申请人:Institute Organicheskogo Sinteza
公开号:US04434095A1
公开(公告)日:1984-02-28
A novel substance, that is a cyclic analogue of a naturally-occurring phagocytosis-stimulant peptide - threonyl-cyclo-[-N.sup..epsilon. -lysyl-prolyl-arginyl-] of the formula: ##STR1## A method for preparing threonyl-cyclo-[-N.sup..epsilon. -lysyl-prolyl-arginyl-] by way of a step-wise building-up of the peptide chain from the C-terminal by means of activated ethers of benzyloxycarbonyl-proline, tert.butyloxycarbonyl- -N.sup..epsilon. -benzyl-oxycarbonyl-lysine and tert.butyloxycarbonyl-threonine, followed by cyclization of the resulting partly blocked tetrapeptide using Woodward reagent in an excess of dimethylformamide and isolation of the desired product.
一种新颖物质,是天然存在的噬菌作用刺激肽的环状类似物 - 赖氨酸-环-[-N.sup..epsilon. -赖氨酰-脯氨酰-精氨酰-]苏氨酸的公式如下:##STR1## 通过使用苯甲氧羰基-脯氨酰活性醚,tert.butyloxycarbonyl- -N.sup..epsilon. -苄基氧羰基-赖氨酸和tert.butyloxycarbonyl-苏氨酸,从C-末端逐步建立肽链的方法来制备赖氨酸-环-[-N.sup..epsilon. -赖氨酰-脯氨酰-精氨酰-]苏氨酸,随后使用过量的二甲基甲酰胺中的伍德沃德试剂将所得的部分阻塞四肽环化,并分离所需产品。