Patent ID: 7834184

Claim:
A method for the synthesis of an opiate intermediate, the method comprising: a) reacting a compound of Formula 1 wherein X is F or Cl; with at least one halide selected from the group consisting of sulfonyl halide and phosphorous halide to form a compound of Formula 2; wherein X is F or Cl; X 1 is Cl or Br; and Y is SO when a sulfonyl halide is used, and P when a phosphorous halide is used; b) reacting the compound of Formula 2 with a compound of Formula 3 wherein R′ is an alkyl, aryl or acyl group; in the presence of at least one base to form a compound of Formula 4; wherein X is a F or Cl; and R′ is an alkyl, aryl or acyl group; c) reacting the compound of Formula 4 with at least one phosphoryl halide and then hydrolyzing to form a compound of Formula 5; wherein X is a F or Cl; and R′ is an alkyl, aryl or acyl group; d) reacting the compound of Formula 5 as a free imine or imine salt with at least one reducing agent to form a compound of Formula 6; wherein X is a F or Cl; and R′ is an alkyl, aryl or acyl group; e) selectively reducing the compound of Formula 6 to form a compound of Formula 7; wherein X is a F or Cl; and R′ is an alkyl, aryl or acyl group; f) reacting the compound of Formula 7 with at least one formic acid ester to form a compound of Formula 8; wherein X is a F or Cl; and R′ is an alkyl, aryl or acyl; and R is selected from the group consisting of H, alkyl, aryl, acyl, formyl, COR″, COOR″, benzyl, alkyl and sulfonamide; and wherein R″ is selected from the group consisting of alkyl or aryl; g) hydrolyzing the compound of Formula 8 forms a compound of Formula 9; and wherein X is a F or Cl; and R is selected from the group consisting of an H, alkyl, aryl, acyl, formyl, COR″, COOR″, benzyl, and sulfonamide; and wherein R″ is selected from the group consisting of alkyl or aryl; h) converting the compound of Formula 9 under Grewe cyclization conditions in at least one strong acid to form an opiate intermediate compound of Formula 10, wherein X is a F or Cl; and R is selected from the group consisting of an H, alkyl, aryl, acyl, formyl, COR″, COOR″, benzyl, (methyl), and sulfonamide; wherein R″ is selected from the group consisting of alkyl or aryl.