Taking 4-bromophenol and bromo-n-pentane as starting materials, anidulafungin side chain was obtained through five steps of addition, boron generation, coupling, hydrolysis and esterification, which structure was confirmed by 1H-NHR, MS and other analytical testing techniques. The obtained optimum synthesis process is the active esters is prepared by coupling reaction of P-pentoxytribenzoic acid IV with hydroxybenzotriazole using boron product as raw material and Pd(dppf)Cl2 as catalyst. The total yield of the synthesis process of anidulafungin side chain reachs 50.8%.
[ 1 ] Campoy S, Adrio J L. Antifungals [ J ]. Biochem Pharmacol, 2017, 133: 86 - 96.
[ 2 ] 孟玲宁，刘锦燕，李文静，等. 抗真菌药物新作用靶点机制的研究进展[ J ]. 诊断学理论与实践，2017（ 5 ）：540 - 543.
[ 3 ] Behme A, Ruhnke M, Buchheidt D, et al. Treatment of invasive fungal infections in caner patients-recommendations of the Infectious Diseases Working Party (AGIHO) of the German Society of Hematology and Oncology(DGHO)[ J ]. Ann Hematol, 2014, 93( 1 ): 13 - 32.
[ 4 ] Pappas PG, Kauffman CA, Andes DR, et al. Clinical practice gui-
deline for the management of candidiasis: 2016 update by the infectious diseases society of America [ J ]. Clin Infect Dis, 2016, 62( 4 ) : 409.
[ 5 ] Chen SC, Slavin MA, Sorrell TC. Echinocandin antifungal drugs in fungal infections:a comparison[ J ]. Drugs, 2011, 71( 1 ): 11 - 41.
[ 6 ] Walker LA, Gow NAR, Munro CA. Fungal echinocandin resistance [ J ]. Fungal Gen Bio Fg B, 2010, 47( 2 ): 117.
[ 7 ] Pappas P G, Kauffman C A, Andes D R, et al. Clinical practice guideline for the management of candidiasis: 2016 update by the infectious diseases society of America [ J ]. Clin Infect Dis, 2016, 62( 4 ) : 1 - 50.
[ 8 ] 伊莱利利公司. 含有成胶束表面活性剂的棘白菌素药物制 剂：美国，00805696.X [ P ]. 2000-03-02.
[ 9 ] 伊莱利利公司. 环肽抗真菌剂及其制备方法：美国，93103587.2[ P ]. 1993-03-18. 专利.
[ 10 ] Frederick J. Burkhardt, Manuel Debono, et al. CYCLIC PEPTIDE ANTIFUNGAL AGENTS: US，5965525A[ P ]. 1999 - 10 - 12.
[ 11 ] BALKOVEC, James M，Clinton Avenue，et al. ANTIFUNGAL AND ANTI - PNEUMOCYSTIS COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF USE: WO，9508341[ P ]. 1995 - 03 - 30.
[ 12 ] 苗 宇，关永霞. 4"-正戊氧基-1, 1': 4', 1 "-三联苯-4-甲酸的合成[ J ]. 药学研究，2013，32（ 8 ）：492 - 493.
[ 13 ] James M. Balkovec, North Plainfield, Frances A. Bouffard, et al.ANTIFUNGAL AND ANTI-PNEUMOCYSTIS COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF USE: US，5541160[ P ]. 1996 - 07 - 30
