Total synthesis of splenocin B, a potent inhibitor of the pro-inflammatory cytokine from marine-derived Streptomyces sp.

[摘要] The first total synthesis of splenocin B (1), a new potent anti-inflammatory antimycin-class antibiotic, has been described. The synthesis of 1 has been accomplished in 8 linear steps, starting from commercially available N-Boc-L-threonine benzyl ester 4 and 3,4-dihydroxypentanoic acid derivative 2. Kita-Trost lactonization via an ethoxyvinyl ester intermediate was utilized for the construction of the 9-membered dilactone core. (C) 2015 Elsevier Ltd. All rights reserved.

[发布日期] 2015-12-30

[关键词] Splenocin B;9-Membered dilactone;Anti-inflammatory;Kita-Trost lactonization;Antimycin-class antibiotics