Yeung Ying-Yeung, Hong Sungwoo, Corey E J
Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA.
J Am Chem Soc. 2006 May 17;128(19):6310-1. doi: 10.1021/ja0616433.
A short synthetic pathway has been developed for the synthesis of oseltamivir (1) or the enantiomer (ent-1). The intermediates and conditions for this process are summarized in Scheme 1. The synthesis provides a number of advantages: (1) use of inexpensive and abundant starting materials; (2) complete enantio-, regio-, and diastereocontrol; (3) avoidance of explosive, azide-type intermediates; (4) good overall yield (ca. 30%, still not completely optimized); and (5) scalability.
已开发出一种用于合成奥司他韦（1）或其对映体（ent - 1）的简短合成路线。该过程的中间体和条件总结于方案1中。该合成具有诸多优点：（1）使用廉价且丰富的起始原料；（2）实现了对映体、区域和非对映体的完全控制；（3）避免了易爆的叠氮化物型中间体；（4）总体产率良好（约30%，仍未完全优化）；以及（5）可扩展性。
