Saltar al contenido
MilliporeSigma

Efficient and scalable synthesis of bardoxolone methyl (cddo-methyl ester).

Organic letters (2013-03-28)
Liangfeng Fu, Gordon W Gribble
RESUMEN

Bardoxolone methyl (2-cyano-3,12-dioxooleane-1,9(11)-dien-28-oic acid methyl ester; CDDO-Me) (1), a synthetic oleanane triterpenoid with highly potent anti-inflammatory activity (levels below 1 nM), has completed a successful phase I clinical trial for the treatment of cancer and a successful phase II trial for the treatment of chronic kidney disease in type 2 diabetes patients. Our synthesis of bardoxolone methyl (1) proceeds in ∼50% overall yield in five steps from oleanolic acid (2), requires only one to two chromatographic purifications, and can provide gram quantities of 1.

MATERIALES
Referencia del producto
Marca
Descripción del producto

Sigma-Aldrich
Oleanolic acid, ≥97%
En este momento no podemos mostrarle ni los precios ni la disponibilidad
Supelco
Oleanolic acid, analytical standard
En este momento no podemos mostrarle ni los precios ni la disponibilidad