专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明公开

KR20070080108A METHOD FOR RESOLVING ENANTIOMER FROM RACEMATE WITH CHIRAL CARBON AT THE alpha;POSITION 审中-公开
标题翻译：用于在α位置上用正丁基碳氢化合物分解成熟剂的方法
公开(公告)号：KR20070080108A
公开(公告)日：2007-08-09
申请号：KR20060011226
申请日：2006-02-06
申请人： CHONG KUN DANG PHARM CORP
发明人： AHN SOON KIL , LEE HONG WOO , LIM IN TAEK , IM DAI SIG , AHN JOONG BOK , LEE JUNG HWA
IPC分类号： C07D411/04
CPC分类号： C07D411/04 , C07D217/14 , C07D217/16
摘要： A method for isolating enantiomer from a racemic derivative having a chiral carbon at alpha position of nitrogen is provided to simply isolate the enantiomer with improved optical purity by forming a salt of an amino acid having the optical activity with the racemic derivative without using a catalyst or an enzyme. The method comprises the steps of: (a) dissolving an amino acid which has the optical activity with a racemic derivative having a chiral carbon at alpha position of a nitrogen represented by the formula(1) or (2) in a protonic organic solvent; (b) adding a non-protonic organic solvent to the reaction solution obtained from the step(a) to crystallize an enantiomer salt; and (c) obtaining a free amine from the crystallized enantiomer salt. In the formulae(1) and (2), each X1, X2, X3 and X4 is independently H, halogen, C1-4 alkyl, hydroxy or C1-4 alkoxy, Y is phenyl which is substituted by at least one substituent selected from the group consisting of halogen, C1-4 alkyl, hydroxy and C1-4 alkoxy or a naphthyl which is substituted by at least one substituent selected from the group consisting of halogen, C1-4 alkyl, hydroxy and C1-4 alkoxy, and n is an integer from 1 to 3.
摘要翻译：提供了从在氮的α位具有手性碳的外消旋衍生物分离对映异构体的方法，通过在不使用催化剂的情况下通过形成具有光学活性的氨基酸的盐与外消旋衍生物的盐来简单地分离具有改善的光学纯度的对映异构体一种酶该方法包括以下步骤：（a）将具有光学活性的氨基酸与式（1）或（2）表示的氮的α位具有手性碳的外消旋衍生物溶解在质子有机溶剂中; （b）向由步骤（a）获得的反应溶液中加入非质子有机溶剂使结晶对映体盐; 和（c）从结晶的对映异构体盐获得游离胺。在式（1）和（2）中，每个X 1，X 2，X 3和X 4独立地是H，卤素，C 1-4烷基，羟基或C 1-4烷氧基，Y是被至少一个选自由卤素，C 1-4烷基，羟基和C 1-4烷氧基取代的基团或被至少一个选自卤素，C 1-4烷基，羟基和C 1-4烷氧基的取代基取代的萘基，n 是1到3的整数。

2. 发明公开

KR20100131245A New preparation of rosuvastatin, the useful intermediates thereof and preparation of the same 无效
标题翻译：罗维沙星的新制剂，其有用的中间体及其制备
公开(公告)号：KR20100131245A
公开(公告)日：2010-12-15
申请号：KR20090050044
申请日：2009-06-05
申请人： CHONG KUN DANG PHARM CORP
发明人： LEE HONG WOO , PARK DAE JONG , YOO CHOONG LEOL , NAM DONG HYUK , RYU HO HYUNG , KIM DONG JIN
IPC分类号： C07D239/42 , A61K31/505 , A61P3/06
CPC分类号： C07D239/42 , C07C67/31 , C07C67/343 , C07C69/675 , C07C69/716 , C07D317/30 , C07D405/06 , C07D405/12 , C07D417/12
摘要： PURPOSE: A method for preparing a novel intermediate compound used for rosuvastatin is provided to obtain rosuvastatin hemicalcium salt. CONSTITUTION: A compound of chemical formula 3 is prepared by reacting a compound of chemical formula 2 with a compound of chemical formula 1 under the presence of base. The base is lithium(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide or potassium(trimethylsilyl)amide. A method for preparing a compound of chemical formula 4 comprises: a step of removing dihydroxy group from 2-methyl-1-phenylpropane-2-yl 2-((4R,6S)-6-((E)-2-(4- (4-fluorophenyl)-6-isopropyl-2-(N-methyl methyl sulfonamido)pyrimidine-5-yl)vinyl)-2,2-dimethyl-1,3-dioxane-4-yl)acetate; a step of decomposing alpha,alpha-dimethylphenylethyl ester group of the product under the presence of base; a step of neutralizing under the presence of acid to obtain (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid; and a step of reacting the resultant with alkyl amine and pharmaceutically acceptable salt-producing reactant to obtain a compound of chemical formula 4.
摘要翻译：目的：提供一种制备用于瑞舒伐他汀的新型中间体化合物的方法，以获得瑞舒伐他汀半钙盐。构成：化学式3的化合物通过化学式2的化合物与化学式1的化合物在碱的存在下反应来制备。碱为锂（三甲基甲硅烷基）酰胺，双（三甲基甲硅烷基）氨基钠或（三甲基甲硅烷基）氨基钾。制备化学式4的化合物的方法包括：从2-甲基-1-苯基丙烷-2-基2 - （（4R，6S）-6 - （（E）-2-（4 - （4-氟苯基）-6-异丙基-2-（N-甲基甲基亚磺酰氨基）嘧啶-5-基）乙烯基）-2,2-二甲基-1,3-二恶烷-4-基）乙酸乙酯; 在碱存在下分解产物中的α，α-二甲基苯乙基酯基的步骤; 得到（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基]（3R，5S）的步骤在酸存在下中和， -3,5-二羟基庚-6-烯酸; 以及使所得物与烷基胺和药学上可接受的产生盐的反应物反应以获得化学式4的化合物的步骤。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式