合成光学活性β,β-二氟谷氨酸和β,β-二氟脯氨酸衍生物的催化途径。
Catalytic route to the synthesis of optically active beta,beta-difluoroglutamic acid and beta,beta-difluoroproline derivatives.
作者信息
Suzuki Atsushi, Mae Masayuki, Amii Hideki, Uneyama Kenji
机构信息
Department of Applied Chemistry, Faculty of Engineering, Okayama University, 3-1-1 Tsushimanaka, Okayama 700-8530, Japan.
出版信息
J Org Chem. 2004 Jul 23;69(15):5132-4. doi: 10.1021/jo049789c.
Beta,beta-difluorinated amino acid derivatives were synthesized via Mg(0)-promoted defluorination of alpha-trifluoromethyl iminoester. Bromination of the difluoroenamine afforded the bromodifluoromethyl iminoester in good yield. Pd-catalyzed asymmetric hydrogenation of the bromodifluoromethyl iminoester and the subsequent transformations provided optically active beta,beta-difluoroglutamic acid and beta,beta-difluoroproline derivatives.
通过镁（0）促进的α-三氟甲基亚胺酯脱氟反应合成了β，β-二氟氨基酸衍生物。二氟烯胺的溴化反应以良好的产率得到溴二氟甲基亚胺酯。溴二氟甲基亚胺酯的钯催化不对称氢化反应及后续转化反应提供了光学活性的β，β-二氟谷氨酸和β，β-二氟脯氨酸衍生物。
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