Caffeine derivatives

Details Caffeine derivatives Caffeine derivatives

1974-09-23

1976-08-17

Coughlan, Jr., Paul M.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424253, 260256, C07D47312

Patent

active

039753891

ABSTRACT:
New derivatives of caffeine are disclosed having the formula: ##SPC1##
Where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, chlorine, bromine, an alkyl or an alkoxy radical containing from 1 to 4 carbon atoms. They are made by transforming 8-.alpha. hydroxyethyl caffeine into the corresponding 8-.alpha.-chloroethyl caffeine by the action of a suitable chlorinating agent such as thionyl chloride, reacting the product so obtained in a suitable solvent such as anhydrous dimethylformamide at a temperature from 40.degree. to 110.degree. C and for a period of time from 1 to 5 hours with the sodium or potassium salt of a nicotinic acid of the formula: ##SPC2##
Where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the above-mentioned meanings, and crystallizing the resulting product from a suitable solvent, such as ethanol. These new compounds have broncholitic activity.

REFERENCES:
patent: 2879271 (1959-03-01), Kallischnigy
Wagner et al., Synthetic Organic Chemistry Wiley & Sons Inc., New York, 1953.

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