Hypocholesteremic agents

A series of hypocholesteremic agents were isolated from Monascus and named monacolin J, K, and L. These polyketides were first isolated from cultures of Penicillium citrinum and they can inhibit specifically the enzyme controlling the rate of cholesterol biosynthesis. They are currently used in China in traditional and modem medicine. 

Kozikowski and Li (268) also made use of this protocol for the construction of the hexahydronaphthalene portion of the hypocholesteremic agent compactin (256) (see Section 6.4.2.2). The oxime derived by from alcohol 253 (via y-lactone 252) was heated with aqueous sodium hypochlorite in the presence of triethylamine to give the tricyclic isoxazoline adduct 254 (Scheme 6.96). Reductive hydrolysis and dehydration afforded enone 255, which in several further steps led to compactin (256) (268). 

Clofibrate (91) has been in clinical use for several years as a serum triglyceride lowering agent. This drug is an important hypocholesteremic... 

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