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公开(公告)号:KR101044880B1
公开(公告)日:2011-06-28
申请号:KR1020080055111
申请日:2008-06-12
Applicant: 일양약품주식회사
IPC: C07D403/06 , C07D403/04 , A61K31/44 , A61K31/335
CPC classification number: C07D403/04
Abstract: 본 발명은 하기 화학식 3의 화합물의 신규한 제조방법에 관한 것으로, 더욱 상세하게는, 본 발명은 하기 화학식 1의 화합물과 하기 화학식 2의 화합물을 반응시켜 항궤양제 화합물의 중간체인 하기 화학식 3의 화합물을 제조하는 방법에 관한 것이다:
[화학식 1]
[화학식 2]
[화학식 3]
상기 식에서, R은 C
1
-6 알킬이다.-
2.
公开(公告)号:KR1020050080965A
公开(公告)日:2005-08-18
申请号:KR1020040009161
申请日:2004-02-12
Applicant: 일양약품주식회사
IPC: C07D487/04
Abstract: 본 발명은 하기 화학식1로 표시되는 새로운 피라졸로피리미디논 유도체와 이의 제조방법에 관한 것으로,
더욱 상세하게는, 본 발명은 하기 화학식1의 신규한 피라졸로피리미디논 유도체를 이용하여 특히 cGMP-대사 포스포디에스테라제의 저해제로서 그의 약제학적 용도를 제공함으로써 기존의 약물보다 체내흡수가 빠르고 생체내 독성이 낮은 약물을 제공하는 특징이 있다.
[화학식1]
상기 화학식 1에서 R
1 , R
2 , R
3 , R
4 및 R
5 는 각각 발명의 상세한 설명에서 정의하는 바와 같다.-
公开(公告)号:KR101144600B1
公开(公告)日:2012-05-16
申请号:KR1020090121209
申请日:2009-12-08
Applicant: 일양약품주식회사
IPC: C07D401/14 , C07D403/14 , C07D235/24
CPC classification number: C07D401/14
Abstract: Disclosed are novel processes for preparing crystalline forms A and B of ilaprazole of formula 1 and the conversion of these crystalline forms. The novel processes include a process of preparing the crystalline form A of high purity by preparing an inorganic salt of ilaprazole or a hydrate thereof and then neutralizing the prepared inorganic salt of ilaprazole or the hydrate thereof with an acid in an organic solvent (single solvent or mixed solvent) a process of preparing the crystalline form B of high purity by removing impurities from ilaprazole using an organic solvent (single solvent or mixed solvent); and a process of conversion from the crystalline A into the crystalline form B or from the crystalline form B into the crystalline form A.
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公开(公告)号:KR1020090129046A
公开(公告)日:2009-12-16
申请号:KR1020080055111
申请日:2008-06-12
Applicant: 일양약품주식회사
IPC: C07D403/06 , C07D403/04 , A61K31/44 , A61K31/335
CPC classification number: C07D403/04
Abstract: PURPOSE: A method for preparing an intermediate which is useful in synthesis of antiulcerant compound is provided to yield the antiulcerant compound of high purity and improve the yield. CONSTITUTION: A 5-(1H-pyrrole-1-yl)-mercaptobenzimidazol of chemical formula 3 is obtained by reacting a compound of chemical formula 1 and 2-mercapto-5-aminobenzimidazole of chemical formula 2. In the chemical formulas 1, 2, and 3, R is alkyl of C1-6. A method for preparing a compound of chemical formula 3 comprises: a step of cyclizing 2-mercapto-5-aminobenzimidazole of chemical formula 2 with a compound of chemical formula 1 under the presence of acid and reaction solvent; a step of adding alkaline solution and neutralizing to separate organic layer; and a step of drying and concentrating the organic layer to crystallize the compound of chemical formula 3.
Abstract translation: 目的:提供一种可用于合成抗溃疡化合物的中间体的方法,以产生高纯度的抗溃疡化合物并提高产率。 构成:化学式3的5-(1H-吡咯-1-基) - 巯基苯并咪唑通过化学式2的化合物与2-巯基-5-氨基苯并咪唑的化学式2反应得到。在化学式1,2 ,和3,R是C1-6的烷基。 制备化学式3的化合物的方法包括:在酸和反应溶剂的存在下,用化学式1的化合物环化化学式2的2-巯基-5-氨基苯并咪唑的步骤; 添加碱性溶液并中和分离有机层的步骤; 以及干燥并浓缩有机层以使化学式3的化合物结晶的步骤。
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公开(公告)号:KR1020110064545A
公开(公告)日:2011-06-15
申请号:KR1020090121209
申请日:2009-12-08
Applicant: 일양약품주식회사
IPC: C07D401/14 , C07D403/14 , C07D235/24
CPC classification number: C07D401/14
Abstract: PURPOSE: A novel method for preparing ilaprazole crystalline form A and B is provided to ensure industrially simple process and to massive production. CONSTITUTION: A method for preparing ilaprazole crystalline A comprises: a step of preparing inorganic salt or inorganic salt hydrate from ilaprazole under the presence of inorganic base and reaction solvent; and a step of neutralizing the inorganic salt or inorganic salt hydrate to prepare ilaprazole crystalline form A. The inorganic base or inorganic salt is lithium, titanium, barium, zinc, sodium, potassium, calcium, magnesium, or strontium.
Abstract translation: 目的:提供一种制备阿拉唑结晶形式A和B的新方法,以确保工业上简单的工艺和大规模生产。 构成:制备伊拉唑结晶A的方法包括:在无机碱和反应溶剂的存在下从伊拉唑制备无机盐或无机盐水合物的步骤; 和无机盐或无机盐水合物中和以制备伊拉帕唑结晶形式A的步骤。无机碱或无机盐是锂,钛,钡,锌,钠,钾,钙,镁或锶。
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