866030-34-4

Upstream product

• 866030-33-3 (2R,5S)-3,6-diethoxy-2-isopropyl-5-((S)-2-(4-methoxy-3-(3-methoxypropoxy)benzyl)-3-methylbutyl)-2,5-dihydropyrazine 
• 621-59-0 isovanillin 
• 916793-76-5 (2R,3S,5S)-tert-butyl 5-((1S,3S)-3-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-1-hydroxy-4-methylpentyl)-3-isopropyl-2-(4-methoxy-3-(3-methoxypropoxy)phenyl)pyrrolidine-1-carboxylate 
• 916793-72-1 (2R,3S,5S)-5-((1S,3S)-3-benzyloxymethyl-1-hydroxy-4-methyl-pentyl)-3-isopropyl-2-[4-methoxy-3-(3-methoxy-propoxy)-phenyl]pyrrolidine-1-carboxylic acid tert-butyl ester 
• 172900-75-3 4-methoxy-3-(3-methoxypropoxy)benzaldehyde 
• 145589-03-3 (R)-4-benzyl-3-(3-methylbutyryl)oxazolidin-2-one 
• 172900-83-3 (1S,3S)-{1-formyl-3-[4-methoxy-3-(3-methoxy-propoxy)-benzyl]-4-methyl-pentyl}-carbamic acid tert-butyl ester 
• 172900-92-4 (1S,4S,2'S)-(4-benzyloxymethyl-2-hydroxy-1-{2'-[4-methoxy-3-(3-methoxypropoxy)benzyl]-3-methylbutyl}-5-methylhexyl)carbamic acid tert-butyl ester 
• 172900-69-5 (R)-4-(2-(bromomethyl)-3-methylbutyl)-1-methoxy-2-(3-methoxypropoxy)benzene 
• 172900-74-2 [4-methoxy-3-(3-methoxypropoxy)-phenyl]methanol 
• 172900-73-1 4-(bromomethyl)-1-methoxy-2-(3-methoxypropoxy)-benzene 
• 172900-72-0 (4R)-3-{(2R)-2-{[4-methoxy-3-(methoxypropoxy)phenyl]methyl-3-methyl}-1-oxobutyl}-4-(phenylmethyl)oxazolidin-2-one 
• 172900-99-1 (2S,4S)-2-Amino-4-[4-methoxy-3-(3-methoxy-propoxy)-benzyl]-5-methyl-hexanoic acid ethyl ester 
• 656241-26-8 (2S)-3-methyl-2-[(phenylmethoxy)methyl]butanoic acid 

Downstream Products

• 866030-35-5 tert-butyl {(1S,3S)-1-((2S,4S)-4-isopropyl-5-oxotetrahydrofuran-2-yl)-3-[4-methoxy-3-(3-methoxypropoxy)benzyl]-4-methylpentyl}carbamate 
• 173334-57-1 (2S,4S,5S,7S)-5-Amino-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxy-propoxy)-benzyl]-8-methyl-nonanoic acid (2-carbamoyl-2-methyl-propyl)-amide 
• 173338-07-3 tert-butyl (3S,5S,6S,8S)-8-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-6-hydroxy-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-2,9-dimethyldecan-5-ylcarbamate 

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.

Practical synthesis of an orally active renin inhibitor aliskiren

A convergent synthesis of aliskiren was accomplished via the use of Segment AB as the key intermediate, which was prepared via the coupling of the Grignard reagent derived from Segment B with Segment A, followed by subsequent oxidative lactonization.