EFFICIENT COUPLING OF ALPHA,ALPHA-DIMETHYL AMINO-ACID USING A NEW CHLORO IMIDAZOLIDIUM REAGENT, CIP

被引:70
作者
AKAJI, K [1 ]
KURIYAMA, N [1 ]
KISO, Y [1 ]
机构
[1] KYOTO PHARMACEUT UNIV,DEPT MED CHEM,YAMASHIMA KU,KYOTO 607,JAPAN
关键词
D O I
10.1016/S0040-4039(00)76895-X
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
CIP (2-chloro-1,3-dimethylimidazolidium hexafluorophosphate) was an efficient coupling agent for N-alpha-protected alpha-aminoisobutyric acid (Aib) in the presence of an additive. The reactivity was enhanced markedly by a catalytic amount of additive in the order of HOAt similar to HODhbt>DMAP>HOBt. These couplings occurred without detectable racemization.
引用
收藏
页码:3315 / 3318
页数:4
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