied.Sixty-five polypeptide compounds of β-hydroxybutyrate were synthesized from ethyl ester of β-hydroxybutyrate,protected by tert-butyl dimethylsilicon,and condensated with α-amino acid.Their structures were determined by NMR and elemental analysis technology.At the same time,animal and cell safety evaluation,weight loss and anti-cancer evaluation of some pseudo-peptide compounds of beta-hydroxybutyric acid amino acid were carried out.The experimental data show that some compounds and their combinations show good activity and efficacy,which provides a basis for the research and development of new drugs,cosmetics and food additives in the later period,and has broad application prospects in biomedicine. |
