| abstract |
The present invention provides a compound of Formula 2aa and Formula 1dg in the presence of sodium hydroxide (NaOH) and potassium hydroxide (KOH), optionally in the presence of a phase transfer catalyst, in particular quaternary ammonium salts or phosphonium salts, in aprotic solvents. Producing a reaction mixture consisting of a compound of 1dh, 1di or 1dj; And heating the resulting reaction mixture under a nitrogen atmosphere.n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n Wheren n n Residue Is a group of the formula 1dc to 1df:n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n n In a preferred embodiment, the aprotic solvent is dimethylsulfoxide (DMSO), the strong base in solid form is NaOH in powder or pellet form, and the phase transfer catalyst is tetra-n-butylammonium chloride (TBAC).n n n At this time, the starting material of Formula 2aa is prepared as follows:n n n The presence of a transition metal catalyst further comprising a palladium metal complex, in the presence of a strong base consisting of sodium hydroxide (NaOH) or potassium hydroxide (KOH), in a solvent consisting of linear or branched aliphatic alcohols of formulas 3ba and 4aa And further in the presence of an auxiliary ligand comprising a bidentate chiral axial incomplete asymmetric aromatic compound of formula 5fa or 5fb: |