Method for synthesizing certain selected pro-drug forms of theop

Details Method for synthesizing certain selected pro-drug forms of theop Method for synthesizing certain selected pro-drug forms of theop

1974-11-22

1976-12-28

Coughlan, Jr., Paul M.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260256, C07D47308

Patent

active

040001326

ABSTRACT:
There is provided, a method for synthesizing certain selected pro-drug forms of theophylline, having the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched C.sub.4 -C.sub.20 alkyl group, a straight or branched C.sub.4 -C.sub.20 alkenyl group, a substituted phenyl group or a substituted or unsubstituted naphthyl group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 acyloxy group, and a halogen atom and a substituted or unsubstituted heteroaromatic group whose substituents are selected from the group consisting of a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 acyloxy group, and a halogen atom, and wherein A represents a member selected from the group consisting of a --CO-- group, a --CO--(CH.sub.2).sub.n --CO-- group, wherein n represents an integer of from 1 to 16, a --CO--CH=CH--CO-- group (cis or trans) a ##STR2## group and a ##STR3## group, which comprises: Reacting theophylline with an appropriate acid in the presence of dimethylformamide, COCl.sub.2 or SOCl.sub.2, organic tertiary or aromatic amine base or inert carrier gas for removing HCl, and suitable solvent. The compounds prepared by this process are useful for treating asthma by releasing theophylline in sustained manner.

REFERENCES:
patent: 2729643 (1956-01-01), Stoll et al.

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