Disclosed herein are methods and systems that relate to various configurations of electrochemical, bromination, oxybromination, bromine oxidation, hydrolysis, neutralization, and epoxidation reactions to form propylene bromohydrin, propanal, and propylene oxide or to form bromoethanol, bromoacetaldehyde, and ethylene oxide.

Disclosed herein are methods and systems that relate to various configurations of electrochemical, bromination, oxybromination, bromine oxidation, hydrolysis, neutralization, and epoxidation reactions to form propylene bromohydrin, propanal, and propylene oxide or to form bromoethanol, bromoacetaldehyde, and ethylene oxide.

The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma. ##STR00001##

The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma. ##STR00001##

A process for preparing an aromatic N-glycidylamine comprising a step of heating a mixture of an amine having at least one aromatic aminohydrogen atom with at least 0.7 equivalent of epichlorohydrin per aminohydrogen equivalent of the amine in presence of a catalyst dissolved in an inert organic solvent, at a pressure in a range of 200 mbar to 600 mbar; and adding a base to the mixture at a pressure in a range of 200 mbar to 600 mbar to facilitate dehydrochlorination of product of the previous step to obtain the aromatic N-glycidylamine.

A process for preparing an aromatic N-glycidylamine comprising a step of heating a mixture of an amine having at least one aromatic aminohydrogen atom with at least 0.7 equivalent of epichlorohydrin per aminohydrogen equivalent of the amine in presence of a catalyst dissolved in an inert organic solvent, at a pressure in a range of 200 mbar to 600 mbar; and adding a base to the mixture at a pressure in a range of 200 mbar to 600 mbar to facilitate dehydrochlorination of product of the previous step to obtain the aromatic N-glycidylamine.

Provided is a method for preparing an epoxide by halohydrination, the method comprising: (1) halohydrination: adding H.sub.2O, a halogen(s) and an olefin compound to a reaction device for reaction to obtain a halohydrin; (2) saponification: saponificating the halohydrin with an alkali metal hydroxide to obtain an epoxide and an alkali metal halide; (3) performing a bipolar membrane electrodialysis of the alkali metal halide to obtain an alkali metal hydroxide and a halogen hydride. Also provided is a method for preparing an epoxide by halohydrination, the method comprising: (1) halohydrination: halohydrinating a halogen hydride, an H.sub.2O.sub.2 and an olefin compound to obtain a halohydrin; optionally, (2) saponification: saponificating the halohydrin with an alkali metal hydroxide to obtain an epoxide and an alkali metal halide; optionally, (3) performing a bipolar membrane electrodialysis of the alkali metal halide to obtain an alkali metal hydroxide and a halogen hydride. The method according to the present invention can prepare a halohydrin or an epoxide at very high selectivity and yield, and greatly reduce the amount of waste water and waste slag discharges.

Provided is a method for preparing an epoxide by halohydrination, the method comprising: (1) halohydrination: adding H.sub.2O, a halogen(s) and an olefin compound to a reaction device for reaction to obtain a halohydrin; (2) saponification: saponificating the halohydrin with an alkali metal hydroxide to obtain an epoxide and an alkali metal halide; (3) performing a bipolar membrane electrodialysis of the alkali metal halide to obtain an alkali metal hydroxide and a halogen hydride. Also provided is a method for preparing an epoxide by halohydrination, the method comprising: (1) halohydrination: halohydrinating a halogen hydride, an H.sub.2O.sub.2 and an olefin compound to obtain a halohydrin; optionally, (2) saponification: saponificating the halohydrin with an alkali metal hydroxide to obtain an epoxide and an alkali metal halide; optionally, (3) performing a bipolar membrane electrodialysis of the alkali metal halide to obtain an alkali metal hydroxide and a halogen hydride. The method according to the present invention can prepare a halohydrin or an epoxide at very high selectivity and yield, and greatly reduce the amount of waste water and waste slag discharges.

The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma.

##STR00001##

The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma.

##STR00001##