Invention Grant
- Patent Title: Method for deprotecting aryl or alkyl sulfonamides of primary or secondary amines
- Patent Title (中): 伯胺或仲胺芳基或烷基磺酰胺脱保护方法
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Application No.: US12300409Application Date: 2007-02-13
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Publication No.: US08263808B2Publication Date: 2012-09-11
- Inventor: Michael Lefenfeld , James L. Dye , Partha Nandi , James Jackson
- Applicant: Michael Lefenfeld , James L. Dye , Partha Nandi , James Jackson
- Applicant Address: US NY New York
- Assignee: SiGNa Chemistry, Inc.
- Current Assignee: SiGNa Chemistry, Inc.
- Current Assignee Address: US NY New York
- Agency: J.A. Lindeman & Co., PLLC
- International Application: PCT/US2007/003874 WO 20070213
- International Announcement: WO2007/095276 WO 20070823
- Main IPC: C07C209/00
- IPC: C07C209/00

Abstract:
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.
Public/Granted literature
- US20090306391A1 METHOD FOR DEPROTECTING ARYL OR ALKYL SULFONAMIDES OF PRIMARY OR SECONDARY AMINES Public/Granted day:2009-12-10
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