| 摘要 |
The present invention relates to furanoid sugar amino acids and their salts which carrying an additional chiral center at C6-position with substituents and resembling the side-chains of natural amino acids. More particularly, 6-substituted-6-deoxy-6-amino-2,5-anhydroaldonic acids and their 3,4-dideoxy congeners, in enantiomerically pure forms, which constitute an important class of conformationally constrained peptide building blocks that can be used as dipeptide isosteres in peptidomimetic studies. R<SUP>1</SUP>=H, Boc, Cbz, Fmoc, acetyl or salts such as HCl, TFA R<SUP>2</SUP>=CH<SUB>3</SUB>-, (CH<SUB>3</SUB>)<SUB>2</SUB>CH-, (CH<SUB>3</SUB>)<SUB>2</SUB>CHCH<SUB>2</SUB>-, CH<SUB>3</SUB>CH<SUB>2</SUB>CH(CH<SUB>3</SUB>)-, alkyl groups, OR<SUP>3</SUP>)CH<SUB>2</SUB>-, CH<SUB>3</SUB>(OR<SUP>3</SUP>)CH-, (R<SUP>3</SUP>S)CH<SUB>2</SUB>-, CH<SUB>3</SUB>SCH<SUB>2</SUB>CH<SUB>2</SUB>-, (RHN)CH<SUB>2</SUB>CH<SUB>2</SUB>CH<SUB>2</SUB>CH<SUB>2</SUB>-, (CONH<SUB>2</SUB>)CH<SUB>2</SUB>-, (CONH<SUB>2</SUB>)CH<SUB>2</SUB>CH<SUB>2</SUB>-, (CO<SUB>2</SUB>R<SUP>5</SUP>)CH<SUB>2</SUB>-, (CO<SUB>2</SUB>R<SUP>5</SUP>)CH<SUB>2</SUB>CH<SUB>2</SUB>-, Ph-, Ar-, PhCH<SUB>2</SUB>-, ArCH<SUB>2</SUB>-, Phenylalkyl-, arylalkyl-, (indolyl)CH<SUB>2</SUB>-, (imidazolyl)CH<SUB>2</SUB>-, and all other amino acid side-chains R<SUP>3</SUP>=H, tert-butyl, alkyl, benzyl, arylCH<SUB>2</SUB>, CO(alkyl), CO(arylalkyl), SO<SUB>3</SUB>H, PO<SUB>3</SUB>H<SUB>2</SUB>, silyl, R<SUB>4</SUB>=-O-alkyl, -O-arylalkyl, -amine, -alkylamine, -arylalkylamine, and others R<SUB>5</SUB>=H, tert-butyl, alkyl, benzyl, arylCH<SUB>2</SUB>, R<SUP>1</SUP>-R<SUP>2</SUP>=-(CH<SUB>2</SUB>)<SUB>n</SUB>- (n=2,3,4)
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