Invention Grant
US08816120B2 Process for the preparation of N-(4-nitro-2-sulfamoyl-phenyl)-malonamic acid methyl ester and N-(4-amino-2-sulfamoyl-phenyl)-malonamic acid methyl ester
有权
制备N-（4-硝基-2-氨磺酰基 - 苯基） - 丙酰甲酸甲酯和N-（4-氨基-2-氨磺酰基 - 苯基） - 丙酰甲酸甲酯的方法
- Patent Title: Process for the preparation of N-(4-nitro-2-sulfamoyl-phenyl)-malonamic acid methyl ester and N-(4-amino-2-sulfamoyl-phenyl)-malonamic acid methyl ester
- Patent Title (中): 制备N-（4-硝基-2-氨磺酰基 - 苯基） - 丙酰甲酸甲酯和N-（4-氨基-2-氨磺酰基 - 苯基） - 丙酰甲酸甲酯的方法
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Application No.: US14153878Application Date: 2014-01-13
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Publication No.: US08816120B2Publication Date: 2014-08-26
- Inventor: Jiang Zhu
- Applicant: Hoffmann-La Roche Inc.
- Applicant Address: US CA South San Francisco
- Assignee: Hoffmann-La Roche Inc.
- Current Assignee: Hoffmann-La Roche Inc.
- Current Assignee Address: US CA South San Francisco
- Agency: Womble Carlyle Sandridge & Rice
- Main IPC: C07C315/00
- IPC: C07C315/00
Abstract:
The present invention provides a novel method for preparing compounds N-(4-nitro-2-sulfamoyl-phenyl)-malonamic acid methyl ester and N-(4-amino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, which are novel intermediates for preparing a key intermediate N-(4-methanesulfonylamino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, for the preparation of N-(3-{(1R,2S,7R,8S)-3-[(4-fluorophenyl)methyl]-6-hydroxy-4-oxo-3-azatricyclo[6.2.1.02,7]undec-5-en-5-yl}-1,1-dioxo-1,4-dihydro-1λ6,2,4-benzothiadiazin-7-yl)methanesulfonamide, also known commercially as Setrobuvir, a compound useful in treating hepatitis C.
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