325154-26-5

Upstream product

• 1227379-41-0 (2S,7S,E)-7-(hydroxy(4-methoxy-3-(3-methoxypropoxy)phenyl)methyl)-2-isopropyl-N,N,8-trimethylnon-4-enamide 
• 172900-70-8 (R)-2-[4-methoxy-3-(3-methoxypropoxy)benzyl]-3-methylbutanol 
• 1350705-30-4 (2S,7R,E)-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methyl non-4-enoic acid tert-butylamine 
• 506-59-2 N,N-dimethylammonium chloride 
• 324763-39-5 (R)-2-[4-methoxy-3-(3-methoxypropoxyl)]phenylmethyl-3-methyl-1-chlorobutane 
• 324519-68-8 trans-(2S)-5-chloro-2-isopropyl-N,N-dimethyl-4-pentenamide 
• 503-74-2 3-methylbutyric acid 
• 172900-71-9 (R)-3-[4-methoxy-3-(3-methoxypropoxy)phenyl]-2-(1-methylethyl)propanoic acid 
• 172900-73-1 4-(bromomethyl)-1-methoxy-2-(3-methoxypropoxy)-benzene 
• 172900-74-2 [4-methoxy-3-(3-methoxypropoxy)-phenyl]methanol 
• 172900-75-3 4-methoxy-3-(3-methoxypropoxy)benzaldehyde 
• 324519-67-7 (S,E)-ethyl 5-chloro-2-isopropylpent-4-enoate 
• 387353-77-7 methyl (S)-(4E)-5-chloro-2-isopropyl-4-pentenoate 
• 387353-70-0 (2S,7R,E)-ethyl 2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methylnon-4-enoate 

Downstream Products

• 1227379-42-1 (3S)-5-((3S)-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-1-bromo-4-methylpentyl)-3-isopropyl-dihydrofuran-2(3H)-one 
• 393108-57-1 (3S,5S)-5-{(1R,3S)-1-bromo-3-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-4-methylpentyl}-dihydro-3-(1-methylethyl)furan-2(3H)-one 
• 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 
• 324763-47-5 (2S,4S,5S,7S)-N-(3-amino-2,2-dimethyl-3-oxopropyl)-5-azido-4-hydroxy-2-isopropyl-7-(4-methoxy-3-(methoxypropoxy)benzyl)-8-methylnonanamide 
• 325740-70-3 (3S,5S)-5-((1S,3S)-1-azido-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-4-methylpentyl)-3-isopropyldihydrofuran-2(3H)-one 
• 324763-46-4 (3S,5S)-5-{(1S,3S)-1-azido-3-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-4-methylpentyl}-dihydro-3-(1-methylethyl)furan-2(3H)-one 
• 393108-57-1 C₂₅H₃₉BrO₅ 
• 1373444-03-1 C₃₀H₄₉N₅O₅ 

Relevant academic research and scientific papers

A aliskiren or its salt separation and analysis method

The invention relates to a separation analysis method using polysaccharide derivative-bonded and coated silica as a stationary phase and an organic solvent as a mobile phase for separation analysis of aliskiren and isomers thereof, effective separation of the aliskiren and isomers thereof can be realized, and the separation analysis method has the important meaning to the product quality control.

PROCESS FOR THE PREPARATION OF ALISKIREN

The present invention relates to an improved process for the preparation of pure compound of Formula-II, which is an intermediate in the preparation of Aliskiren and further conversion of compound of Formula-II into Aliskiren or its pharmaceutically accep

Investigation of a kumada cross coupling reaction for large-scale production of (2 S, 7 R, E)-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)- N, N,8-trimethylnon-4-enamide

An investigation into the Kumada cross coupling reaction was conducted by developing a reliable, efficient procedure for the Grignard reagent and its subsequent cross coupling reaction. Safe Mg metal activation as well as a moisture-free system was create

The development of a complementary pathway for the synthesis of aliskiren

The synthesis of aliskiren (1), a recently marketed drug for the treatment of hypertension, is presented. The focus of our synthetic effort is to develop an efficient pathway for the synthesis of (2S,7R,E)-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy) benzyl)-N,N,8-trimethylnon-4-enamide (2a), which has been used as the advanced intermediate toward aliskiren. After an extensive investigation of three different strategies designed to construct the E-olefin functionality in 2a by employing the olefin cross-metathesis, Horner-Wadsworth-Emmons (HWE), and Julia-type olefinations, we have established a new protocol for the synthesis of 2a with a substantially improved overall efficiency in terms of the yield (ca. 33%), and diastereo- and E/Z-selectivity. The key transformations were the Evans chiral auxiliary-aided asymmetric allylation for the synthesis of the appropriate chiral intermediates in excellent enantiomeric purity of higher than 97% ee and a modified Julia-Kocienski olefination for the highly selective construction of E-2a with up to 13.6:1 E/Z ratio from the chiral intermediates. Consequently, the results provide an appealing option for the synthesis of aliskiren. This journal is

AN IMPROVED PROCESS FOR THE PREPARATION OF ALISKIREN

The present invention relates to an improved process for the preparation of renin inhibitor Aliskiren intermediates of Formula-II and further conversion into Aliskiren and its pharmaceutically acceptable salts.

AN IMPROVED PROCESS FOR THE PREPARATION OF ALISKIREN

The present invention relates to an improved process for the preparation of pure compound of Formula-II, which is an intermediate in the preparation of Aliskiren and further conversion of compound of Formula-II into Aliskiren or its pharmaceutically acceptable salts.

SYNTHESIS OF ALISKIREN

The present invention provides novel process for the preparation of renin inhibitor Aliskiren or its derivatives, and its pharmaceutically acceptable salts. The present invention also provides novel intermediates used in the preparation of Aliskiren.

PROCESS FOR THE PREPARATION OF (2S,4S,5S,7S)-N-(2-CARBAMYL-2- METHYLPROPYL)-5-AMINO-4-HYDROXY-2,7-DIISOPROPYL-8-[4-METHOXY-3-(3- METHOXYPROPOXY)PHENYL]-OCTANAMIDE HEMIFUMARATE AND ITS INTERMEDIATES THEREOF

The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.

AMIDE INHIBITORS OF RENIN

The present invention relates to new amide inhibitors of renin, pharmaceutical compositions thereof, and methods of use thereof