发明名称 |
Synthesis of propargyl modified nucleosides and phosphoramidites and their incorporation into defined sequence oligonucleotides |
摘要 |
The present invention describes a novel 2'-O-alkylation reaction to produce a novel series of nucleosides carrying the 2'-O-propargyl group, using propargyl bromide, dibutyl tin oxide and tetrabutyl ammonium bromide. The procedure involves novel techniques for regioselective introduction of 2'-/3'-O-propargyl group directly on the 5'-DMT-N-protected- nucleosides using dibutyl tin oxide as a mild base in conjunction with a phase transfer catalyst, tetrabutyl ammonium bromide. The reaction process has many significant features and leads to isomeric ratios in favor of the 2'-regio isomer. This allows the synthesis of the corresponding phosphoramidites of high purity. |
申请公布号 |
AU1436995(A) |
申请公布日期 |
1995.07.17 |
申请号 |
AU19950014369 |
申请日期 |
1994.12.30 |
申请人 |
CHEMGENES CORPORATION |
发明人 |
SURESH C SRIVASTAVA;SYED KAZIM RAZA |
分类号 |
C07H19/04;C07H19/10;C07H19/20;C07H21/00 |
主分类号 |
C07H19/04 |
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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