Objective To improve the synthetic procedure of the HIV integrase inhibitor raltegravir. Methods With 2-ami-no-2-methyl-propionitrile hydrochloride as starting material,the target compound raltegravir was synthesized through amino protection by benzyl chloroformate ,amidoxime formation,cyclization induced by michael addition&Claisen rearrangement,N-methylation,N-acylation,hydroxyl protection by trimethylacetyl chloride,hydrogenolysis by the system of Pd/C and formic acid,amidation with the 5-methyl-1,3,4-oxadiazol-formyl chloride,and immediate hydrolysis without more purification. Results The chemical structure of raltegravir and the intermediates were characterized by 1H NMR,13C NMR and MS. The overall yield was about 19.45%. Conclusion Compared with the preceding process,the developed route is easy to operate,safe and suitable for industrialized production in accor-dance with the quality standard of active pharmaceutical ingredient(API).

AIM: To study the effect of curcumin on the expression of p21 and CD44V6 in breast carcinoma in nude mice.METHODS: Nude mice were xenografted with human breast cancer cell line MCF-7 and randomly divided into 2 groups(n=4 in each group): control group and curcumin group.In latent period,the percentage of tumor development was observed.Tumors were measured and the surface areas were calculated.RT-PCR was performed to detect the expression level of cyclin D1,p21 and CD44V6 mRNA.RESULTS: The tumor surface areas in the curcumin group were significantly lower than those in control group.In curcumin treatment group,the expression of p21 was up-regulated while cyclin D1 was nearly not changed.The expression of CD44V6 was significantly down-regulated in curcumin group.CONCLUSION: Curcumin inhibits the expression of CD44V6 and up-regulates the expression of p21 in nude mice bearing human breast cancer cell line MCF-7.