专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明授权

US4801735A Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US4801735A
公开(公告)日：1989-01-31
申请号：US801524
申请日：1985-11-25
申请人： Mark A. W. Finch , John R. Harris
发明人： Mark A. W. Finch , John R. Harris
IPC分类号： C07C43/23 , A61K31/047 , A61K31/05 , A61K31/11 , A61K31/12 , A61K31/135 , A61K31/15 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/23 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P11/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C27/00 , C07C39/11 , C07C39/19 , C07C45/00 , C07C47/27 , C07C47/277 , C07C47/565 , C07C47/575 , C07C49/825 , C07C49/835 , C07C49/84 , C07C51/00 , C07C59/48 , C07C59/52 , C07C59/64 , C07C67/00 , C07C69/732 , C07C69/734 , C07C213/00 , C07C215/50 , C07C215/78 , C07C231/00 , C07C231/12 , C07C235/34 , C07C235/46 , C07C239/00 , C07C241/00 , C07C251/24 , C07C251/32 , C07C251/86 , C07D295/145 , C07D295/16 , C07D295/18 , C07D295/185 , C07D295/22 , C07D295/30 , C07C69/76 , C07C65/01
CPC分类号： C07D295/185 , C07C251/72 , C07C47/27 , C07C47/277 , C07C47/565 , C07C47/575 , C07C49/835 , C07C49/84 , C07D295/145 , C07D295/30 , Y02P20/55
摘要： Compounds are described of the following formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, at least one of R.sup.1 and R.sup.2 being C.sub.1-12 alkyl or C.sub.2-12 alkenyl; X.sup.1 and X.sup.2 are each hydrogen or a protecting group; and Y is(a) --(CH.dbd.CH).sub.n Z in which n is 1, 2 or 3 and Z is --CHO, --CH.sub.2 OH, --COR.sup.3, --(CH.sub.2).sub.m --COR.sup.3 or --(CH.sub.2).sub.p CH.dbd.CH(CH.sub.2).sub.q --COR.sup.3 in which m is an integer of 1 to 12, p is an integer of 1 to 4, q is an integer of 1 to 10 and R.sup.3 is (i) --OH or (ii) --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl, or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a morpholino, pyrrolidinyl or piperidino ring,(b) --CH.dbd.NR.sup.6 in which R.sup.6 is (i) --OH, (ii) C.sub.1-12 alkyl optionally substituted by --OH, --COOH or --NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-4 alkyl, (iii) optionally substituted phenyl or (iv) --NR.sup.9 R.sup.10 in which R.sup.9 is hydrogen and R.sup.10 is optionally substituted phenyl or C.sub.1-4 alkyl CO--, or in which R.sup.9 and R.sup.10 together with the nitrogen atom to which they are attached form a morpholino, pyrrolidinyl or piperidino ring,(c) --CH.sub.2 NHR.sup.11 in which R.sup.11 is C.sub.1-12 alkyl optionally substituted with hydroxy or carboxy or optionally substituted phenyl, or(d) --CHOHR.sup.12 or ##STR2## in which R.sup.12 is hydrogen or C.sub.1-12 alkyl; and lactones, salts and esters thereof; provided that when one of R.sup.1 and R.sup.2 is hydrogen and the other is C.sub.1-12 alkyl, Y is --(CH.dbd.CH).sub.n Z, n is 1 and Z is --COOH only salts are included.The compounds have pharmaceutical activity.
摘要翻译：其中R 1和R 2各自为氢，C 1-12烷基或C 2-12烯基，R 1和R 2中的至少一个为C 1-12烷基或C 2-12链烯基; X1和X2各自为氢或保护基; 并且Y是（a） - （CH = CH）nZ，其中n是1,2或3，Z是-CHO，-CH 2 OH，-COR 3， - （CH 2）m -CON 3或 - （CH 2）p CH = CH CH 2）q-COR 3，其中m为1至12的整数，p为1至4的整数，q为1至10的整数，R 3为（i）-OH或（ii）-NR 4 R 5，其中R 4和 R5分别是氢，C1-4烷基或任选取代的苯基，或者R4和R5与它们所连接的氮原子一起形成吗啉代，吡咯烷基或哌啶子基环，（b）-CH = NR6，其中R6是（i ）-OH，（ii）任选被-OH，-COOH或-NR 7 R 8取代的C 1-12烷基，其中R 7和R 8各自为氢或C 1-4烷基，（iii）任选取代的苯基或（iv）-NR 9 R 10，其中R 9 是氢，R 10是任选取代的苯基或C 1-4烷基CO-，或者其中R 9和R 10与它们所连接的氮原子一起形成吗啉代，吡咯烷基或哌啶子基环，（c）-CH 2 NHR 11，其中R 11是任选被羟基或羧基或任选取代的苯基取代的C 1-12烷基，或（d）-CHOH R12或其中R12是氢或C1-12烷基; 及其内酯，其盐和酯; 条件是当R1和R2中的一个是氢而另一个是C 1-12烷基时，Y是 - （CH = CH）nZ，n是1，Z是-COOH，只包括盐。这些化合物具有药物活性。

42. 发明授权

US4608195A Preparing a tertiary hydroxyl carboxaldehyde containing perfume composition 失效
标题翻译：制备含羟基甲醛的香料组合物
公开(公告)号：US4608195A
公开(公告)日：1986-08-26
申请号：US768839
申请日：1985-08-23
申请人： Futoshi Fujioka , Richard M. Boden , William L. Schreiber
发明人： Futoshi Fujioka , Richard M. Boden , William L. Schreiber
IPC分类号： C07C45/49 , C07C47/27 , C07C47/36 , C11B9/00 , A61K7/46
CPC分类号： C11B9/0061 , C07C45/49 , C07C47/27 , C07C47/36
摘要： Described are tertiary hydroxyl carboxaldehydes defined according to the generic structure: ##STR1## wherein the lines ##STR2## represent covalent carbon-carbon bonds when m does not=0; and wherein the lines ##STR3## do not represent any bonds when m=0; wherein R represents hydrogen or methyl; wherein p and q each represents 0 or 1 with the proviso that p=1 when q=0 and p=0 when q=1; wherein X and Z each represent one or more carbon atoms required to complete a bicyclo ring with the lines ##STR4## representing carbon-carbon bonds; wherein X and Z complete a phenyl moiety when the line ##STR5## represents no bond; wherein X and Z complete a cycloalkyl ring moiety with the lines ##STR6## represent carbon-carbon bonds and with the line ##STR7## representing no bond; and wherein when m is 0, X represents an alkylene moiety, processes for preparing same by means of reacting carbon monoxide and hydrogen with an unsaturated tertiary alcohol defined according to the structure: ##STR8## by means of an oxo reaction, and uses thereof in augmenting or enhancing the aroma of perfume compositions, colognes and perfumed articles (e.g., cosmetic powders, perfumed polymers solid or liquid anionic, cationic, nonionic or zwitterionic detergents, fabric softener compositions, fabric softener articles, hair preparations, face creams, and the like).
摘要翻译：描述的是根据通用结构定义的叔羟基甲醛：其中当m不为0时，线* * * * *和 - - - - - 和/或+ + + + +代表共价碳 - 碳键 ; 并且当m = 0时，线+ + + + + * * * * *和 - - - - - 不表示任何键; 其中R表示氢或甲基; 其中p和q各自表示0或1，条件是当q = 0时p = 1，q = 1时p = 0; 其中X和Z各自表示一个或多个完成具有代表碳 - 碳键的线+ + + + + * * * * *和 - - - - 的双环的所需的碳原子。当线 - - - - 表示无键时，X和Z完全为苯基部分; 其中X和Z完全是环烷基环部分，其中线* * * *和+ + + +代表碳 - 碳键，并且线 - - - - - 不表示键; 并且其中当m为0时，X表示亚烷基部分，通过使一氧化碳和氢与根据以下结构定义的不饱和叔醇反应制备其方法：通过氧代反应，其用途在增加或增强香水组合物，古龙水和香水制品（例如，化妆品粉末，加香聚合物固体或液体阴离子，阳离子，非离子或两性离子洗涤剂，织物柔软剂组合物，织物柔软剂制品，头发制剂，面霜等）的香气）。

43. 发明授权

US4584409A Tertiary hydroxyl carboxaldehydes 失效
标题翻译：三羟基羧醛
公开(公告)号：US4584409A
公开(公告)日：1986-04-22
申请号：US709808
申请日：1985-03-08
申请人： Futoshi Fujioka , Richard M. Boden , William L. Schreiber
发明人： Futoshi Fujioka , Richard M. Boden , William L. Schreiber
IPC分类号： C07C45/49 , C07C47/27 , C07C47/36 , C11B9/00 , C07C47/32 , C07C47/11
CPC分类号： C11B9/0061 , C07C45/49 , C07C47/27 , C07C47/36
摘要： Described are tertiary hydroxyl carboxaldehydes defined according to the generic structure: ##STR1## wherein the lines ##STR2## represent covalent carbon-carbon bonds when m does not=0; and wherein the lines ##STR3## do not represent any bonds when m=0; wherein R represents hydrogen or methyl; wherein p and q each represents 0 or 1 with the proviso that p=1 when q=0 and p=0 when q=1; wherein X and Z each represent one or more carbon atoms required to complete a bicyclo ring with the lines ##STR4## represents carbon-carbon bonds; wherein X and Z complete a phenyl moiety when the line ##STR5## represents no bond; wherein X and Z complete a cycloalkyl ring moiety with the lines ##STR6## represent carbon-carbon bonds and with the line ##STR7## representing no bond; and wherein when m is 0, X represents an alkylene moiety, processes for preparing same by means of reacting carbon monoxide and hydrogen with an unsaturated tertiary alcohol defined according to the structure: ##STR8## by means of an oxo reaction, and uses thereof in augmenting or enhancing the aroma of perfume compositions, colognes and perfumed articles (e.g., cosmetic powders, perfumed polymers, solid or liquid anionic, cationic, nonionic or zwitterionic detergents, fabric softener compositions, fabric softener articles, hair preparations, face creams, and the like).
摘要翻译：描述的是根据通用结构定义的叔羟基甲醛：其中当m不为0时，线* * * * *和 - - - - - 和/或+ + + + +代表共价碳 - 碳键 ; 并且当m = 0时，线+ + + + + * * * * *和 - - - - - 不表示任何键; 其中R表示氢或甲基; 其中p和q各自表示0或1，条件是当q = 0时p = 1，q = 1时p = 0; 其中X和Z各自代表完成具有+ + + + + * * * * *和 - - - - - - 表示碳 - 碳键的双环的一个或多个碳原子; 当线 - - - - 不表示键时，X和Z完成苯基部分; 其中X和Z完全是环烷基环部分，其中线* * * *和+ + + + +代表碳 - 碳键，并且线 - - - - 不表示键; 并且其中当m为0时，X表示亚烷基部分，通过使一氧化碳和氢与根据以下结构定义的不饱和叔醇反应制备其方法：通过氧代反应，其用途在增加或增强香水组合物，古龙水和香水制品（例如，化妆品粉末，加香聚合物，固体或液体阴离子，阳离子，非离子或两性离子洗涤剂，织物柔软剂组合物，织物柔软剂制品，头发制剂，面霜和喜欢）。

44. 发明授权

US3365481A Process for the production of alpha, beta-unsaturated carbonyl compounds 失效
标题翻译：制备α，β-不饱和羰基化合物的方法
公开(公告)号：US3365481A
公开(公告)日：1968-01-23
申请号：US31315563
申请日：1963-10-02
申请人： BASF AG
发明人： GEORG WITTIG , WALTER STILZ , HORST POMMER
IPC分类号： C07C27/22 , C07C45/51 , C07C47/20
CPC分类号： C07C403/24 , C07C45/516 , C07C403/14 , C07C403/18 , C07C2601/16 , C07C47/232 , C07C49/796 , C07C47/27 , C07C47/21

45. 发明申请

WO2014062965A1 2-CYCLOALKYL RESORCINOL CANNABINERGIC LIGANDS 审中-公开
标题翻译： 2-CYCLOALKYL RESORCINOL CANNABINERGG LIGANDS
公开(公告)号：WO2014062965A1
公开(公告)日：2014-04-24
申请号：PCT/US2013/065516
申请日：2013-10-17
申请人： NORTHEASTERN UNIVERSITY
发明人： MAKRIYANNIS, Alexandros , D'SOUZA, Marsha, R. , BAJAJ, Shama , NIKAS, Spyridon, P. , THAKUR, Ganeshsingh, A.
IPC分类号： C07C39/10 , C07C49/23 , C07D311/78
CPC分类号： C07C39/23 , C07C39/42 , C07C43/168 , C07C43/1788 , C07C47/27 , C07C47/46 , C07C49/603 , C07C49/747 , C07C62/32 , C07C69/16 , C07C69/18 , C07C69/63 , C07C235/40 , C07C245/24 , C07C247/06 , C07C255/36 , C07C255/38 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/42 , C07C2603/04 , C07C2603/74 , C07D295/092 , C07D295/096 , C07D295/192 , C07D309/06 , C07D311/78 , C07D339/06
摘要： The present invention relates to novel 2-cycloalkyl resorcinol compounds; to pharmaceutical compositions comprising the compounds; and to methods of preparing the compounds and uses thereof. The disclosed compounds can bind to and modulate the cannabinoid receptors and thus, they are specific ligands for these receptors. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.
摘要翻译：本发明涉及新的2-环烷基间苯二酚化合物; 涉及包含该化合物的药物组合物; 以及制备化合物的方法及其用途。所公开的化合物可以结合并调节大麻素受体，因此它们是这些受体的特异性配体。当以治疗有效量施用于个体或动物时，本发明的化合物在个体或动物中导致足够高的该化合物水平以引起生理反应。生理反应可用于治疗许多生理条件。

46. 发明申请

WO2012121659A1 REDUCTION OF C-0 BONDS BY CATALYTIC TRANSFER HYDROGENOLYSIS 审中-公开
标题翻译：通过催化转移氢化法还原C-0
公开(公告)号：WO2012121659A1
公开(公告)日：2012-09-13
申请号：PCT/SE2012/050262
申请日：2012-03-08
申请人： SAMEC, Joseph , LUNDSTEDT, Anna , SAWADJOON, Supaporn , KAT2BIZ AB C/O INTERPARES KONSULT AB
发明人： SAMEC, Joseph , LUNDSTEDT, Anna , SAWADJOON, Supaporn
IPC分类号： C07C1/22
CPC分类号： C07D317/46 , C07B31/00 , C07C1/2076 , C07C1/22 , C07C1/321 , C07C5/03 , C07C29/132 , C07C29/60 , C07C37/055 , C07C41/18 , C07C45/61 , C07C45/65 , C07C67/00 , C07C67/31 , C07C2523/44 , C07C15/073 , C07C15/085 , C07C15/06 , C07C33/22 , C07C49/84 , C07C47/27 , C07C39/11 , C07C43/23 , C07C69/732 , C07C39/04
摘要： The present invention relates to a method of reducing a C-O bond to the corresponding C-H bond in a substrate which could be a benzylic alcohol, allylic alcohol, ester,or ether or an ether bond beta to a hydroxyl group or alpha to a carbonyl group.
摘要翻译：本发明涉及在底物中还原C-O键的方法，该底物可以是苄基醇，烯丙醇，酯或醚或与羰基的α或α的醚键的醚键。

47. 发明申请

WO2012060387A1 新規ジヒドロキシベンゼン誘導体およびそれらを有効成分とする抗原虫剤审中-公开
标题翻译：新型二羟基苯甲醛衍生物和包含其的抗真菌药物作为活性成分
公开(公告)号：WO2012060387A1
公开(公告)日：2012-05-10
申请号：PCT/JP2011/075216
申请日：2011-11-01
申请人：アリジェン製薬株式会社 , 斎本博之 , 北潔 , 薮義貞 , 山本雅一
发明人：斎本　博之 , 北　潔 , 薮　義貞 , 山本　雅一
IPC分类号： C07C47/56 , A61K31/11 , A61K31/12 , A61K31/192 , A61K31/216 , A61K31/336 , A61K31/351 , A61K31/357 , A61P33/00 , C07C49/86 , C07C59/74 , C07C69/73 , C07D303/32 , C07D307/33 , C07D317/26
CPC分类号： C07C255/53 , A61K31/047 , A61K45/06 , C07C47/27 , C07C47/56 , C07C47/575 , C07C49/248 , C07C49/258 , C07C49/835 , C07C49/84 , C07C59/74 , C07C59/90 , C07C69/738 , A61K2300/00
摘要：　下記の新規な化合物は、原虫類によって引き起こされる疾患を予防または治療するために有用である。　式（Ｉ）（式中、　Ｘは、水素原子またはハロゲン原子を表し、　Ｒ１は、水素原子を表し、　Ｒ２は、水素原子または炭素数１－７のアルキル基を表し、　Ｒ 3 は、－ＣＨＯ、－Ｃ(＝Ｏ)Ｒ 5 、－ＣＯＯＲ 5 （式中Ｒ 5 は、炭素数１－７のアルキル基を表す）、－ＣＨ２ＯＨまたは－ＣＯＯＨを表し、　Ｒ４は、末端の炭素上および／若しくは非末端の炭素上に各種置換基を有する炭素数１－１６のアルキル基、末端の炭素上および／若しくは非末端の炭素上に各種置換基を有する炭素数２－１６のアルケニル基または末端の炭素上および／若しくは非末端の炭素上に各種置換基を有する炭素数２－１６のアルキニル基を表す。）で示される化合物、それらの光学異性体、およびそれらの医薬上許容される塩のうち１種または２種以上を用いる。
摘要翻译：由式（I）表示的新型化合物可用于预防或治疗由原生动物引起的疾病。使用由选自式（I）表示的化合物，其旋光异构体和其药学上可接受的盐中的一种或多种成员制成。式（I）中，X表示氢原子或卤原子; R1表示氢原子; R2表示氢原子或C1-7烷基; R3表示-CHO，-C（= O）R5，-COOR5 [其中R5表示C1-7烷基]，-CH2OH或-COOH; 并且R 4表示在末端碳原子和/或非末端碳原子上具有各种取代基的C1-16烷基，在末端碳原子上具有各种取代基的C2-16烯基和/或末端碳原子和/或非末端碳原子上具有各种取代基的非末端碳原子或C 2-6-16炔基。

48. 发明申请

WO2008042921A2 TETRA-O-SUBSTITUTED BUTANE-BRIDGE MODIFIED NDGA DERIVATIVES, THEIR SYNTHESIS AND PHARMACEUTICAL USE 审中-公开
标题翻译： TETRA-O-取代的丁烷桥改性NDGA衍生物的合成及其药物应用
公开(公告)号：WO2008042921A2
公开(公告)日：2008-04-10
申请号：PCT/US2007080231
申请日：2007-10-02
申请人： ERIMOS PHARMACEUTICALS LLC , CHEN QINGQI , LOPEZ ROCIO A , HELLER JONATHAN D , MORRIS AMANDA JEAN
发明人： CHEN QINGQI , LOPEZ ROCIO A , HELLER JONATHAN D , MORRIS AMANDA JEAN
IPC分类号： A01N37/02
CPC分类号： C07D295/088 , C07C37/50 , C07C39/21 , C07C39/367 , C07C43/2055 , C07C43/225 , C07C43/23 , C07C47/27 , C07C47/273 , C07C217/20 , C07C217/54 , C07C255/33 , C07D277/24 , C07C39/16
摘要： The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.
摘要翻译：本发明涉及去甲二氢愈创木酸衍生物化合物，即丁烷桥改性的去甲二氢愈创木酸（NDGA）化合物和丁烷桥改性的四-O-取代的NDGA化合物，含有它们的药物组合物，其制备方法以及使用它们和试剂盒的方法包括它们用于治疗疾病和病症，特别是由病毒感染如HIV感染，HPV感染或HSV感染引起的或与之相关的疾病，炎性疾病如各种类型的关节炎和炎症性肠病，代谢疾病如糖尿病和高血压，或增殖性疾病如不同类型的癌症。

49. 发明申请

WO00000456A1 PREPARATION OF AN ALDOL USING A BASE-MODIFIED CLAY CATALYST 审中-公开
标题翻译：使用碱改性粘土催化剂制备ALD
公开(公告)号：WO00000456A1
公开(公告)日：2000-01-06
申请号：PCT/US1999/014785
申请日：1999-06-30
IPC分类号： B01J21/16 , B01J23/02 , C01B33/44 , C07B61/00 , C07C29/145 , C07C29/17 , C07C45/62 , C07C45/66 , C07C45/72 , C07C45/73 , C07C45/74 , C07C45/75 , C07C67/44 , C07C69/28 , C07C29/141 , C07C31/20
CPC分类号： C07C29/145 , B01J21/16 , B01J23/02 , C07C29/175 , C07C45/62 , C07C45/66 , C07C45/72 , C07C45/73 , C07C45/74 , C07C45/75 , C07C67/44 , C12C11/02 , Y02P20/52 , C07C31/20 , C07C49/04 , C07C47/02 , C07C47/19 , C07C47/27 , C07C47/36 , C07C31/12 , C07C31/202
摘要： The invention is a base-modified clay and an improved process for preparing a beta-hydroxy compound via an aldol condensation reaction using the base-modified clay as a catalyst. The base-modified clay comprises a clay having secluded conjugate base sites and exchangeable interstitial cationic spaces. In the base-modified clay, the interstitial hydroxyl groups have been converted to oxide sites, at least one structural hydroxyl group has been converted to an oxide site. The base-modified clay contains sufficient conjugate base cations to balance the charge of said oxide groups. The process for preparing a beta-hydroxy compound includes reacting a first carbonyl compound having at least one alpha hydrogen with a second carbonyl compound in the presence of a catalytic amount of a base-modified clay as described above. The invention also relates to a process for preparing a 1,3-diol comprising the hydrogenation of a beta-hydroxy compound prepared by the process described above. In yet another embodiment, the invention relates to a process for preparing a ketone or an alcohol comprising the dehydration of the above described beta-hydroxy-containing carbonyl compound followed by hydrogenation to produce the ketone. The alcohol is prepared by further hydrogenation of the ketone.
摘要翻译：本发明是碱改性的粘土和通过使用碱改性粘土作为催化剂的醛醇缩合反应制备β-羟基化合物的改进方法。碱改性粘土包括具有隐蔽共轭碱基位点和可交换的间隙阳离子空间的粘土。在基础改性的粘土中，间隙羟基已经转化为氧化物位点，至少一个结构羟基已转化为氧化物位点。碱改性粘土含有足够的共轭碱阳离子以平衡所述氧化物基团的电荷。制备β-羟基化合物的方法包括如上所述在催化量的碱改性粘土存在下使具有至少一个α氢的第一羰基化合物与第二羰基化合物反应。本发明还涉及一种制备1,3-二醇的方法，其包括通过上述方法制备的β-羟基化合物的氢化。在另一个实施方案中，本发明涉及一种制备酮或醇的方法，该方法包括将上述含有β-羟基的羰基化合物脱水，然后氢化制备酮。通过酮的进一步氢化制备醇。

50. 发明公开

KR1020120006057A 벤제노이드 다이아조늄 염의 교차-커플링 산물의 제조 방법 无效
标题翻译：生产二苯并二氮鎓盐的交叉偶联产物的方法
公开(公告)号：KR1020120006057A
公开(公告)日：2012-01-17
申请号：KR1020117027308
申请日：2010-04-22
申请人： 칠룸 베타일리공스 게젤샤프트 엠베하 운트 코. 파텐테 II 카게
发明人： 보에게,니콜라 , 크레이펠,안드레아스 , 슈미트,베른트 , 홀터,프랭크 , 버거,르네
IPC分类号： C07C245/20 , C07C37/14 , C07C39/15 , C07C39/19
CPC分类号： C07C37/11 , C07C37/14 , C07C41/48 , C07C45/511 , C07C245/20 , Y02P20/55 , C07C39/15 , C07C39/19 , C07C47/27 , C07C43/307 , C07C43/315
摘要： 본 발명은 하기의 단계를 포함하는, 화학식 1 에 따른 벤제노이드 다이아조늄 염(benzenoid diazonium salt)을 사용한 교차-커플링 산물(cross-coupling product)의 제조 방법에 관한 것이다 :
화학식 1

이 식에서,
R
1 , R
2 , R
3 , R
4 및 R
5
기는 서로 독립적으로 수소, 할로겐, 알킬, 알켄닐, 아릴, 알콕시, 아릴옥시, 니트로, 시아노, 히드록시, 아세틸 및/또는 다이아조 기(diazo group)를 나타내고,
X 는 BF
4 , Cl, F, SO
3 CH
3 , CO
2 CH
3 , PF
6 , ClO
2 CH
3 또는 ClO
4 를 나타낸다.
(a) 다이아조 기(diazo function)를 제외하고는 상기 화학식 1 의 벤제노이드 다이아조늄 염과 동일한 치환기 R
1 , R
2 , R
3 , R
4 및 R
5 를 갖는 벤제노이드 아미드를 가수분해적으로 분해하여 아민을 준비하거나, 이에 상응하는 아민을 준비하는 단계 ;
(b) 상기 아민을 아질산염과 다이아조화(diazotizing)하는 단계 ; 및
(c) 벤제노이드 다이아조늄 염과 하기 화학식 2 의 커플링 파트너(coupling partner)를 촉매 존재 하에 반응시켜 교차-커플링 산물을 형성하는 단계를 포함하고,
화학식 2

이 식에서
R
6 , R
7 및 R
8 은 동일하거나 상이하고, 수소, 카르복시알킬기, 카르복시아릴기, 알킬기, 아릴기, 알콕시기, 아릴옥시기를 나타내고, 각각의 경우에서 Si, N, S, O 및/또는 할로겐 원자를 포함할 수 있으며,
또는 이중결합과 함께, R
6 및 R
7 은 방향족 고리를 형성하고, 이는 R
8 , 및 1 내지 4 개의 추가적인 치환기와 함께 제공될 수 있으며, 이들은 서로 독립적으로, 선형 또는 가지형 (C
1 -C
6 )-알킬기, (C
3 -C
7 )-시클로알킬기, 선형 또는 가지형 (C
1 -C
6 )-알켄닐기, 선형 또는 가지형 (C
1 -C
6 )-알콕시기, 할로겐, 히드록시기, 아미노, 디(C
1 -C
6 )-알킬아미노, 니트로, 아세틸, 시안, 벤질, 4-메톡시벤질, 4-니트로벤질, 페닐 및 4-메톡시페닐기를 포함하는 군으로부터 선택되고,
Y 는 H, -B(OR)
2 , -SnR
3 , -ZnR, -SiR
3 또는 Mg(할로겐)이다.
적어도 단계 (b) 및 (c)는 중간체 산물(intermediate product)의 중간 분리(intermediate isolation) 없이 수행된다. 상기 방법에 따라, 교차-커플링을 보다 단순하게 수행할 수 있고, 보호기(protective group)로부터 제공된 히드록실기를 포함하는 방향족 반응물(aromatic reactant)에서의 히드록실기 없이 개선된 수득률을 나타내었다.

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