申请人:Van der Westhuizen Jan Hendrik
公开号:US20130018182A1
公开(公告)日:2013-01-17
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:
wherein
each of R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, R
8
, R
9
and R
10
is independently selected from the group consisting of —H, —OH, hydrocarbyl groups, saccharide moieties and —OR
15
;
R
15
is selected from the group consisting of hydrogen, a hydrocarbyl group (e.g. methoxy or ethoxy), an acyl group and a benzyl group; and
R
11
, R
12
, R
13
and R
14
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选择自羟基、烃基、糖基团和—OR15的群组;R15选择自氢、烃基(例如甲氧基或乙氧基)、酰基和苄基;而R11、R12、R13和R14则独立选择自—H、烃基、糖基团、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,或将糖与用于产生二氢黄烷酮、黄烷酮或黄酮的中间体偶联,然后将糖-中间体加合物偶联到用于产生二氢黄烷酮、黄烷酮或黄酮的进一步中间体上,并将其转化为式1或其类似物或衍生物的化合物。