| 摘要 |
A novel method of covalently coupling polysaccharides to other biopolymers is provided, using an amino-thiol linker represented by formula (1): H2N-[(CH2)m- CHR1-CR2R3-A]q-CHR4-(CHR5)p-CHR6-S-R7 wherein A is a direct bond or a group having the formula -{Z-(CH2)m-CHR1-CHR2R3}nZ-, m is an integer from 0 to 5; n is an integer from 0 to 3; p is an integer from 0 to 2; q is the integer 0 or 1; R1 is hydrogen or C1-C6 alkyl, optionally substituted by amino, hydroxyl, carboxyl, C1-C4 alkoxycarbonyl, carbamoyl, mono- or di(C1-C4alkyl)carbamoyl or N-(.alpha.-carboxyalkyl)carbamoyl, or, if m <> 0, R1 is hydroxyl, amino or peptidylamino; R2 and R3 are independently hydrogen or C1-C4 alkyl, or together form an oxo group; R4 is hydrogen, C1-C4 alkyl, carboxyl, C1-C4 alkoxycarbonyl, carbamoyl, mono- or di(C1-C4 alkyl)carbamoyl or N-(.alpha.- carboxyalkyl)carbamoyl; R5 is hydrogen, methyl, hydroxy or C1-C7 acyloxy; R6 is hydrogen or methyl; R7 is hydrogen or a thiol-protecting group or a group having the formula -S-CHR6-(CHR5)p-CHR4-[A-CR2R3-CHR1-(CH2)m]q-NH2; and z is imino, methylimino, oxygen or sulphur.
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