8311. Saccharin

Nomenclature

CAS number: 81-07-2
1,2-Benzisothiazol-3(2H)-one 1,1-dioxide; 2,3-dihydro-3-oxobenzisosulfonazole; 1,2-dihydro-2-ketobenzisosulfonazole; saccharin insoluble; benzosulfimide; o-sulfobenzimide; benzoic sulfimide; o-sulfobenzoic acid imide; Gluside; Glucid; Garantose; Saccharinol; Saccharinose; Saccharol; Saxin (Burroughs Wellcome); Sykose; Hermesetas.
C7H5NO3S; mol wt 183.18.
C 45.90%, H 2.75%, N 7.65%, O 26.20%, S 17.50%.

Description and references

Prepn from o-sulfamoylbenzoic acid: Remsen, Fahlberg, Ber. 12, 470 (1879). History and comparison with other sweetening agents: R. W. Moncrieff, The Chemical Senses (Wiley, New York, 1946). Mfg processes: O. Beyer, Handbuch der Saccharinfabrikation (Rascher, Zürich, 1923); FIAT Report PB 901 (1945); Chem. Eng. (N.Y.) 61, 128, 150 (July 1954). Maumee Chemical's process: Chem. Eng. News 41, 76-78 (Dec. 9, 1963). Stability studies: DeGarmo et al., J. Am. Pharm. Assoc. Sci. Ed. 41, 17 (1952). Toxicity data: J. D. Taylor et al., Food Cosmet. Toxicol. 6, 313 (1968). Series of articles on toxicology and metabolism: Food Chem. Toxicol. 23, 419-546 (1985). Review of toxicology and carcinogenicity studies of saccharin and its salts: IARC Monographs 22, 111-170 (1980); D. L. Arnold, Fundam. Appl. Toxicol. 4, 674-685 (1984). Review: R. Mazur, “Sweeteners” in Kirk-Othmer Encyclopedia of Chemical Technology vol. 22 (John Wiley & Sons, New York, 3rd ed., 1983) pp 448-464.

Chemical structure

Properties

Monoclinic crystals, mp 228.8-229.7°. Twinning on (001). Perfect 100 cleavage. Acicular crystals by vacuum sublimation. In dil aq soln it is 500 times as sweet as sugar; the sweet taste is still detectable in 1:100,000 dilution. Bitter, metallic aftertaste. d 0.828. Heat of combustion at constant volume: 4753.1 cal/g. uv max (0.1N NaOH): 267.3 nm (ε 1570). One gram dissolves in 290 ml water, 25 ml boiling water, 31 ml alcohol, 12 ml acetone, about 50 ml glycerol; freely sol in solns of alkali carbonates; slightly sol in chloroform, ether. pH of 0.35% aq soln 2.0. Hydrolysis products of saccharin are o-sulfamoylbenzoic acid (alkaline hydrolysis) and ammonium o-sulfobenzoic acid (acid hydrolysis).

Derivative

Ammonium salt.

Nomenclature

Saccharin ammonium; Daramin; Sucline (Soekami).
C7H8N2O3S; mol wt 200.22.
C 41.99%, H 4.03%, N 13.99%, O 23.97%, S 16.01%.

Derivative

Sodium salt dihydrate.

Nomenclature

Soluble saccharin; saccharin sodium; Kristallose; Crystallose (Tenneco); Dagutan; Sucaryl (Abbott); Sucromat (Mayoly-Spindler).
C7H4NNaO3S.2H2O; mol wt 241.20.
C 34.86%, H 3.34%, N 5.81%, Na 9.53%, O 33.17%, S 13.29%.

Properties

Crystalline powder; effloresces in dry air. In dil aq soln it is 300-500 times as sweet as sugar. One gram dissolves in 1.2 ml water, in about 50 ml alcohol. Aq solns are neutral or alkaline to litmus, but not alkaline to phenolphthalein. LD50 in mice, rats (g/kg): 6.3, 7.1 i.p.; 17.5, 17.0 orally (Taylor). Anhydrous form, Sucrédulcor.

Note

Saccharin was formerly listed as reasonably anticipated to be a human carcinogen: Eighth Report on Carcinogens (PB99-128746, 1998) p III-905; delisted because the cancer data are not sufficient to meet the current criteria for this listing: Ninth Report on Carcinogens (PB2000-107509, 2000) p B-3.

Use

Non-nutritive sweetener; pharmaceutic aid (flavor). In formulations for electroplating-bath brighteners.