Lonza Inc.

Almirall, LLC

Bristol-Myers Squibb Compnay

Meinrad Brenner

Erick Moran Carreira

Aleksander Warm

Nicka Chinkov

Miriam Lorenzi

Lothar Zimmermann

Giuseppe Motta

Sean M Johnston

Farzaneh Seyedi

Giovanni Palombi

Eugenio Castelli

Ruiliang Lu

Shaozhi Huang

William Paul Armstrong

Gajanan Joshi

The described invention relates to sarecycline, related compounds, intermediates and salts thereof and processes for preparing the same.

Process for making sarecycline hydrochloride

The invention is directed to a process for the preparation of a cyclic carbamate starting with o-aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C-alkyl C-carboxylates and mixtures of at least one C-alkyl C-carboxylate with at least one C-alkane.

Process for the synthesis of cyclic carbamates

The invention is directed to a process for the preparation of a cyclic carbamate starting with a chiral propargylic alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C-alkyl C-carboxylates and mixtures of at least one C-alkyl C-carboxylate with at least one C-alkane. Another aspect of the invention is directed to a process for the synthesis of said cyclic carbamate starting described above, wherein also a process for the preparation of the chiral propargylic alcohol is provided.

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Steg, Switzerland

Meinrad Brenner