Patent – The application relates to an improved synthetic process for the preparation of the C13 taxol side chain. The proposed route utilises heterogeneous catalysis to effect a Heck coupling followed by an asymmetric dihydroxylation (AD) reaction to prepare an enantiomerically enriched 1,2-diol, offering the advantage over the prior art that separation of the catalyst from the final product is more straightforward, whilst in addition precluding osmium traces (and hence eliminating osmium toxicity) from the final product.
The Hearing Officer held that the skilled worker would consider it obvious to attempt the production of the (2R, 3S)-isomer of methyl 2,3-dihydroxy-3-phenylpropionate using prior art methodology in conjunction with common general knowledge and subsequently, use the (2R, 3S)-isomer so produced, in a further method to access the taxol side chain. The application was refused.
Judges:
Mrs C L Davies
Citations:
[2008] UKIntelP o03808
Links:
Jurisdiction:
England and Wales
Intellectual Property
Updated: 17 July 2022; Ref: scu.456929