Synthetic Process Of Apixaban, Fxa(Coagulation Factor Xa) Inhibitor, And N-Methyl-Amino-Acid Ester

Thromboembolism disease has become a dangerous disease which leads to worldwide high rate of morbidity and mortality. VTE (venous thromboembolism) is the third most prevalent CVD (cardiovascular disease), after MI (myocardial infarction) and stroke. Thrombogenesis prevention, which is actualized well by new anticoagulants, contributes to the reduced incidence of VTE in high-risk groups. As a result, evidence-based clinical guidelines strongly suggest VTE patients to use anticoagulants because of the drugs irreplaceable advantage. This article sum up research progresses in Apixaban, a kind of FXa(Coagulation factor Xa) inhibitor, as well as the formation mechanism of VTE. According to these analyses, we designed a new synthesize technique for Apixaban, by which the total Apixaban recovery is 25.67%. Using bromobenzene as raw material, we successfully synthetized Apixaban. by cross-coupling, bromination, condensation reaction and [3 + 2] cyclization reaction. This method is suitable for commercial production because of its convenience, low cost and high efficiency.N-methyl-amino acids and its. derivative form the primary of many natural nitrogenous products. Polypeptide with N-methyl-amino acid residue can not only protect itself from proteolysis by protease, but also increase the permeability of cytomembrane. Besides, it can change the conformations of polypeptide or the nature of amido bond. This article sum up research progresses in the synthetic method of N-methyl-amino acids published at home and abroad, then developed a new convenient method for N-methyl-amino-acid ester synthesis. The new method is praised by its convenience, mild reaction, high efficiency and environment protection.