Dsm IP Assets B.v.

Jeroen Antonius Franciscus Boogers

Andreas Hendrikus Maria De Vries

Quirinus B Broxterman

Ben De Lange

Gerardus Karel Maria Verzijl

Johannes Gerardus De Vries

Anna Maria Cornelia Francisca Castelijns

Henricus Martinus Maria Gerardus Straatman

Lizette Schmieder

Described is a method for the preparation of renin inhibitors such as aliskiren, and intermediates useful therein. The method introduces a nitrogen-containing intermediate such as a lactone of formula (8). with Rbeing a branched Calkyl. In the preparation of the lactone, or related intermediates, a desired stereochemical configuration can be controlled by starting from a chiral aldehyde satisfying formula (10). 

Convergent synthesis of renin inhibitors and intermediates useful therein

The invention relates to a compound according to Formula (IX) and salts thereof, wherein R, Rand Rare each independently selected from H and hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, or when the compound according to formula (IX) is a salt, Rand/or Rmay be a cation, R, and Reach independently selected from hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, and wherein any two of R, R, R, Rand Rare optionally linked together to form a ring structure. The invention further relates to the preparation of such a compound and to the use of such a compound for preparing a pharmaceutical compound, an agrochemical compound, an intermediate for a pharmaceutical compound or an intermediate for an agrochemical compound. 

Preparation of a saturated aldehyde

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Maastricht, Netherlands

Jeroen Antonius Franciscus Boogers