A solid-phase total synthesis of the cyclic depsipeptide HDAC inhibitor spiruchostatin A

作者：Iijima Yusuke; Munakata Asami; Shin ya Kazuo; Ganesan A; Doi Takayuki^*; Takahashi Takashi

来源：Tetrahedron Letters, 2009, 50(24): 2970-2972.

DOI：10.1016/j.tetlet.2009.04.005

• Cyclic depsipeptide
• Histone deacetylase
• Natural product synthesis
• Solid-phase synthesis

Spiruchostatin A, a potent histone deacetylase inhibitor, was efficiently synthesized from (3S,4R)-4-amino-3-hydroxy-5-methylhexanoic acid utilizing solid-phase peptide elongation with D-cysteine, D-alanine, and (E)-3-hydroxy-7-thio-4-heptenoic acid and solution-phase macrolactonization, followed by intra molecular disulfide formation.

• 出版日期2009-6-17