公开(公告)号：KR1020070003463A

公开(公告)日：2007-01-05

申请号：KR1020050059458

申请日：2005-07-02

Applicant: 재단법인서울대학교산학협력재단

Inventor： 이윤식 ,  김용권 ,  쩡춘리우 ,  신동식 ,  이규택 ,  전봉현

IPC: C07H19/10

CPC classification number: Y02P20/55 ,  C07K5/04

Abstract: Peptide nucleic acid(PNA) monomers having a photolabile protecting group are provided to improve preparation speed and economical efficiency of PNA through photolithograph method. The peptide nucleic acid monomers represented by the formulas(I) to (IV) are provided, wherein P is the photolabile protecting group; An is 4-methoxybenzoyl group; iBu is isobutyryl group; and the photolabile protecting group is selected from 2-nitrobenzyl derivative, 2-methyl-2-(2-nitrophenyl)propyloxycarbonyl derivative, benzoin derivative and ortho-nitrobenzyloxy derivative or further includes the compound represented by the formula(V). A method for preparing the peptide nucleic acids represented by the formula(XV) comprises the steps of: (i) reacting the compound represented by the formula(XIII) with the photolabile protecting group so as to prepare the compound represented by the formula(XIV); and (ii) independently reacting the compound represented by the formula(XIV) with 1-(carboxymethyl)-4-N-(4-methoxybenzoyl)cytosine, 9-(carboxymethyl)-2-N-(isobutyryl) guanine, 1-N-carboxymethylthymine and 9-(carboxymethyl)-6-N-(4-methoxybenzoyl)adenine.

Abstract translation: 提供具有光不稳定保护基的肽核酸（PNA）单体，通过光刻法提高PNA的制备速度和经济性。 提供由式（I）至（IV）表示的肽核酸单体，其中P是光不稳定保护基; An是4-甲氧基苯甲酰基; iBu是异丁酰基; 并且光不稳定保护基选自2-硝基苄基衍生物，2-甲基-2-（2-硝基苯基）丙氧基羰基衍生物，苯偶姻衍生物和邻硝基苄氧基衍生物，或还包括由式（V）表示的化合物。 制备由式（ⅩⅤ）表示的肽核酸的方法包括以下步骤：（ⅰ）使由式（ⅩⅢ）代表的化合物与光不稳定保护基反应，以制备由式（ⅩⅣ）表示的化合物 ）; 和（ii）使式（XIV）表示的化合物与1-（羧甲基）-4-N-（4-甲氧基苯甲酰基）胞嘧啶，9-（羧甲基）-2-N-（异丁酰基）鸟嘌呤， N-羧甲基胸腺嘧啶和9-（羧甲基）-6-N-（4-甲氧基苯甲酰基）腺嘌呤。