公开(公告)号：KR1019950032220A

公开(公告)日：1995-12-20

申请号：KR1019950012400

申请日：1995-05-18

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  김성훈 ,  남길수 ,  김하영 ,  손현주 ,  장은숙

IPC: C07D501/46

Abstract: 본 발명은 그람 음성균 및 그람 양성균에 대해 폭넓은 항균력을 나타내며 여러 내성균에 대해서도 강한 항균력을 나타내는 일반식(I)로 표시되는 새로운 세팔로스포린 화합물, 이의 수화물, 이의 약리학적으로 허용가능한 염, 이의 제조방법 및 이의 제조에 사용되는 중간체 화합물에 관한것이다.

상기 일반식(I)에서 A, R
1 및 R
2 는 발명의 상세한 설명에서 정의한 바와 같다.

公开(公告)号：KR1020070119422A

公开(公告)日：2007-12-20

申请号：KR1020060054040

申请日：2006-06-15

Applicant: 한국과학기술연구원 ,  이연제약주식회사

Inventor： 남길수 ,  김중협 ,  최경일 ,  장은숙 ,  이광호 ,  최용현 ,  신선호

IPC: C07H19/00 ,  C07H19/01

CPC classification number: C07H3/08 ,  C07H1/00

Abstract: A method for preparing a novel D-erythro-2-deoxy-2,2-difluoro-1-oxoribose compound is provided to synthesize the compound with high purity and high yield selectively, which is able to be used as an intermediate for preparing beta-2,2-difluoro nucleoside. A D-erythro-2-deoxy-2,2-difluoro-1-oxoribose compound is represented by the formula(1), wherein R1 is piperonyloyl, 2,3-dimethoxybenzoyl or 2,4-dimethoxybenzoyl; and R2 is benzoyl, biphenylcarbonyl, naphthoyl, benzyloxycarbonyl, para-methoxy benzyloxycarbonyl, or para-nitrobenzyloxycarbonyl substituted by a substituent selected from the group consisting of acetyl, monochloroacetyl, dichloroacetyl, pivaloyl, nitro, methyl, trifluoromethyl, chloro, fluoro, hydroxy and methoxy. A method for preparing the compound of the formula(1) comprises the steps of: reacting a compound represented by the formula(4) with piperonyloyl, 2,3-dimethoxybenzoyl or 2,4-dimethoxybenzoyl compound to prepare a compound represented by the formula(3); reacting the compound of the formula(3) with an acid to prepare a compound represented by the formula(2); and protecting 5-hydroxy of the compound of the formula(2). In the formulae(2) to (4), R is the same as defined above.

Abstract translation: 提供了一种制备新型D-赤式-2-脱氧-2,2-二氟-1-氧代核糖化合物的方法，可以选择性地合成具有高纯度和高产率的化合物，其能够用作制备β的中间体 -2,2-二氟核苷。 D-赤式-2-脱氧-2,2-二氟-1-氧代核糖化合物由式（1）表示，其中R 1是哌嗪基，2,3-二甲氧基苯甲酰基或2,4-二甲氧基苯甲酰基; R2是由选自乙酰基，一氯乙酰基，二氯乙酰基，新戊酰基，硝基，甲基，三氟甲基，氯，氟，羟基的取代基取代的苯甲酰基，联苯基羰基，萘甲酰基，苄氧基羰基，对甲氧基苄氧基羰基或对硝基苄氧基羰基。 甲氧基。 制备式（1）化合物的方法包括以下步骤：使式（4）表示的化合物与哌嗪基，2,3-二甲氧基苯甲酰或2,4-二甲氧基苯甲酰化合物反应，制备式 （3）; 使式（3）的化合物与酸反应以制备由式（2）表示的化合物; 并保护式（2）化合物的5-羟基。 式（2）〜（4）中，R与上述相同。