Quimica Sintetica, S.a.

Giovanni Marras

Giuseppe Barreca

Maurizio Taddei

Luca Carcone

Marcello Rasparini

Damian Mark Grainger

Fabio Morana

Elena Cini

Roberto Rocco Tufaro

Samantha Louise Staniland

Bruno Romanò

Andrea Poggiali

Claudio Cianferotti

Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process. 

Process for the preparation of sphingosine-1-phosphate receptor agonist

It is described an industrially viable and advantageous process for the preparation of (S)-beta-aminosulfone (1) starting from the corresponding racemic compound, said (S)-beta-aminosulfone being a 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. 

Resolution of racemic beta-aminosulfone compounds

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.

Racemic beta-aminosulfone compounds

Two processes are described for preparing, in different diastereomeric purity degrees, the compound (S)-isopropyl-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)-phosphoryl)amino) propanoate, having the formula given below, known as Sofosbuvir and used for the treatment of hepatitis C. 

Nucleoside phosphoramidates useful for the treatment of viral infections and preparation thereof

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Galliate, Italy

Giovanni Marras