PREPARATION OF 7-HYDROXYPROSTACYCLINE DERIVATIVE
PURPOSE:To prepare the titled compound useful as pharmaceuticals or their intermediates, from an easily available raw material, in high efficiency, by reacting a 7-hydroxyprostaglandin F2alpha derivative with a mercury compound in an inert organic medium, and treating the product with a borohydride...
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Zusammenfassung: | PURPOSE:To prepare the titled compound useful as pharmaceuticals or their intermediates, from an easily available raw material, in high efficiency, by reacting a 7-hydroxyprostaglandin F2alpha derivative with a mercury compound in an inert organic medium, and treating the product with a borohydride compound. CONSTITUTION:The compound of formula III can be prepared economically by reacting the compound of formula I [the dotted line is a bond which may be present or absent; G is CO2R , etc.; R is H, 1-10C alkyl, etc.; R is H, CH , CHidenticalCH, etc.; R is 5-8C alkyl, alicyclic group, etc.; R and R are H, 2- 7C acyl, tri(1-7C hydrocarbon group)-silyl, etc.; the configuration between the 8 and 9 positions is trans.] with a mercury compound, preferably a mercury salt of carboxylic acid (e.g. mercury acetate), a mercury halide (especially mercury chloride) or mercury oxide, in an inert organic medium, and reacting the reaction product preferably with a borohydride compound of formula II (M is alkali metal; R8 is 1-6C alkyl, 1-6C alkoxy, or CN; m is integer of 1-4), especially sodium borohydride, etc. |
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