Synthesis of an Aza Isomer of 2-Deoxy-D-galantofuran

来源 :第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会 | 被引量 : 0次 | 上传用户:kldxn
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  Nitrogen-incorporated polyhydroxylated carbocylic ring systems,commonly known as azasugars or iminosugars1,which are widesperade in plants and microorganisms,2 exhibit significant glycosidase and glycosyltransferases inhibitory activity.3 Recent study have shown that these azasugars open the way to treat a wide range of diseases,including diabetes,viral infections,cystic fibrosis4,tumor metastasis and lysosomal storage disorders.Owing to their potent inhibition activity,a large number of natural and unnatural analogues have also been prepared and tested as therapeutically potent inhibitors.In this paper,we reported an Aza isomer of 2-deoxy-D-galantofuranose from the commercial available D-glucose through a series of reactions.The key step was hydrogenolysis of N-Cbz group to give in-situ formation of primary amine and concomitant reductive aminocyclization to give the polyhydroxylated pyrrolidine.It is believed this methodology of synthesizing azasugars will be generally applicable.
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