Process for the preparation of .beta.-methyldigoxin

Details Process for the preparation of .beta.-methyldigoxin Process for the preparation of .beta.-methyldigoxin

1984-05-21

1986-07-29

Brown, Johnnie R.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 5, 536120, C07J 1700

Patent

active

046031960

ABSTRACT:
The invention relates to a process for the preparation of .beta.-methyldigoxin by the selective methylation of digoxin with dimethyl sulfate in the presence of a basic strontium compound and, if appropriate, of an inert inorganic adsorbent. Strontium hydroxide octahydrate, strontium methylate or strontium hydroxymethylate is used as the basic strontium compound, and an oxide, silicate or phosphate of magnesium, calcium, aluminum, silicon or titanium, with a water content in the range of 0 to 20% by weight, is used as the inorganic adsorbent. The reaction is carried out at temperatures of -15.degree. to 15.degree. C. in the presence of 3 to 24 moles of water per mole of digoxin, the water being introduced in the reaction mixture by the water content of strontium hydroxide octahydrate and/or the inorganic adsorbent used and purification of the methylation product so formed by column chromatography on SiO.sub.2 with a mixture of chlorohydrocarbon and a lower aliphatic alcohol.

REFERENCES:
patent: 4145528 (1979-03-01), Pelan et al.

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