Details

Autor(en) / Beteiligte

• Fu, Liqiang
• Liu, Xin
• Cheng, Jianjun
• He, Huili
• Cai, Zhan
• Guo, Xingsheng
• Ding, Shi
• Yang, Yushe

Titel

First Scale-Up Synthesis of FU-23, a Novel Water-Soluble Pleuromutilin-Derived Antibiotic

Ist Teil von

• Organic process research & development, 2010-07, Vol.14 (4), p.815-819

Ort / Verlag

American Chemical Society

Erscheinungsjahr

2010

Link zum Volltext

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• A first scale-up synthesis of FU-23 (1), a potent and effective water-soluble pleuromutilin-derived antibiotic, is described. The original synthesis from the medicinal chemistry group provided 1 in seven steps and 10.9% overall yield, required four chromatographies and employed expensive reagents such as AgOCN and 4-acetylsalicoyl chloride. The optimized synthetic route for the preparation of phosphate salt 1 consists of seven linear steps with a 42.8% overall yield. Significant cost reduction and more robust reaction conditions have been developed with no chromatography required at any stage.