公开(公告)号：KR1020080075832A

公开(公告)日：2008-08-19

申请号：KR1020087002688

申请日：2006-03-24

Applicant: 포항공과대학교 산학협력단

Inventor： 김기문 ,  박경민 ,  고영호 ,  셀바팔람나라야난 ,  나가라잔에루마이파티알.

IPC: C07D487/04

CPC classification number: C07D487/04 ,  B01J20/286 ,  C07D305/14

Abstract: A stationary phase and column by using cucurbituril bonded silica gel are provided to separate high purity of taxane from low purity of taxane extract and reduce the costs for purification of taxane, so that high purity of taxane and paclitaxel isolated therefrom are useful for treating cancer. A stationary phase contains cucurbituril represented by the formula(1) or formula(2), in which R1 and R2 are each independently hydrogen, hydroxyl group, C1-C30 alkyloxy group, C1-C30 alkynyloxy group, C2-C30 carbonylalkyloxy group, C1-C30 thioalkyloxy group, C1-C30 alkylthioloxy group, C1-C30 hydroxyalkyloxy group, C1-C30 alkylsiloxy group, C1-C30 aminoalkyloxy group, C1-C30 aminoalkylthioalkyloxy group, C5-C30 cycloalkyloxy group, C2-C30 heterocycloalkyloxy group, C6-C30 aryloxy group, C6-C20 arylalkyloxy group, C4-C30 heteroaryloxy group, C4-C30 heteroarylalkyloxy group, C1-C30 alkylthio group, C1-C30 alkenylthio group, C1-C30alkynylthio group, C2-C30 carbonylalkylthio group, C1-C30 thioalkylthio group, C1-C30 hydroxyalkylthio group, C1-C30 alkylsilylthio group, C1-C30 aminoalkylthio group, C1-C30 aminoalkylthiolalkylthio group, C5-C30 cycloalkylthio group, C2-C30 heterocycloalkylthio group, C6-C30 arylthio group, C6-C20 arylalkylthio group, C4-C30heteroarylthio group, C4-C30 heteroarylalkylthio group, C1-C30 alkylamine group, C1-C30 alkenylamine group, C1-C30 alkynylamine group, C2-C30 carbonylalkylamine group, C1-C30 thioalkylamine group, C1-C30 hydroxyalkylamine group, C1-C30 alkylsilylamine group, C1-C30 trialkyloxysilyl alkyl-carbamate group, C1-C30 trialkyloxysilyl alkyl-thiocarbamate group, C1-C30 trialkyloxysilyl alkyloxy group, C1-C30 trialkyloxysilyl alkyl-carbonyloxy group, C1-C30 trialkyloxysilyl heteroalkyl-alkyloxy group, C1-C30 aminoalkylamine group, C1-C30 aminoalkylthioalkylamine group, C5-C30 cycloalkylamine group, C2-C30 heterocycloalkylamine group, C6-C30 arylamine group, C6-C20 arylalkylamine group, C4-C30 heteroarylamine, C4-C30 heteroarylamine group, C1-C30 alkylazide group, C1-C30 arylazide group, C1-C30 alkylcarboxylazide group or C1-C30 arylcarboxylazide group; X is O, S or NH; and n is an integer from 4 to 20, which is covalently bonded to silica gel represented by the formula(3), in which R2 is C2-C10 alkylthiol group, C2-C10 alkylamine group, C2-C10 epoxyalkyloxyalkyl group, C2-C10 isocyanatoalkyl group, C2-C10 halogenated alkyl group or hydroxyl group.

Abstract translation: 提供了使用葫芦巴键合硅胶的固定相和柱，以从紫杉烷提取物的低纯度中分离出高纯度的紫杉烷，降低了紫杉烷的纯化成本，从而分离出紫杉烷和紫杉醇的高纯度可用于治疗癌症。 固定相含有由式（1）或式（2）表示的葫芦巴脲，其中R 1和R 2各自独立地为氢，羟基，C 1 -C 30烷氧基，C 1 -C 30炔氧基，C 2 -C 30羰基烷氧基，C 1 -C30硫代烷氧基，C1-C30烷硫基氧基，C1-C30羟基烷氧基，C1-C30烷基甲硅烷氧基，C1-C30氨基烷氧基，C1-C30氨基烷硫基烷氧基，C5-C30环烷氧基，C2-C30杂环烷氧基，C6-C30 芳氧基，C 6〜C 20芳烷氧基，C 4〜C 30杂芳氧基，C 4〜C 30杂芳基烷氧基，C 1 -C 30烷硫基，C 1 -C 30烯硫基，C 1 -C 30炔硫基，C 2〜C 30羰基烷硫基，C 1 -C 30硫代烷硫基， C1-C30羟烷基硫基，C1-C30烷基甲硫基，C1-C30氨基烷硫基，C1-C30氨基烷硫基烷硫基，C5-C30环烷基硫基，C2-C30杂环烷硫基，C6-C30芳硫基，C6-C20芳烷硫基， C30杂芳基硫基，C4-C30杂 芳基烷硫基，C1-C30烷基胺基，C1-C30链烯基胺基，C1-C30炔基胺基，C2-C30羰基烷基胺基，C1-C30硫代烷基胺基，C1-C30羟烷基胺基，C1-C30烷基甲硅烷基胺基，C1-C30三烷基甲硅烷基烷基 氨基甲酸酯基，C1-C30三烷氧基甲硅烷基烷基 - 硫代氨基甲酸酯基，C1-C30三烷氧基甲硅烷基烷氧基，C1-C30三烷氧基甲硅烷基烷基 - 羰基氧基，C1-C30三烷基甲硅烷基杂烷基 - 烷氧基，C1-C30氨基烷基胺基，C1-C30氨基烷硫基烷基胺基， C 5 -C 30环烷基胺基，C 2 -C 30杂环烷基胺基，C 6 -C 30芳基胺基，C 6 -C 20芳烷基胺基，C 4 -C 30杂芳基胺，C 4 -C 30杂芳基胺基，C 1 -C 30烷基叠氮基，C 1 -C 30芳基叠氮基，C 1 -C 30 烷基羧基叠氮基或C 1 -C 30芳基羧基叠氮基; X是O，S或NH; 和n为4〜20的整数，与式（3）表示的硅胶共价键合，其中R2为C2-C10烷基硫醇基，C2-C10烷基胺基，C2-C10环氧烷氧基烷基，C2-C10 异氰酸根合烷基，C 2 -C 10卤代烷基或羟基。

公开(公告)号：KR100948143B1

公开(公告)日：2010-03-18

申请号：KR1020087002688

申请日：2006-03-24

Applicant: 포항공과대학교 산학협력단

Inventor： 김기문 ,  박경민 ,  고영호 ,  셀바팔람나라야난 ,  나가라잔에루마이파티알.

IPC: C07D487/04

CPC classification number: C07D487/04 ,  B01J20/286 ,  C07D305/14

Abstract: 쿠커비투릴이 결합된 실리카겔을 이용한 정지상 및 컬럼, 그리고 상기 컬럼을 이용한 탁산의 분리 방법이 개시된다. 개시된 탁산의 분리방법은 (a) 하기 화학식 1 또는 2로 표시되는 쿠커비투릴과 하기 화학식 3의 변형된 실리카겔이 공유결합된 물질을 포함하는 정지상을 충진하여 탁산 분리용 컬럼을 준비하는 단계; (b) 탁산 분말을 소정의 용매에 녹여 용액을 제조하는 단계; (c) 단계 (b)에서 얻어진 용액을 단계 (a)에서 얻어진 컬럼에 적용하는 단계; (d) 이동상 용매를 상기 컬럼에 제공하여 컬럼으로부터 탁산 추출물을 추출하는 단계; 및 (e) 단계 (d)에서 얻어진 탁산 추출물로부터 탁산을 정제하는 단계;를 포함한다.
따라서, 개시된 탁산의 분리방법은 저순도의 원료 탁산 추출물에서도 고순도의 탁산을 분리해 낼 수 있다.