发明名称 |
Converting an alcohol to an azide with SN2 inversion using a phosphoryl azide |
摘要 |
Described is a process for converting an alcohol to an azide with SN2 inversion using a phosphoryl azide, e.g. diphenylphosphoryl azide (DPPA). Good yields of azide in high enantiomeric excess can be achieved specifically for benzylic alcohols and alpha-hydroxy alkyl esters. The process is carried at preferably room temperature in an inert dry aprotic solvent, e.g. toluene, and in the presence of a proton acceptor, e.g. 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) to afford high yields of high enantiomeric purities.
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申请公布号 |
US5391772(A) |
申请公布日期 |
1995.02.21 |
申请号 |
US19930089315 |
申请日期 |
1993.07.08 |
申请人 |
MERCK & CO., INC. |
发明人 |
THOMPSON, ANDREW S.;GRABOWSKI, EDWARD J. J. |
分类号 |
C07C247/06;C07D213/42;C07D215/12;C07D307/52;C07D307/78;C07D333/20;C07D333/54;C07D333/58;C07D495/04;(IPC1-7):C07D307/02;C07C247/00 |
主分类号 |
C07C247/06 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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