1110767-89-9

Usage

Uses

Used in Pharmaceutical Industry:
(E)-3,5-dichloro-4-(3-ethoxy-2-methyl-3-oxoprop-1-enyl)benzoic acid is used as a key intermediate in the synthesis of Lusutrombopag (L474985) for the treatment of patients with chronic ITP. (E)-3,5-dichloro-4-(3-ethoxy-2-methyl-3-oxoprop-1-enyl)benzoic acid contributes to the development of a new class of drugs that target the thrombopoietin receptor, helping to increase platelet production and improve the condition of patients suffering from ITP.

Upstream product

• 153203-80-6 3,5-dichloro-4-formylbenzoic acid 
• 3699-66-9 ethyl 2-diethoxyphosphorylpropionate 
• 51-36-5 3,5-dichlorobenzoic acid 
• 4394-85-8 4-morpholinecarboxaldehyde 

Downstream Products

• 1110767-87-7 ethyl (S)-(E)-3-(2,6-dichloro-4-{4-[2-methyloxy-3-(1-methyloxyheptyl)phenyl]thiazol-2-ylcarbamoyl}phenyl)-2-methylacrylate 

Relevant academic research and scientific papers

Development of manufacturing processes for the carboxylic acid key intermediate of lusutrombopag: One-pot reaction process of formylation and the horner-wadsworth-emmons reaction

We describe the development of a one-pot preparation process of (E)-3,5-dichloro-4-(3-ethoxy-2-methyl-3-oxoprop- 1-en-1-yl)benzoic acid (3), which is a key carboxylic acid intermediate of lusutrombopag. This one-pot reaction process is composed of lithiation of 3,5-dichlorobenzoic acid with lithium diisopropylamide (LDA), formylation using N-formylmorpholine, followed by olefination employing the Horner-Wadsworth-Emmons reaction with triethyl 2-phosphonopropionate. This method enabled kilogram-scale manufacturing of carboxylic acid 3, a key intermediate of lusutrombopag with high purity, together with a reduced number of steps, improvement of yield, and avoidance of a cumbersome procedure for isolation of the intermediate.

PHARMACEUTICAL COMPOSITION CONTAINING OPTICALLY ACTIVE COMPOUND HAVING THROMBOPOIETIN RECEPTOR AGONIST ACTIVITY AND INTERMEDIATE THEREOF

An optically active 4-phenylthiazole derivative having a thrombopoietin receptor agonist activity and a pharmaceutical composition containing the present compound as an active ingredient are created, and a platelet production regulating agent which can be