公开(公告)号：EP1257558A1

公开(公告)日：2002-11-20

申请号：EP01901031.3

申请日：2001-01-12

申请人： Alchemia Pty Ltd

发明人： BORNAGHI, Laurent ,  DEKANY, Gyula ,  DRINNAN, Nicholas, Barry ,  PAPAGEORGIOU, John ,  WEST, Michael, Leo

IPC分类号： C07H15/18 ,  C07H17/04 ,  C07H15/26 ,  C07H15/08 ,  C07H23/00 ,  C07H15/12 ,  C07H1/00 ,  C07H5/04 ,  C07H3/04 ,  C07D493/04 ,  A61K31/702 ,  A61K31/7016

CPC分类号： C07D493/04 ,  C07B2200/11 ,  C07H13/12 ,  C07H15/08 ,  C07H15/14 ,  C07H15/18

摘要： This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R3 is methoxy or methyl; R1 is H, benzoyl, pivaloyl, , 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.

摘要翻译： 本发明涉及用于合成包含α-D-Gal（1→3）-D-Gal的生物活性二糖和三糖的试剂和方法。 特别地，本发明提供用于溶液或固相合成α-D-吡喃半乳糖基 - （1→3）-D-半乳糖及其衍生物的新试剂，中间体和方法。 在一个优选实施方案中，本发明提供了通式（II）的受保护的单糖结构单元：其中R 3是甲氧基或甲基; 乙酰基，氯乙酰基，乙酰丙酰基，4-甲基苯甲酰基，苄基，3,4-亚甲二氧基苄基，4-甲氧基苄基，4-氯苄基，4-乙酰氨基苄基或4-叠氮基苄基; 乙酰基，氯乙酰基，乙酰丙酰基，4-甲基苯甲酰基，苄基，3,4-亚甲二氧基苄基，4-甲氧基苄基，4-氯苄基，4-乙酰氨基苄基或4-叠氮基苄基。