申请人:——
公开号:US20020038026A1
公开(公告)日:2002-03-28
The invention provides a method of synthesizing a diketopiperazine of the formula:
1
wherein:
R
1
is —CH
2
COR
3
, or —CH
2
CH
2
COR
3
;
R
2
is the side chain of an amino acid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroxylysine, histidine, arginine, phenylalanine, tyrosine, tryptophan, thyroxine, cysteine, methionine, norvaline and onithine;
R
3
is —OH, —NH
2
, —OR
4
, —NHR
4
, or —NR
4
R
4
; and
each R
4
is independently an alkyl, aryl, alkylaryl, or arylalkyl.
本发明提供了一种合成式中二酮哌嗪的方法:
1
其中
R
1
是-CH
2
COR
3
或-CH
2
CH
2
COR
3
;
R
2
是选自甘氨酸、丙氨酸、缬氨酸、亮氨酸、异亮氨酸、丝氨酸、苏氨酸、天门冬氨酸、天冬酰胺、谷氨酸、谷氨酰胺、赖氨酸、羟基赖氨酸、组氨酸、精氨酸、苯丙氨酸、酪氨酸、色氨酸、甲状腺素、半胱氨酸、蛋氨酸、去甲缬氨酸和鸟氨酸的氨基酸侧链;
R
3
是-OH、-NH
2
、-OR
4
、-NHR
4
或-NR
4
R
4
且
每个 R
4
独立地为烷基、芳基、烷芳基或芳烷基。