摘要 |
Disclosed is a process for preparing 8-substituted oxy-5-((R)-2-halo-1-hydroxy-ethyl)-(1H)-quinolin-2-ones or acceptable solvates thereof comprising reacting a 5-(alpha-haloacetyl)-8-substituted oxy-(1H)quinolin-2-one with a reducing agent in the presence of a chiral agent and a base to form a 8(substituted oxy)-5-((R)-2-halo-l-hydroxy-ethyl)-(1H)-quinolin-2-one, said chiral agent having a formula I or II wherein: M is Ru, Rh, Ir, Fe, Co or Ni; L is aryl or an aryl-aliphatic residue, in either case being optionally linked to a polymer; X is hydrogen or halo; R1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, aryl-aliphatic residue or a 4- to 12-membered heterocyclic group, which, in each case, is optionally linked to a polymer; and R2 and R3 are phenyl, or R2and R3 together with the carbon atom to which they are attached form a cyclohexane or cyclopentane ring.
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