237073-61-9

Upstream product

• 314729-27-6 7-1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-8(S)-(2-methylbutyryloxy)-1(S)-naphthyl-3(R),5(R)-dihydroxyheptanoic acid 
• 237073-64-2 Ammonium-7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R),dimethyl-8(S)-(2-methylbutyryloxy)-1(S)-naphthyl]-3(R),5(R)-dihydroxyheptanoate 

Relevant academic research and scientific papers

PROCESS FOR SELECTIVE LACTONIZATION

The invention has its object to provide a method of lactonization for a compound of the general formula (1) in which the dimer formation reaction can be drastically inhibited. The invention provides a process for producing a compound of the general formula (2) ???comprising lactonizing a compound of the general formula (1) under conditions such that the solubility of the compound of the general formula (1) and/or the compound of the general formula (2) is not more than 0.5 w/w % to thereby give a compound of the general formula (2) with a dimer content of not more than 0.3 mole %.

Process of lactonization in the preparation of statins

An improved process of lactonization in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises treating the open ring hydroxy acid form of the statins with an excess of acetic acid and in the absence of a strong acid catalyst under mild heating conditions (e.g., ambient to 55° C.), and adding an anti-solvent to the reaction mixture, thereby causing the statins in lactone form to crystalize from the reaction mixture. The acetic acid serves as both a solvent and a catalyst for the lactonization reaction.

Process of lactonization in the preparation of statins

A novel process of lactonizaton in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises dissolving the open ring hydroxy acid form of the statins in an organic solvent by heating at a temperature, which ranges from ambient to reflux of the solvent, under anhydrous conditions to produce a solution, treating the solution with a mild catalyst at a temperature from about ambient to 50° C., and adding water to the solution to cause the statins in lactone form to crystalize from the reaction mixture. The mild catalyst used in the reaction is a salt of an organic base with an organic or inorganic acid, such as pyridine hydrobromide, pyridine hydrochloride, or pyridinium, p-toluene sulfonate. The organic solvent comprises a lower alkanol, a non-alcoholic polar solvent, or a mixture of the two.

Process for the lactonization of mevinic acids and analogs thereof

A process for the lactonization of mevinic acid HMG-CoA reductase inhibitors and analogs thereof is disclosed.