摘要:
The present invention is directed to a novel process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid 2-acetylamino-ethyl ester, useful in the treatment of metabolic disorders and further to a process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid, a synthesis intermediate.
摘要:
The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate as well as intermediates for use in said process. More in particular the invention relates to processes for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate which make use of 4-amino-N-((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-(isobutyl)benzene sulfonamide intermediate, and to processes amenable to industrial scaling up. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as HIV protease inhibitors.
摘要:
A process for the preparation of N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives in which a (1-benzyl-2-hydroxy-3-isobutyl-amino-propyl)-carbamic acid derivative is reacted with a p-nitrophenylsulfonyl halide to provide the desired product in a high yield and degree of purity.
摘要:
The present invention is directed to a novel process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid 2-acetylamino-ethyl ester, useful in the treatment of metabolic disorders and further to a process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid, a synthesis intermediate.
摘要:
The present invention is directed to a novel process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid 2-acetylamino-ethyl ester, useful in the treatment of metabolic disorders and further to a process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid, a synthesis intermediate.
摘要:
A process for the preparation of N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives in which a (1-benzyl-2-hydroxy-3-isobutylamino-propyl)-carbamic acid derivative is reacted with a p-nitrophenylsulfonyl halide to provide the desired product in a high yield and degree of purity.