申请人:SYMBICOM AB
公开号:EP0239194A2
公开(公告)日:1987-09-30
A method for preparing an unprotected hydroxy compound from a protected hydroxy compound of the general formula I
in which R, is the non-hydroxy moiety of the protected hydroxy compound; R2, R3, R4 and R5 which may be the same or different are hydrogen, CI-4 alkyl or aryl;
and R6, R7 and R8 which may be same or different are C1-4 alkyl, optionally substituted phenyl or a carrier in which the compound of formula 1 is reacted with a Lewis acid followed by reaction with water forming a hydroxy compound of the general formula II
A method for preparing a compound of the general formula III
in which R1 is the non-hydroxy moiety of a hydroxy compound; and A is an acyl group;
A compound of the general formula IV
in which R1 is the non-hydroxy moiety of a hydroxy compound; and X is a residue of a Lewis acid;
A method according to claim 4 in which R1 is the non-hydroxy moiety of a hydroxy-containing amino acid forming part of a peptide, and one of R6, R7 and R8 is a carrier; and
A compound of the general formula la
wherein R1 is a carbohydrate moiety containing two or more sugar units or a derivative thereof.
一种用通式 I 的受保护羟基化合物制备非受保护羟基化合物的方法
其中 R,是受保护羟基化合物的非羟基;R2、R3、R4 和 R5(可以相同或不同)是氢、CI-4 烷基或芳基;以及 R6、R7 和 R8(可以相同或不同)是 C1-4 烷基、任选取代的苯基;
式 1 的化合物与路易斯酸反应,然后与水反应,形成通式 II 的羟基化合物。
制备通式 III 化合物的方法
其中 R1 为羟基化合物的非羟基;A 为酰基;
通式 IV 的化合物
其中 R1 是羟基化合物的非羟基;X 是路易斯酸的残基;
根据权利要求 4 的方法,其中 R1 是构成肽的一部分的含羟基氨基酸的非羟基分子, R6、R7 和 R8 中的一个是载体;以及
通式 la 的化合物
其中 R1 是含有两个或两个以上糖单位的碳水化合物分子或其衍生物。