[EN] RAPAMYCIN CARBOHYDRATE DERIVATIVES<br/>[FR] DERIVES DE RAPAMYCINE CARBOHYDRATE
申请人:ISOTECHNIKA INTERNAT INC
公开号:WO2004101583A1
公开(公告)日:2004-11-25
This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin carbohydrate derivatives having enhanced pharmacokinetic and/or pharmacodynamic profiles. For example, administration of the rapamycin carbohydrate derivative results in altered pharmacokinetic profiles and reduced toxicities. Thus, the present invention provides compounds with characteristics that are distinct from other drugs in its class such as rapamycin.
Conversion of fructose into 5-hydroxymethylfurfural (HMF) and its derivatives promoted by inorganic salt in alcohol
作者:Jitian Liu、Yu Tang、Kaigui Wu、Caifeng Bi、Qiu Cui
DOI:10.1016/j.carres.2011.12.006
日期:2012.3
The conversion of D-fructose to 5-hydroxymethylfurfural (HMF) on a 1 mmol scale was achieved in good yield (68%) using NH(4)Cl as catalyst in isopropanol at 120°C. About 3% of 5-i-propoxymethylfurfural was formed. The reaction in ethanol at 100°C on a 10g scale gave a total yield of HMF and 5-ethoxymethylfurfural of 42%. No mineral acid such as H(2)SO(4) and HCl are required.
This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin carbohydrate derivatives having enhanced pharmacokinetic and/or pharmacodynamic profiles. For example, administration of the rapamycin carbohydrate derivative results in altered pharmacokinetic profiles and reduced toxicities. Thus, the present invention provides compounds with characteristics that are distinct from other drugs in its class such as rapamycin.