Zach System

Patricia Poirier

Livius Cotarca

Massimiliano Forcato

Yvon Derrien

Alain Burgos

Tony Pintus

Valéry Dambrin

Jacques Tonnel

Sebastien Meunier

Denis Lucet

Pierrick Morice

Laurence Graindorge

Sébastien Meunier

The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of preparing micro size abiraterone or derivatives thereof in high yield and purity by means of a spherical agglomeration process.

Process for producing a solid form of abiraterone acetate

The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing abiraterone or derivatives thereof in high yield and purity by means of a key 3-formate intermediate.

Process for preparing 17-substituted steroids

An in situ or one-pot process for the preparation of the compounds of formula (I) uses a compound of general formula (I):  and includes: a) the hydrogenation of a nitrile group of the compound of general formula (II):  in which Rto R4 are especially H or alkyl and n varies from 0 to 4, in the presence of a hydrogenation catalyst, a methylating agent and an organic acid as solvent, and at a temperature Ta below the initiation temperature of a reductive amination reaction, to give a primary amine from the nitrile group; and b) the reductive amination of the primary amine in the presence of hydrogen, at a temperature Tb above Ta, to give the dimethylated amine of general formula (I) by activation of the methylating age.

In situ or one-pot hydrogenation and reductive amination process

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Saint Clement de la Place, France

Patricia Poirier