The present invention, relates to solid state forms of N-[2-[(1 S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide represented by the following structural formula-1 and process for their preparation. The present invention also relates to an improved process for the preparation of N-[2-[(1 S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide compound of formula-1 and intermediates thereof.

The present invention, relates to solid state forms of N-[2-[(1 S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide represented by the following structural formula-1 and process for their preparation. The present invention also relates to an improved process for the preparation of N-[2-[(1 S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide compound of formula-1 and intermediates thereof.

It is described an industrially viable and advantageous process for the preparation of racemic beta-aminosulfone (1), an useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.

##STR00001##

It is described an industrially viable and advantageous process for the preparation of racemic beta-aminosulfone (1), an useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.

##STR00001##

It is described an industrially viable and advantageous process for the preparation of racemic beta-aminosulfone (1), an useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.

##STR00001##

A chemoselective and reactive Mn(CF.sub.3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic CH hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.

A chemoselective and reactive Mn(CF.sub.3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic CH hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.

The invention relates to the field of organic chemistry and medicine, and more particularly to a method of producing synthetic biologically active derivatives of carbopentoxysulfanilic acid. The present method of producing a sodium salt of (2,6-dichlorophenyl)amide carbopentoxysulfanilic acid is characterized in that the reaction mass formed during the production of (2,6-dichlorophenyl)amide carbopentoxysulfanilic acid is agitated in a medium which is acidified with a solution of hydrochloric acid to pH 5-5.5, and the isolated precipitate may be washed with water acidified with a solution of hydrochloric acid to pH 5-5.5. This increases the yield of a sodium salt of (2,6-dichlorophenyl)amide carbopentoxysulfanilic acid to 70% (compared to a prior art yield of 32%) and also increases the purity of the target sodium salt.

The invention relates to the field of organic chemistry and medicine, and more particularly to a method of producing synthetic biologically active derivatives of carbopentoxysulfanilic acid. The present method of producing a sodium salt of (2,6-dichlorophenyl)amide carbopentoxysulfanilic acid is characterized in that the reaction mass formed during the production of (2,6-dichlorophenyl)amide carbopentoxysulfanilic acid is agitated in a medium which is acidified with a solution of hydrochloric acid to pH 5-5.5, and the isolated precipitate may be washed with water acidified with a solution of hydrochloric acid to pH 5-5.5. This increases the yield of a sodium salt of (2,6-dichlorophenyl)amide carbopentoxysulfanilic acid to 70% (compared to a prior art yield of 32%) and also increases the purity of the target sodium salt.

The present invention relates to a method for producing (functionalized) biaryls by employing a visible-light-driven, gold-catalyzed CC cross-coupling reaction system involving boron- and silicon-containing aryl compounds and aryldiazonium compounds. Moreover, the present invention relates to the use of such boron- and silicon-containing aryl compounds and aryldiazonium compounds, as well as related gold catalysts, in the manufacture of (functionalized) biaryls.