ABSTRACT
Objective: To design and investigate an effective synthetic route of the antivirus compound favipiravir (T-705) with a stable and high yield. Methods: The commercial available diethyl aminomalonate hydrochloride was selected as the starting material. The product of aminolysis was cyclized with glyoxal to yield 3-hydroxy-2-pyraziamide, which was subjected to nitration with KNO3, chlorination and dehydration with POCl3 and fluorination with KF to afford 3, 6-difluoropyrazin-2-carbonnitrile. The difluorate product was further hydrolyzed and oxidized to give favipiravir. Results: The target compound was efficiently prepared by the above synthetic route. Conclusion: The reaction conditions are mild except the fluoro-substitution, in which all reagents should be dried completely. The synthetic procedure is simple, high-yield and suitable for scale preparation.
ABSTRACT
Objective To design and investigate an effective synthetic route of the antivirus compound favipiravir(T-705) with a stable and high yield. Methods The commercial available diethyl aminomalonate hydrochloride was selected as the starting material. The product of aminolysis was cyclized with glyoxal to yield 3-hydroxy-2-pyraziamide, which was subjected to nitration with KNO3, chlorination and dehydration with POCl3 and fluorination with KF to afford 3, 6-difluoropyrazin-2-carbonnitrile. The difluorate product was further hydrolyzed and oxidized to give favipiravir. Results The target compound was efficiently prepared by the above synthetic route. Conclusion The reaction conditions are mild except the fluoro-substitution, in which all reagents should be dried completely. The synthetic procedure is simple, high-yield and suitable for scale preparation.
ABSTRACT
Objective To observe the effect of Antivirus Compound Capsule in protecting liver and reducing enzyme level in chronic type B hepatitis and acute hepatic injury caused by D-GlaN.Methods Mice model was established by intraperitoneal injecting of D-GlaN 800mg/Kg.The level of ALT and AST was obviously increased after 48hours.Pathological test proved to be acute liver cell damage.Clinically 117 cases of chronic hepatitis B was recruited into a control group(57 cases)and a treatment group(60 cases).The treatment group was treated with Antivims Compound Capsule and Silymarin tablet,and the control group was treated with Silymarin tablet.Besides,both groups were infused with diammonium Compound Capsule Can obviously reduce level of AST(P＜0.001、＜0.01、＜0.01、＜0.001);Three dosage levels of Antivirus Compound Capsule can obviously reduce the degree hepatic pathological changes caused by D-GlaN induced(P＜0.01、＜for the treatment group andtlle control group) between the two groups with P＞0.02.while there was obvious difference of negative conversion rate of AST.[92.98%(53/57)and 78.9%(45/57)for the treaunent group and the consul group]between the two groups with P＜0.01.Conclusion Antivirus Compound Capsule is effective in protecting liver and reducing enzyme level of patients with chronic hepatitis B and acute hepatic injury caused bv D-GlaN.