abstract |
The present invention relates to process for the production of chiral ligands comprising providing a starting material of Formula (A): wherein X* is a chiral or achiral directing group; and (i) is an optionally substituted mono- or polycyclic aryl or cycloalkyl group; ortholithiating the substrate; converting the ortho-lithiated substrate to a phosphine group having the formula -PR1 R1', R1 being selected from substituted and unsubstituted, branched- and straight-chain alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted carbocyclic aryl, and substituted and unsubstituted heteroaryl wherein the or each heteroatom is independently selected from sulphur, nitrogen, and oxygen, R1' being different from R1 and being selected from substituted and unsubstituted, branched- and straight-chain alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted carbocyclic aryl, and substituted and unsubstituted heteroaryl wherein the or each heteroatom is independently selected from sulphur, nitrogen, and oxygen; and optionally or if necessary converting X* to a different grouping to produce a chiral ligand. |