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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. C07C/14 Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups. Aliskiren, a renin inhibitor drug, has received considerable attention, primarily Herein, the formal synthesis of aliskiren by iridium‐catalyzed.


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Angiotensin II has both direct and indirect effects on blood pressure. Aliskiren is also available as combination therapy aliskiren synthesis hydrochlorothiazide. However, when these drugs are used chronically, the body increases renin production, which drives blood pressure up again.

WOA1 - Synthesis of aliskiren - Google Patents

Therefore, doctors have been looking for a drug to inhibit renin directly. Aliskiren is the first drug aliskiren synthesis do so.


Caution should be exercised when aliskiren is administered with ketoconazole or other moderate P-gp inhibitors itraconazole, clarithromycin, telithromycin, erythromycin, or amiodarone.

The base used here may be organic or inorganic base, preferably inorganic base such as alkaline earth metal hydroxides, carbonates, bicarbonates etc. The process comprises reducing the azide group of compound of Formula-IV in the presence of alcoholic solvents and isolating Aliskiren or its pharmaceutically acceptable salts.

In one embodiment, the reduction aliskiren synthesis compound of Formula-IV is carried out in the presence of Palladium catalyst. In one more embodiment, alcoholic solvents used in the reduction of azide intermediate is selected from ethanol, methanol and isopropanol, preferably methanol aliskiren synthesis ethanol.

USB2 - Synthesis of Aliskiren - Google Patents

The prior art processes involves the use of tert-butyl methyl ether as a solvent in the reduction of azide intermediate. Aliskiren synthesis yield obtained by this process is low.

In one more embodiment the lactone compound of Formula-II is aliskiren synthesis by the conventional prior art methods for example disclosed in U.

The compound of Formula-II is alternatively prepared by cyclisation and azidation of the compound of Formula-V. The process for the preparation of compound of Formula-II from compound of Aliskiren synthesis is schematically shown below.

Formal total synthesis of aliskiren.

Present invention provides purification of compound aliskiren synthesis formula V aliskiren synthesis using fractional distillation method. The condensation of compound of Formula-A and compound of Formula-B takes place in the presence of alkali or alkaline earth metals like magnesium.


The coupling of Grignard reagents with compound of formula B in an ether such as, for example, tetrahydrofuran, methyl tetrahydrofuran or dioxan as solvents in the presence of catalytic quantities of a soluble metal complex, for example an iron complex such as iron acetonyl acetate, and in the presence of more than equimolar quantities of a solvent stabilizing the metal complex, for example N-methylpyrrolidone.

It is expedient to carry out the reaction so aliskiren synthesis initially a compound of formula-A is converted to a Grignard compound for example with magnesium and then adding a solution of a compound of formula-B, metal complex and N-methylpyrrolidone, or vice versa.

This purity will enhance the purity of Aliskiren. The compounds of Formula-A and Formula-B are prepared as per the conventional methods, for example the processes disclosed in U. Process for the preparation of Aliskiren as per the present invention, is summarized in the scheme-I.

In one embodiment, the compound of Formula-III is converted into Aliskiren or its pharmaceutically acceptable salts thereof.

Aliskiren - Wikipedia

The following examples are provided to illustrate the process of the present invention. They, are however, not intended to limiting the scope of the present invention in any way and several variants of these examples would be evident to person ordinarily skilled in the art.

The reaction mixture was concentrated to remove excess thionyl chloride aliskiren synthesis the residue was diluted with dichloromethane and washed with saturated sodium hydrogen carbonate solution.

The dichloromethane solution was aliskiren synthesis washed with brine and concentrated to get 3-Amino-2,2-dimethyl-propionitrile as an oil.