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Selective N-desulfation of heparin with dimethyl sulfoxide containing water or methanol.
Authors:Y Inoue  K Nagasawa
Affiliation:School of Pharmaceutical Sciences, Kitasato University, 9-1, Shirokane, 5 Chome, Minato-ku, Tokyo 108 Japan
Abstract:A solvolytic N-desulfation of heparin was developed by treatment of its pyridinium salt with dimethyl sulfoxide containing 5% of water or methanol for 1.5 h at 50 degrees. Chemical and chromatographic studies showed that the solvolytic desulfation is a useful method for N-desulfation of heparin without depolymerization of the heparin molecule. The partially N-desulfated heparins were also obtained by treatment with dimethyl sulfoxide containing 5% of water at 20 degrees, and their anticoagulant activity is related to the degree of N-desulfation.
Keywords:To whom correspondence should be addressed.
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