Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 15, Issue 6, Pages 1358-1364Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op2002326
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The development of a highly efficient two-step process for the manufacture of the alpha 2 delta-ligand imagabalin hydrochloride 1 is described in 50% overall yield from (R)-3-methylhexanoic acid 2. Key aspects of this route include the development of a one-pot process for the synthesis of beta-enamine ester 7 and its subsequent diastereoselective hydrogenation with a Ru-(S)-BINAP catalyst. The use of a combination of TFA, ammonium trifluoroacetate, and relatively low pressures in the asymmetric hydrogenation are novel conditions reported for this type of transformation. The simplified process described realised a 4-fold reduction in cost of goods compared with the previously described enabling route.
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