Process

C - Chemistry – Metallurgy – 07 – C

Patent

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260/363, 260/366

C07C 237/08 (2006.01) C07C 231/02 (2006.01) C07D 263/26 (2006.01) C07D 307/33 (2006.01)

Patent

CA 2017426

ABSTRACT PROCESS The invention provides a novel process for the manufacture of enantiomerically-pure halolactones of the formula I which are useful for the production of certain 5-amino-4-hydroxyvaleric acid derivatives, themselves valuable intermediates in the production of compounds which are renin inhibitors. The process involves a diastereoselective alkylation of an oxazolidinone of the formula III, followed by a highly stereoselective and novel halolactonisation of an oxazolidinone of the formula II. Certain of the oxazolidinones of the formula II are novel and are provided as a further feature of the invention. The invention also provides a novel process for the production of the pharmaceutically-useful 5-amino-4-hydroxyvaleric acid derivatives of formula VI.

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