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US 6,448,449 B2Granted
Process for preparation of (R)-1- (aryloxy)propan-2-ol
AssigneeRhodia ChiRex, Inc.
InventorJay Francis Larrow
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AssigneeRhodia ChiRex, Inc.
InventorJay Francis Larrow
Estimating the term…
A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol, which is a useful intermediate in the synthesis of the widely used antibiotic Levofloxacin is provided. A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-2-trimethylsiloxypropane is also described. The process includes the ring opening of (R)-propylene oxide with 2,3-difluoro-6-nitrophenyl trimethylsilyl ether in the presence of an optically active Co(salen) catalyst. The trimethylsilyl group of the reactant is transferred to the product aryloxy alcohol, which serves to protect the secondary alcohol in situ. Upon isolation, the trimethylsilyl group is removed and the resulting regioisomeric mixture purified to yield the desired (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol in high purity and yield.
A process for the preparation of an (R)-1-(aryloxy)propan-2-ol with high regioselectivity and enantioselectivity, said process comprising the steps of:
A process for the preparation of an (R)-1-aryloxy-2-trialkylsiloxypropane with high regioselectivity and enantioselectivity, said process comprising the step of:
A regioisomeric mixture prepared by a process comprising the step of:
A kinetic resolution process for the preparation of an (R)-1-aryloxy-2-trialkylsiloxypropane with high regioselectivity and enantioselectivity, comprising the step of:
A regioisomeric mixture prepared by a process comprising the step of:
Dependencies are inferred from the claim text.