1007358-76-0

Usage

Uses

Used in Pharmaceutical Industry:
Ambrisentan is used as an antihypertensive agent for the treatment of pulmonary arterial hypertension (PAH). It works by blocking the endothelin ETA receptors, which helps to relax the blood vessels and reduce blood pressure in the lungs. This, in turn, improves the symptoms and overall quality of life for patients suffering from PAH.
Additionally, ambrisentan may have potential applications in other areas of medicine, such as the treatment of other forms of hypertension or cardiovascular diseases. However, further research and clinical trials are necessary to establish its efficacy and safety in these contexts.

Upstream product

• 35144-22-0 4,6-dimethyl-2-methylsulfonylpyrimidine 
• 178306-51-9 (S)-2-hydroxy-3-methoxy-3,3-diphenyl propionic acid 
• 1260633-84-8 (S)-1-(3-methoxyphenyl)ethylammonium (S)-2-hydroxy-3-methoxy-3,3-diphenylpropionate 
• 177036-94-1 ambrisentan 

Downstream Products

• 177036-94-1 ambrisentan 

Relevant academic research and scientific papers

Process Research for (+)-Ambrisentan, an Endothelin-A Receptor Antagonist

An efficient and robust synthetic route to (+)-ambrisentan ((+)-AMB) was designed by recycling the unwanted isomer from the resolution mother liquors. The racemization of AMB in the absence of either acid or base in the given solvents was reported. The recovery process was developed to produce racemates with purities over 99.5%. The mechanism of the formation of the process-related impurities of (+)-AMB is also discussed in detail. (+)-AMB was obtained in 47% overall yield with >99.5% purity and 99.8% e.e. by chiral resolution with only one recycling of the mother liquors on a 100-g scale without column purification.

PROCESS FOR THE PREPARATION OF AMBRISENTAN AND NOVEL INTERMEDIATES THEREOF

The invention relates to improved processes for the preparation of ambrisentan. The invention also relates to a novel intermediate useful in the preparation of ambrisentan and a process for the preparation of the intermediate. The invention also relates to new polymorphic form of ambrisentan. In particular, it relates to a polymorphic form, designated as Form I of ambrisentan and a process for the preparation of the Form I.

IMPROVED PROCESS FOR THE PREPARATION OF AMBRISENTAN AND NOVEL INTERMEDIATES THEREOF

The invention relates to improved processes for the preparation of ambrisentan. The invention also relates to a novel intermediate useful in the preparation of ambrisentan and a process for the preparation of the intermediate. The invention also relates to new polymorphic form of ambrisentan. In particular, it relates to a polymorphic form, designated as Form I of ambrisentan and a process for the preparation of the Form I.