| abstract |
A process for the production of a compound of formula VI: wherein R 1 is a labile acid protecting group from a compound of formula VII: said process comprising: (g) reacting a compound of formula VII with a suitable chlorinating agent in the presence of a suitable base and a suitable solvent, wherein the reaction carried out by: (g-1) adding a mixture of a compound of formula VII and a base in a solvent to a mixture of chlorinating agents in a solvent at a temperature in the range of 60 to 90 ° C for a time of about 60 minutes; or (g-2) adding a chlorinating agent to a mixture of a compound of Formula VII and a base in a solvent at room temperature for a period of about 15 minutes, and then heating the reaction mixture for a period of about 90 minutes at a temperature in the range of 70 to 90 ° C and with stirring the reaction mixture at the same temperature for about 1 h; or (g-3) adding a chlorinating agent to a mixture of a compound of formula VII and a base in a solvent at a temperature in the range of 60 to 110 ° C for a period of about 15 minutes, to obtain a compound of Formula VIII: and (h) reacting the compound of formula VIII with 4-bromo-2-fluoroaniline in situ in the presence of the solvent used in step (g) for the purpose of preparing the hydrogen chloride salt of the compound of formula VI; and wherein the compound of formula VI, obtained in the form of the hydrochloride salt, may be converted into the free base or into the form of an alternative salt, if necessary. The patent comprises a further 27 claims. |