卡培他滨的合成

Synthesis of Capecitabine

D-核糖经缩酮化、酯化、还原、水解和酰化反应制得1,2,3-三-O-乙酰基-5-脱氧-β-D-呋喃核糖(7),7与5-氟胞嘧啶进行Silyl反应,再与氯甲酸正戊酯进行酰胺化,最后水解去除乙酰基得到卡培他滨,总收率约21%。

Capecitabine was synthesized from D-ribose by ketalization, esterification, reduction with NaBH4, hydrolysis and acylation to give 1,2,3-tri-O-acetyl-5-deoxy-β-D-ribose, which was subjected to Silyl reaction with 5-fluorocytosine, amidation with n-pentyl chloroformate, and then hydrolysis with an overall yield of about 21% （based on D-ribose）.