CAS: 1401-69-0; Tylosin

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20-Dihydrotylosin置于sodium Hypochlorite,2,2,6,6-四甲基哌啶氧化物,碳酸氢钠,Potassium Bromide体系中,用 乙酸乙酯 用作溶剂,化学反应 6.0H,反应生成泰乐菌素
参考文献:一种以泰乐菌素d为原料制备替米考星的方 法
标题:一种以泰乐菌素d为原料制备替米考星的方 法
摘要:本发明涉及一种以泰乐菌素d为原料制备替米考星的方法,该方法以泰乐菌素d为原料,通过选择性氧化剂将20位伯羟基氧化为醛基得到中间体1,再水解脱碳霉糖得到中间体2,通过甲酸与3,5二甲基哌啶还原氨化反应得到产品替米考星.本发明以泰乐菌素d为原料,通过特定的选择性氧化剂使泰乐菌素d转变为合成替米考星的有效成分,避免转变为杂质,为替米考星的制备开辟了一条新途径,解决了现有以泰乐菌素为起始原料制备替米考星的杂质残留高与收率偏低的问题.

专利信息

专利号:US-8518900-B2
优先权日:2006-07-28
标题 :Macrolide synthesis process and solid-state forms
发明人：WARRASS RALF; BLATTER FRITZ; BRENNER MEINRAD; HU GUIXAN; RAGER TIMO
权利人:WARRASS RALF; BLATTER FRITZ; BRENNER MEINRAD; HU GUIXAN; RAGER TIMO; INTERVET INT BV
摘要:Described are methods for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, among other uses, may be used to make macrolides. Also described are solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.