发明授权
- 专利标题: Method for deprotecting aryl or alkyl sulfonamides of primary or secondary amines
- 专利标题(中): 伯胺或仲胺芳基或烷基磺酰胺脱保护方法
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申请号: US12300409申请日: 2007-02-13
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公开(公告)号: US08263808B2公开(公告)日: 2012-09-11
- 发明人: Michael Lefenfeld , James L. Dye , Partha Nandi , James Jackson
- 申请人: Michael Lefenfeld , James L. Dye , Partha Nandi , James Jackson
- 申请人地址: US NY New York
- 专利权人: SiGNa Chemistry, Inc.
- 当前专利权人: SiGNa Chemistry, Inc.
- 当前专利权人地址: US NY New York
- 代理机构: J.A. Lindeman & Co., PLLC
- 国际申请: PCT/US2007/003874 WO 20070213
- 国际公布: WO2007/095276 WO 20070823
- 主分类号: C07C209/00
- IPC分类号: C07C209/00
摘要:
The invention relates to a method for removing an alkyl sulfonyl or aryl sulfonyl protecting group from a primary or secondary amine by contacting an alkyl sulfonamide or an aryl sulfonamide with a Stage 0 or Stage I alkali metal-silica gel material in the presence of a solid proton source under conditions sufficient to form the corresponding amine. The invention also relates to a method for removing an alkyl sulfonyl or aryl sulfonyl protecting group from a primary or secondary amine by a) reacting an alkyl sulfonamide or an aryl sulfonamide with a Stage 0 or Stage I alkali metal-silica gel material, and b) subsequently reacting the reaction product from step a) with an electrophile or a proton source. Preferred Stage 0 or Stage I alkali metal-silica gel materials include Na, K2Na, and Na2K.
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