| abstract |
A process of preparing a compound of Formula (II): ** (See formula) ** in which Q is S or O, X is Cl or Br, and R1, R2 and R3 are each independently C (1) alkyl -6), in accordance with the following General Scheme (I): ** (See formula) ** process comprising: converting boronic acid A1 to carbaldehyde B1 through the activation of boronic acid with an activation reagent A2; convert carbaldehyde B1 into acetal C1 in acid catalysis with an adequate source of orthoformate; converting acetal C1 to nitrile D1 by catalytic cyanation with a metal catalyst and a cyanide source; hydrolyze D1 with a suitable acid, giving the carboxylic acid E1; converting the carboxylic acid E1 into F1 amide with a suitable base, a suitable coupling reagent and an amine source; converting the amide F1 into a compound of Formula (II) with an anionic coupling reagent having the structure H1, in which M is a Group I metal, a Group II, Cu or Zn metal; R is C (1-6) alkyl; m is 1, 2, 3 or 4; p is 1, 2, 3 or 4; and optionally, converting the compound of Formula (II) into a salt. |