387353-77-7

Usage

Uses

Used in Hypertension Treatment:
Aliskiren inter-11 is used as an antihypertensive agent for lowering blood pressure. It works by inhibiting the enzyme renin, which in turn reduces the production of angiotensin II, a hormone that constricts blood vessels and increases blood pressure.
Used in Chronic Kidney Disease Management:
In patients with chronic kidney disease, aliskiren inter-11 is used to improve kidney function. By reducing the activity of renin and lowering angiotensin II levels, it helps to protect the kidneys from further damage and slow down the progression of the disease.
Used in Heart Failure Management:
Although still under investigation, aliskiren inter-11 has potential applications in the management of heart failure. Its ability to lower blood pressure and improve fluid balance may help alleviate symptoms and improve the overall prognosis of patients with heart failure.
Used in Diabetes Management:
Ongoing research is exploring the potential of aliskiren inter-11 in managing diabetes. Its effects on blood pressure and fluid balance may contribute to better glucose control and overall metabolic health in diabetic patients.
Used in Drug Development for Renin Inhibition:
As a direct renin inhibitor, aliskiren inter-11 serves as a valuable compound in the development of new drugs targeting the renin-angiotensin-aldosterone system (RAAS). Its unique mechanism of action and potential applications in various diseases make it an important candidate for further research and drug development.

InChI:InChI=1/C9H15ClO2/c1-7(2)8(5-4-6-10)9(11)12-3/h4,6-8H,5H2,1-3H3/b6-4+/t8-/m0/s1

Upstream product

• 475562-17-5 methyl (4E)-5-chloro-2-isopropyl-4-pentenoate 
• 51122-91-9 dimethyl isopropylmalonate 
• 705259-97-8 dimethyl 2-[(2E)-3-chloro-2-propenyl]-2-isopropyl malonate 
• 72651-95-7 5-isopropyl-2,2-dimethyl-[1,3]dioxane-4,6-dione 
• 67-56-1 methanol 
• 1350705-33-7 (S,E)-5-chloro-2-isopropyl pent-4-enoic acid phenyl ethanamine 
• 324519-66-6 (S)-(4E)-5-chloro-2-isopropyl-4-pentenoic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 87953-16-0 (4E)-5-chloro-2-isopropyl-4-pentenoic acid 

Downstream Products

• 387353-71-1 (2S,7R,E)-methyl 2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methylnon-4-enoate 
• 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 
• 325154-26-5 (2S,7R,E)-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-N,N,8-trimethylnon-4-enamide 
• 1350705-30-4 (2S,7R,E)-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methyl non-4-enoic acid tert-butylamine 
• 325740-70-3 (3S,5S)-5-((1S,3S)-1-azido-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-4-methylpentyl)-3-isopropyldihydrofuran-2(3H)-one 
• 324519-68-8 trans-(2S)-5-chloro-2-isopropyl-N,N-dimethyl-4-pentenamide 
• 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 
• 900811-48-5 (S)-5-((S)-1-amino-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-4-methylpentyl)-3-isopropyldihydrofuran-2(3H)-one 

Relevant academic research and scientific papers

PROCESS FOR PREPARING ALISKIREN AND ITS INTERMEDIATES

The present application relates to a process for the preparation of aliskiren and its pharmaceutically acceptable salts. In particular, the present application relates to a process for the preparation of intermediates for aliskiren, and their conversion to aliskiren or its salts.

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.

METHOD FOR PRODUCING OPTICALLY ACTIVE (4E)-5-CHLORO-2-ISOPROPYL-4-PENTENOIC ACID OR BASIC AMINO ACID SALT THEREOF

To provide a method for producing an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid, a basic amino acid salt thereof or an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid ester with high yield and high optical purity by simple operation. An optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid is obtained by precipitating a basic amino acid salt of optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid from a solvent solution containing an optical isomer mixture of (4E)-5-chloro-2-isopropyl-4-pentenoic acid and an optically active basic amino acid or a salt thereof, and then the basic amino acid salt of optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid is subjected to a desalting reaction. Further, an esterification reaction is carried out to obtain an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid ester.

PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE (4E)-5- HALO-2-ALKYLPENT-4-ENOIC ACIDS AND THEIR ESTER DERIVATIVES

A process for the preparation of optically active (4E)-5-halo-2-alkylpent-4-enoic acids and their ester derivatives by a stereoselective synthesis which employs camphorsultam as chiral auxiliary is disclosed; in particular methyl (2S, 4E)-5-chloro-2-isopropylpent-4-enoate is prepared, which is a key intermediate in the manufacturing of the new anti-hypertension drug Aliskiren. Furthermore novel N-(5-halo-2-alkylpent-4-enoyl) camphorsultams are provided. A process for the hydrolysis of substituted N-acylcamphorsultams with strong acids is also provided.

METHOD FOR PRODUCING (4E)-5-CHLORO-2-ISOPROPYL-4-PENTENOATE AND OPTICALLY ACTIVE SUBSTANCE THEREOF

To provide a process for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate in high yield and efficiently. A compound (2) is reacted with a base in the presence of an aprotic solvent and then with (1E)-1,3-dichloro-1-propene in the same reaction vessel to obtain a compound (3), and then either of -COOR moieties in the compound (3) is replaced with a hydrogen atom in the same reaction vessel to obtain a compound (4): wherein R is a lower alkyl group or an aralkyl group.

PROCESSES FOR PRODUCING (4E)-5-CHLORO-2-ISOPROPYL-4-PENTENOIC ESTER AND OPTICALLY ACTIVE ISOMER THEREOF

The present invention provides processes for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate and an optical isomer of the (4E)-5-chloro-2-isopropyl-4-pentenoate, namely a process for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate represented by the following formula (4), which comprises reacting a compound represented by the following formula (2) in the presence of an aprotic solvent (II) with a base (II) and then with (1E)-1,3-dichloro-1-propene to give a compound represented by the following formula (3), and dealkoxycarbonylating either ester in the compound represented by the following formula (3), and a process for producing a (S)-(4E)-5-chloro-2-isopropyl-4-pentenoate represented by the following formula (5), which comprises optically resolving a (4E)-5-chloro-2-isopropyl-4-pentenoate represented by the formula (4) obtained by the above-mentioned process (wherein R is a lower alkyl group or an aralkyl group).