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1. 发明授权

KR800001086B1 METHOD FOR THE PREPARATION OF DEOXYAMINOGLYCOSIDE ANTIBIOTICS 失效
公开(公告)号：KR800001086B1
公开(公告)日：1980-10-06
申请号：KR740000125
申请日：1974-01-01
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： HIRAGA KENTARO , YOSHIOKA KOUICHI , OKUTANI TETSUYA
IPC分类号： C07H3/08 , C07H5/06 , C07H15/22
摘要： Halogenodeoxyaminoglycoside antibiotic, intermediate of deoxyaninoglycoside antibiotic and inhibitor of bacteria resisting to known aminoglycoside antibiotic, is prepd. Kanamycin, neomycin, neomycin, paromomycin and ribostamycin derivs., which are phosphorylated at 3`-hydroxy1 group, are sillylated or acylated to protect functional group and chlorinated by trialkylsillylhalide, triarylsillylhalide etc. at 80-150≦̸C. Phosphines, halogenated metal, AlCl3, BF3or Ti(Cl3) can be added to the reactant.

2. 发明公开

KR1020070092309A 탄소-감소된 알도오스 화합물의 제조 방법 无效
标题翻译：生产碳化二醛化合物的方法
公开(公告)号：KR1020070092309A
公开(公告)日：2007-09-12
申请号：KR1020077017165
申请日：2005-12-28
申请人： 아스비오파마 가부시키가이샤
发明人： 오키츠미츠히토 , 가메이가츠히데
IPC分类号： C07H3/02 , C07H3/08
CPC分类号： C07C319/14 , C07C315/02 , C07H3/02 , C07H3/08 , C07C317/18 , C07C323/12
摘要： A process by which 5-deoxy-L-arabinose, which is important as a material for the production of saproterin, a useful therapeutic agent for atypical hyperphenylalaninemia, can be industrially and efficiently produced even with a simple production apparatus. The process for 5-deoxy-L-arabinose production is characterized by reacting L-rhamnose with a C11-16 linear alkyl mercaptan compound in the presence of an acid catalyst to yield an L-rhamnose di(alkyl mercaptal), subsequently subjecting the resultant compound to an oxidation reaction to obtain a sulfonyl derivative, and then subjecting it to a carbon diminution reaction. This production process is applicable to a process for the production of a compound formed by removing one carbon atom from another aldol compound. Thus, the process is one for producing carbon-diminished compounds of general aldoses.
摘要翻译：作为用于生产非特异性高苯丙氨酸血症的有用的治疗剂，对于非典型性高的苯丙氨酸血症来说，重要的5-脱氧-L-阿拉伯糖是工业上有效生产的方法。 5-脱氧-L-阿拉伯糖生产方法的特征在于L-鼠李糖与C11-16直链烷基硫醇化合物在酸催化剂存在下反应，得到L-鼠李糖二（烷基巯基），随后使所得的化合物进行氧化反应得到磺酰基衍生物，然后进行碳减少反应。该制造方法适用于通过从另一种醛醇化合物除去一个碳原子而形成的化合物的制造方法。因此，该方法是用于生产通常醛糖的减碳化合物的方法。

3. 发明公开

KR1020030038043A 2-데옥시-Ｌ-리보스의 제조방법 有权
标题翻译：制备2-脱氧-L-赖氨酸的方法
公开(公告)号：KR1020030038043A
公开(公告)日：2003-05-16
申请号：KR1020010069451
申请日：2001-11-08
申请人： 주식회사 삼탄인터내셔널
发明人： 강재성 , 박영원 , 윤미홍 , 유기원 , 장순기 , 이지영 , 김민규 , 이영재
IPC分类号： C07H3/08
摘要： PURPOSE: A process for preparing 2-deoxy-L-ribose is provided, thereby simply and cheaply preparing 2-deoxy-L-ribose in higher yield without side-products. CONSTITUTION: A process for preparing 2-deoxy-L-ribose represented by formula (IV) comprises the steps of: (a) reacting a compound of formula (II) with ozone to prepare a compound of formula (III); and (b) deprotection of the compound of formula (III) to prepare a compound of formula (IV), wherein R1 and R2 are independently H, C1-15 alkyl, C3-15 cycloalkyl or phenyl; and R3 and R4 are independently H, C1-15 alkyl, C3-C15 cycloalkyl or phenyl, and R3 and R4 may form 5-, 6-, 7- or 8-membered ring and one or more substituents.
摘要翻译：目的：提供2-脱氧-L-核糖的制备方法，从而简单且廉价地制备2-脱氧-L-核糖，而没有副产物。构成：由式（IV）表示的制备2-脱氧-L-核糖的方法包括以下步骤：（a）使式（II）化合物与臭氧反应制备式（III）化合物; 和（b）式（III）化合物的脱保护以制备式（IV）化合物，其中R 1和R 2独立地为H，C 1-15烷基，C 3-15环烷基或苯基; 并且R 3和R 4独立地为H，C 1-15烷基，C 3 -C 15环烷基或苯基，并且R 3和R 4可以形成5-，6-，7-或8-元环和一个或多个取代基。

4. 发明授权

KR1019940004065B1 고순도 아카르보스의 제조방법 失效
标题翻译：非常纯粹的反感
公开(公告)号：KR1019940004065B1
公开(公告)日：1994-05-11
申请号：KR1019860010629
申请日：1986-12-12
申请人： 바이엘 악티엔게젤샤프트
发明人： 에리히라우엔부쉬
IPC分类号： C07H3/08
CPC分类号： C07H15/22
摘要： 내용 없음.

5. 发明公开

KR870006074A 고순도 아카르보스 및 그의 제조방법 失效
公开(公告)号：KR870006074A
公开(公告)日：1987-07-09
申请号：KR860010629
申请日：1986-12-12
IPC分类号： C07H15/203 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P3/08 , A61P3/10 , C07H3/08 , C07H15/22
摘要： 내용없음

6. 发明公开

KR1020080086629A 광학적으로 순수한 옥소라이보스유도체의 제조방법 有权
标题翻译：制备光学纯OXORIBOSE衍生物的方法
公开(公告)号：KR1020080086629A
公开(公告)日：2008-09-26
申请号：KR1020070028526
申请日：2007-03-23
申请人： 이니스트에스티 주식회사
发明人： 오천림 , 박수진 , 김영덕
IPC分类号： C07H3/08
摘要： A process for preparing optically pure oxoribose derivatives is provided to improve economical efficiency of preparation, reaction yield, preparation simplicity and purity of oxoribose derivatives by using a novel intermediate, so that enantiomers of oxoribose derivatives are selectively prepared. A process for preparing optically pure oxoribose derivatives represented by the formula(I-D) or (I-L) comprises the steps of: (1) reacting ethyl 3-hydroxy propionic acid ester compounds represented by the formula(V) with optically pure amine-based compounds to prepare optically pure 3S- or 3R-hydroxy propane amide derivatives represented by the formula(II-R) and the formula(II-S); (2) protecting the compounds represented by the formula(II-R) and the formula(II-S) with a hydroxyl group to prepare compounds represented by the formula(IV-R) and the formula(IV-S); (3) reacting the compounds represented by the formula(IV-R) and the formula(IV-S) with acid to prepare 5-hydroxy-1-oxo-ribose compounds having erythro or threo structure, represented by the formula(III-D) and the formula(III-L); and (4) protecting the compounds represented by the formula(III-D) and the formula(III-L) with 5-hydroxyl group, wherein R and R1 are each independently benzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 4-cyanobenzoyl, 3-cyanobenzoyl, 4-propylbenzoyl, 2-ethoxybenzoyl, 4-t-butylbenzoyl, [1,1'-biphenyl]-4-carbonyl, 1-naphtoyl or 2-naphtoyl group; R2 and R3 are each independently C1-C3 alkyl; R4 is methyl or ethyl group; and R5 is hydrogen, methyl, methoxy or Cl.
摘要翻译：提供了一种制备光学纯的氧代核糖衍生物的方法，以通过使用新的中间体来提高制备的经济效率，反应产率，氧代核糖衍生物的制备简单性和纯度，从而选择性地制备氧代核糖衍生物的对映异构体。制备由式（ID）或（IL）表示的光学纯的氧代核糖衍生物的方法包括以下步骤：（1）使由式（V）表示的3-羟基丙酸酯化合物与光学上纯的胺类化合物制备由式（II-R）和式（II-S）表示的光学纯的3S-或3R-羟基丙烷酰胺衍生物。（2）用羟基保护由式（II-R）和式（II-S）表示的化合物以制备由式（IV-R）和式（IV-S）表示的化合物。（3）使由式（IV-R）和式（IV-S）表示的化合物与酸反应，以制备具有式（III-（R））表示的具有赤式或苏式结构的5-羟基-1-氧代 - D）和式（III-L）; 和（4）用5-羟基保护由式（III-D）和式（III-L）表示的化合物，其中R和R 1各自独立地是苯甲酰基，4-甲基苯甲酰基，3-甲基苯甲酰基，4-氰基苯甲酰基，3-氰基苯甲酰基，4-丙基苯甲酰基，2-乙氧基苯甲酰基，4-叔丁基苯甲酰基，[1,1'-联苯] -4-羰基，1-萘甲酰基或2-萘甲酰基; R2和R3各自独立地为C1-C3烷基; R4是甲基或乙基; R5是氢，甲基，甲氧基或C1。

7. 发明授权

KR100699099B1 1-α-할로-2,2-다이플루오로-2-데옥시-Ｄ-라이보퓨라노스유도체 및 이의 제조방법 有权
标题翻译： 1-α-HALO-2,2-二氟-2-脱氧-D-呋喃糖醛酸衍生物及其制备方法
公开(公告)号：KR100699099B1
公开(公告)日：2007-03-22
申请号：KR1020050041278
申请日：2005-05-17
申请人： 한미사이언스 주식회사
发明人： 이재헌 , 박가승 , 이문섭 , 김한경 , 방효정 , 장영길 , 이관순
IPC分类号： C07H3/08 , C07H3/02
CPC分类号： C07H3/08
摘要： 본 발명은 하기 화학식 1로 표시되는 1-α-할로-2,2-다이플루오로-2-데옥시-D-라이보퓨라노스 유도체 및 이의 제조방법에 관한 것으로, 본 발명의 1-α-할로-라이보퓨라노스 유도체는 고체 상태로 수득되어 젬시타빈(gemcitabine)의 제조를 위한 중간체로서 유용하게 사용될 수 있다.

상기 식에서,
R
1 은 벤조일 또는 이고,
R
2 는 이고,
R
3 은 시아노, 할로겐, 카보알콕시, 톨루엔, 니트로, C
1-2 알콕시, C
1-2 알킬 및 다이알킬 아미노로 이루어진 군으로부터 선택된 하나 이상의 기로 치환되거나 치환되지 않은 페닐이며,
X는 Cl, Br 또는 I이다.

8. 发明公开

KR1020060008056A Ｄ-에리트로-2,2-다이플루오로-2-데옥시-1-옥소라이보스화합물의 제조방법 失效
标题翻译： D-呋喃基-2,2-二氟-2-氧代-1-氧化物的制备方法
公开(公告)号：KR1020060008056A
公开(公告)日：2006-01-26
申请号：KR1020040057711
申请日：2004-07-23
申请人： 한미사이언스 주식회사
发明人： 이재헌 , 박가승 , 이문섭 , 김철경 , 이재철 , 장영길 , 이관순
IPC分类号： C07H3/08 , C07H3/02
CPC分类号： C07H3/08 , C07H3/02 , C07H1/00
摘要： 3R-carboxylate enantiomer derivative of formula (III) can be prepared easily and selectively by the method of the present invention, and a highly pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose derivative can be prepared efficiently from the compound of formula (III) as an intermediate.

9. 发明公开

KR1020000025033A 탄수화물 분해효소 저해 물질 및 그것의 제조방법 失效
标题翻译：碳硼酸盐抑制剂及其制备方法
公开(公告)号：KR1020000025033A
公开(公告)日：2000-05-06
申请号：KR1019980041908
申请日：1998-10-01
申请人： 박관화
发明人： 박관화 , 김묘정 , 김태집 , 이희섭 , 차현주 , 윤현근 , 김영완 , 이수복 , 김도만 , 오병하 , 김정완
IPC分类号： C07H3/08
摘要： PURPOSE: A carbohydrate lyase inhibitor and preparation method thereof using a degradable amylase is provided which can produce enzymatically isoacarbose capable of effectively controlling the carbohydrate lyase inhibitor without byproduct. CONSTITUTION: A carbohydrate lyase inhibitor is prepared by reacting acarbose with an acetous-degradable amylase in the presence of a sugar receptor such as glucose. The carbohydrate lyase inhibitor can produce enzymatically isoacarbose capable of effectively controlling the carbohydrate lyase inhibitor without byproduct. The acarbose as a representative compound which inhibits carbohydrate lyase is effective for effectively inhibiting alpha-glucosidase such that it is used widely in treating diabetes.
摘要翻译：目的：提供一种使用可降解淀粉酶的碳水化合物裂解酶抑制剂及其制备方法，其可以产生能够有效控制碳水化合物裂解酶抑制剂而不产生副产物的酶异丙糖。构成：在糖受体如葡萄糖存在下，通过使阿卡波糖与乙酰肝素可降解淀粉酶反应来制备碳水化合物裂解酶抑制剂。碳水化合物裂解酶抑制剂可以产生能够有效控制碳水化合物裂解酶抑制剂而不产生副产物的酶异丙糖。作为抑制碳水化合物裂解酶的代表性化合物的阿卡波糖对于有效抑制α-葡萄糖苷酶有效，因此其广泛用于治疗糖尿病。

10. 发明授权

KR100863463B1 광학적으로 순수한 옥소라이보스유도체의 제조방법 有权
标题翻译：制备光学纯的氧代核糖衍生物的方法
公开(公告)号：KR100863463B1
公开(公告)日：2008-10-16
申请号：KR1020070028526
申请日：2007-03-23
申请人： 이니스트에스티 주식회사
发明人： 오천림 , 박수진 , 김영덕
IPC分类号： C07H3/08
摘要： 본 발명은 광학 활성을 지닌 키랄 아민을 이용하여 하기 화학식 Ⅱ의 3-(2,2-다이알킬-1,3-다이옥소란-4-일)-2,2-다이플루오로-3-하이드록시)프로판아미드를 (R) 또는 (S) 형태로 광학적으로 순수하게 고체형태로 제조한 후 산에서 반응시키는 것을 포함하는, 하기 화학식 1의 에리트로 또는 트레오-2,2-다이플루오로-2-데옥시-1-옥소라이보스 화합물을 선택적으로 제조하는 방법에 관한 것이다.
[화학식 Ⅰ-D]

[화학식 Ⅰ-L]

[화학식 Ⅱ-R]

[화학식 Ⅱ-S]

상기 식에서, R과 R
1 은 보호기로서 각각 독립적으로 벤조일, 4-메틸벤조일, 3-메틸벤조일, 4-시아노벤조일, 3-시아노벤조일, 4-프로필벤조일, 2-에톡시벤조일, 4-t-부틸벤조일, [1,1'-바이페닐]-4-카보닐, 1-나프토일 또는 2-나프토일기이고, R
2 및 R
3 는 각각 독립적으로 C
1 내지 C
3 알킬이며 R
4 은 메틸 또는 에틸기, R
5 은 수소, 메틸, 메톡시 또는 Cl 이다.
옥소라이보스 화합물, 키랄아민, 젬시타빈

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