Apixaban is a novel oral anticoagulant.Synthesis of apixaban intermediate from nitroaniline and 5-chloro-valeryl chloride is described through four steps,including acylation-cyclization,chlorination to the dichloro-intermediate,condensationelimination of the chloro groups and[3+2]cyclization-elimination.The total yield of the 4-step procedure is 58.1%.The raw materials are easily available,the reaction steps are less,the reaction condition is mild,and the high product purity(by HPLC)reaches 99.5%.The procedure provides raw material for synthesis of apixaban.

Objective: To prepare and characterize the iloperidone tablets.Methods: Hydroxypropyl methyl cellulose(HPMC) was used as carrier of the solid dispersion,and lactose monohydrate and microcrystalline cellulose(MCC) as loading agents.The formulation was optimized via single factor tests.The differential scanning calorimeter(DSC) and powder X-ray diffractometry were used to identify the states of the drug existence in the product.Results: The optimized formulation was composed of 3.243% iloperidone,6.486% HPMC,11% crospovidone(PVPP,exterior addition 8% and interior addition 3%),52.314% lactose monohydrate,26.157% MCC,0.5% magnesium stearate(MS),and 0.3% colloidal silicon dioxide.Iloperidone existed in the product at amorphous forms or solvates according to DSC and X-ray diffractometry.Conclusion: The drug dissolution behavior of obtained iloperidone tablets is similar to commercial products.

In order to improve the synthetic procedure of 7-ANCA,a cephalosporin nuclei,by the method of the target compound was synthesized from 7-phenyacetylamino-3-hydroxy-3-cepham-4-carboxylic acid diphenylmethy ester by the step of deoxidization,esterification,deprotection.The result show that the improveding synthetic procedure has the advantage of low cost and is suitable for industrial production and total yield was 56.0%,the product HPLC purity was more than 98%.