[EN] METHOD FOR THE SYNTHESIS OF ASPALATHIN AND ANALOGUES THEREOF<br/>[FR] PROCÉDÉ DE SYNTHÈSE D'ASPALATHINE ET DE SES ANALOGUES
申请人:SOUTH AFRICAN MEDICAL RES COUNCIL
公开号:WO2011064726A1
公开(公告)日:2011-06-03
A method of synthesising Aspalathin and its analogues or derivatives is disclosed. The method comprises synthesising a compound of formula 1 or its analogues or derivatives (I) wherein each of R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 is independently selected from the group consisting of -H, -OH, hydrocarbyl groups, saccharide moieties and -OR15; R15 is selected from the group consisting of hydrogen, a hydrocarbyl group (e.g. methoxy or ethoxy), an acyl group and a benzyl group; and R11, R12, R13 and R14 are independently selected from the group consisting of -H, hydrocarbyl groups, saccharide moieties, an acyl group and a benzyl group. The method comprises the step of coupling a sugar to a dihydrochalcone, chalcone or flavanone, or coupling the sugar to an intermediate for producing a dihydrochalcone, chalcone or flavanone followed by coupling of the sugar-intermediate adduct to a further intermediate for producing a dihydrochalcone, chalcone or flavanone, and transforming the product thereof into a compound of formula 1 or an analogue or derivative thereof.
公开了一种合成Aspalathin及其类似物或衍生物的方法。该方法包括合成式1或其类似物或衍生物(I)的化合物,其中R1、R2、R3、R4、R5、R6、R7、R8、R9和R10中的每一个都是独立地选自-H、-OH、烃基、糖基和-OR15的群组;R15选自氢、烃基(例如甲氧基或乙氧基)、酰基和苄基的群组;R11、R12、R13和R14独立地选自-H、烃基、糖基、酰基和苄基的群组。该方法包括将糖与二氢黄烷酮、黄烷酮或黄酮偶联,或将糖与产生二氢黄烷酮、黄烷酮或黄酮的中间体偶联,然后将糖-中间体加合物与产生二氢黄烷酮、黄烷酮或黄酮的进一步中间体偶联,并将其产物转化为式1或其类似物或衍生物的化合物。