1. The Synthesis Of Molecules Based On Biodegradable And Glucose-responsive 2. The Synthesis Of The Treatment Drug Mozavatan Of Chronic Heart Failure

Chronic heart failure (CHF) is generally defined as the inability of the heart to supply sufficient blood flow to meet the needs of the body. In the recent years, the incidence of chronic heart failure showed a rising trend year after year. Due to the poor treatment, it has aroused extensive attention.Mozavaptan is a new kind of non-peptide V2 receptor antagonist. It has significant therapeutic effect to chronic heart failure. In this paper, we has a depth research of its intermediates, and the synthesis conditions were optimized. The best reaction conditions of compound 1 is n(p-amino benzoic acid methyl ester)/n(o-methyl benzoyl chloride)=1/1.2, n(p-amino benzoic acid methyl ester):n (pyridine)=1/1.2, n (p-amino benzoic acid A ester)/n(4-N, N-dimethyl aminopyridine)=1/0.05, the reaction solvent is dichloromethane, n (methyl benzoate) (mmoL)/V(dichloromethane)(mL)=3.71/15, yield is 95.64%; the optimal reaction conditions of compound 2 is n(product 1)/n(NaOH)=1/5, the concentration of methanol in aqueous 50%, reaction temperature is 45℃, reaction time was 1 h, yield is 96.15%. Results of this study can make more patients benefit by reducing the cost of, and similar structure optimization of synthesis of drug intermediates has certain significance.