发明授权
US5166330A Process for the preparation of nucleoside alkyl-aralkyl- and
aryl-phosphonites and -phosphonates
失效
核苷烷基 - 芳烷基 - 和芳基 - 亚膦酸酯和膦酸酯的制备方法
- 专利标题: Process for the preparation of nucleoside alkyl-aralkyl- and aryl-phosphonites and -phosphonates
- 专利标题(中): 核苷烷基 - 芳烷基 - 和芳基 - 亚膦酸酯和膦酸酯的制备方法
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申请号: US139112申请日: 1987-12-28
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公开(公告)号: US5166330A公开(公告)日: 1992-11-24
- 发明人: Joachim Engels , Alfred Jager
- 申请人: Joachim Engels , Alfred Jager
- 申请人地址: DEX Frankfurt am Main
- 专利权人: Hoechst Aktiengesellschaft
- 当前专利权人: Hoechst Aktiengesellschaft
- 当前专利权人地址: DEX Frankfurt am Main
- 优先权: DEX3332068 19830906
- 主分类号: C07F9/48
- IPC分类号: C07F9/48 ; C07H19/04 ; C07H21/00
摘要:
Deoxyribonucleoside phosphonates, thiophosphonates and selenophosphonates are obtained by condensation of a difunctional phosphonylating reagent of the formulaR--PXY,in which R is an inert non-cytotoxic organic radical, X is chlorine or Y and Y is a secondary amino group, with a deoxyribonucleoside of which the 5-hydroxyl group and any exo-amino group presents in the base radical are protected, and further condensation with a nucleoside of which the 3-hydroxyl group and any exo-amino group present in the base radical are protected, and then oxidation. The thiophosphonates and selenophosphonates and the intermediates of the first condensation stage are new.
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