An Improved Process for the Preparation of (+)-3-Methoxy-N-formylmorphinan

被引:6
作者
Kumaraguru, Thenkrishnan [1 ]
Fadnavis, Nitin W. [1 ]
机构
[1] Indian Inst Chem Technol, Nat Prod Chem Div, Hyderabad 500007, Andhra Pradesh, India
关键词
N-FORMYLATION; FORMIC ANHYDRIDE; SECONDARY-AMINES; ACIDS;
D O I
10.1021/op400309q
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Two major steps, N-formylation of (-)-octabase and cyclization of the N-formylated product, involved in synthesis of (+)-3-methoxy-N-formylmorphinan, a key intermediate for production of dextromethorphan (DXM), have been improved to achieve higher yields in shorter time with fewer effluents. Methods of analysis of chemical and enantiomeric purities of the intermediates by HPLC and strategies for easy recovery and recycle of the reagents have been devised.
引用
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页码:174 / 178
页数:5
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