916793-67-4

Upstream product

• 934298-33-6 (2S,4S,5R)-4-isopropyl-5-[4-methoxy-3-(3-methoxy-propoxy)-phenyl]-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester 2-ethyl ester 
• 916793-69-6 {(2S,4S,5R)-4-isopropyl-5-[4-methoxy-3-(3-methoxy-propoxy)-phenyl]-pyrrolidin-2-yl}-methanol (Z)-but-2-enedioic acid 

Downstream Products

• 916793-70-9 (2R,3S,5S)-5-formyl-3-isopropyl-2-[4-methoxy-3-(3-methoxy-propoxy)-phenyl]pyrrolidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

SYTHESIS OF RENIN INHIBITORS INVOLVING A CYCLOADDITION REACTION

The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula (III), wherein R, R1, and R' are as defined in the specification, or a salt thereof, and a compound of formula (IV) wherein R, R1, R2 and R' are as defined in the specification, and processes of manufacturing these.

ORGANIC COMPOUNDS

The invention related to a novel process, novel process Steps and novel intermediates useful in the synthesis of pharmaceutically active Compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a Compound of the formula III, wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof, said manufacture comprising (preferably consisting in) reacting a Compound of the formula I, (I) with a reagent able to transform hydroxy into X where X is for example a leaving group.