Chemistry:Cetraxate
From HandWiki
Cetraxate (INN) is an oral gastrointestinal medication which has a cytoprotective effect.[1][2][unreliable medical source?]
Synthesis
Cetraxate is a prodrug of tranexamic acid. The latter is a hemostatic agent because it inhibits the activation of plasminogen to plasmin. The result is to prevent excess loss of blood in gastrointestinal ulcers. The synthesis begins with the esterification of 3-(p-hydroxyphenyl)propionic acid (2) by trans-4-cyanocyclohexanecarbonyl chloride (1). The product (3) is reduced to cetraxate (4) by catalytic hydrogenation with hydrogen and Raney nickel.[3][4]
References
- ↑ "Cytoprotective action of cetraxate against HCl.ethanol-induced gastric lesion in rats". Japanese Journal of Pharmacology 46 (1): 17–25. January 1988. doi:10.1254/jjp.46.17. PMID 3367546.
- ↑ "Effect of p-hydroxyphenyl-propionic ester of tranexamic acid hydrochloride (Cetraxate) on peptic ulcer. Multi-center clinical study". Arzneimittel-Forschung 29 (10): 1625–1632. 1979. PMID 391240.
- ↑ Japan Kokai, 59/134,758 (1984)
- ↑ "Tranexamic acid derivatives with enhanced absorption". Journal of Medicinal Chemistry 29 (4): 448–453. April 1986. doi:10.1021/jm00154a004. PMID 3959024.
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