Ma Dawei, Xie Weiqing, Zou Bin, Lei Qiong, Pei Duanqing
State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China.
Department of Pharmacology, University of Minnesota, Minneapolis, MN 55455, USA.
Tetrahedron Lett. 2004 Oct 18;45(43):8103-8105. doi: 10.1016/j.tetlet.2004.08.179. Epub 2004 Sep 21.
Aldol reaction of ,-dibenzyl valinal with propiolic acid ethyl ester derived lithium reagent provides -aminoalcohol and -aminoalcohol , which are converted into the lactone via two different routes. Alkylation of followed by lactone ring opening afford the acid , which is coupled with the amine and 5-methylisoxazole-3-carboxylate acid , respectively, to deliver AG7088.
α,β-二苄基缬氨醛与丙炔酸乙酯衍生的锂试剂发生羟醛反应，生成α-氨基醇和β-氨基醇，它们通过两条不同的路线转化为内酯。α-氨基醇进行烷基化反应，随后内酯开环得到酸，该酸分别与胺和5-甲基异恶唑-3-羧酸偶联，得到AG7088。
