Francis G. FANG,Dae- Shik KIM,Hyeong- Wook CHOI,Charles E. CHASE
申请号:
MX2017014237
公开号:
MX2017014237A
申请日:
2016.05.09
申请国别(地区):
MX
年份:
2018
代理人:
摘要:
The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.En general, la invención presenta compuestos útiles para la síntesis de análogos de halicondrina B, tales como aribulina o sales farmacéuticamente aceptables de la misma, v.gr., mesilato de eribulina. Compuestos ejemplares son de la formula (I), (II), o (III).