18-11-2021 дата публикации
Номер: US20210355086A1
Принадлежит:
The present invention provides a novel process for preparing a diastereomeric mixture of the phenicol of Formula (1), its use for the treatment of bacterial infections in animals, and veterinary compositions containing the Formula (1) compound, diastereomers thereof, and veterinary acceptable salts thereof. 2. The process of comprising the steps of:{'sub': 2', '2', '2', '3', '2', '3', '3', '3, 'a) pre-activating the Formula (B) compound with a palladium catalyst selected from the group consisting of Pd(OAc), PdCl, Pd-G2-XPhos, Pd-XPhos Crotyl Cl, Pd(dppf)Cl, Pd-G2-PCy, and Pd(dba), in the presence of an alcohol, a ligand selected from the group consisting of XPhos, SPhos, dppp, dppf, dba, PPh, and PCy, and a borylation buffer that comprises an acid and a base, wherein said acid is selected from the group consisting of HOAc, citric acid, formic acid, chloroacetic acid, and ammonium acetate;'}{'sub': 2', '2', '2', '2', '4, 'b) borylating the preactivated Formula (B) compound of step (a) by adding a borylating agent in an alcohol; wherein the borylating agent is selected from the group consisting of bisboronic acid, bisboronic acid and ethylene glycol, bisboronic acid and propylene glycol, BPin, and B(NMe);'}c) mixing the Formula (A) compound with a base in an alcohol, co-solvent, or mixtures thereof; andd) mixing the reactants of Step (c) to the reactants of Step (b) to give the compound of Formula (1), and diastereomers thereof.3. The process of claim 1 , wherein the base in Step (a) and (c) is selected from the group consisting of KOAc claim 1 , CsOAc claim 1 , TEA claim 1 , KCO claim 1 , NaCO claim 1 , CsCO claim 1 , DIPEA claim 1 , and KPO claim 1 , and mixtures thereof; and wherein the alcohol in Steps (a) claim 1 , (b) claim 1 , and (c) is selected from the group consisting of methanol claim 1 , ethanol claim 1 , 1-propanol claim 1 , 2-propanol and 2-butanol.4. The process of claim 3 , wherein the alcohol in Steps (a) and (b) is anhydrous ethanol and the alcohol ...
Подробнее