发明名称 METHOD OF SYNTHESIS OF SUBSTITUTED HEXITOLS SUCH AS DIANHYDROGALACTITOL
摘要 The present invention provides an efficient method of synthesizing and purifying dianhydrohexitols such as dianhydrogalactitol. In general, as applied to dianhydrogalactitol, the method comprises: (1) reacting dulcitol with a concentrated solution of hydrobromic acid at a temperature of about 80� C. to produce dibromogalactitol; (2) reacting the dibromogalactitol with potassium carbonate in t-butanol to produce dianhydrogalactitol; and (3) purifying the dianhydrogalactitol using a slurry of ethyl ether to produce purified dianhydrogalactitol. Another method produces dianhydrogalactitol from dulcitol; this method comprises: (1) reacting dulcitol with a reactant to convert the 1,6-hydroxy groups of dulcitol to an effective leaving group to generate an intermediate; and (2) reacting the intermediate with an inorganic weak base to produce dianhydrogalactitol through an intramolecular SN2 reaction. Other methods for the synthesis of dianhydrogalactitol from dulcitol are described.
申请公布号 US2014066642(A1) 申请公布日期 2014.03.06
申请号 US201314072603 申请日期 2013.11.05
申请人 DEL MAR PHARMACEUTICALS 发明人 BROWN DENNIS M.;LI MIKE TSO-PING
分类号 C07D301/19;C07D303/14 主分类号 C07D301/19
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