24. Acefylline

Nomenclature

CAS number: 652-37-9
1,2,3,6-Tetrahydro-1,3-dimethyl-2,6-dioxo-7H-purine-7-acetic acid; carboxymethyltheophylline; 7-theophyllineacetic acid.
C9H10N4O4; mol wt 238.20.
C 45.38%, H 4.23%, N 23.52%, O 26.87%.

Description and references

Prepn: DE 352980 (1922 to E. Merck); Frdl. 14, 1320; S. M. Ride et al., Pharmazie 32, 672 (1977) PubMed. Prepn of salts: J. Baisse, Bull. Soc. Chim. Fr. 1949, 769; M. Milletti, F. Virgili, Chimica 6, 394 (1951), C.A. 46, 8615h (1952). GC determn in urine: J. Zuidema, H. Hilbers, J. Chromatogr. 182, 445 (1980) DOI PubMed. HPLC determn in serum and pharmacokinetics: S. Sved et al., Biopharm. Drug Dispos. 2, 177 (1981) DOI PubMed.

Chemical structure

Properties

Crystals from water, mp 271°.

Derivative

Sodium salt.

Nomenclature

CAS number: 837-27-4
C9H9N4NaO4; mol wt 260.18.
C 41.55%, H 3.49%, N 21.53%, Na 8.84%, O 24.60%.

Properties

Silky needles, mp >300°.

Derivative

Compd with piperazine.

Nomenclature

Acefylline piperazine; acepifylline; Dynaphylline (Welcker-Lyster); Etaphylline (Delalande); Etafillina (Delalande).

Properties

Undefined mixture of the 1:1 and 2:1 salts; contains 75-78% theophylline acetic acid and 22-25% anhydrous piperazine.

Therapeutic Category

Bronchodilator.

Keywords

Bronchodilator; Xanthine Derivatives