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. 发明申请

WO2010115098A2 PALLADIUM-CATALYZED ORTHO-FLUORINATION 审中-公开
标题翻译：钯催化的ORTHO-FLUORINATION
公开(公告)号：WO2010115098A2
公开(公告)日：2010-10-07
申请号：PCT/US2010/029775
申请日：2010-04-02
申请人： THE SCRIPPS RESEARCH INSTITUTE , YU, Jin-Quan
发明人： YU, Jin-Quan
CPC分类号： C07C209/74 , C07C303/40 , C07C211/29 , C07C311/09
摘要： A new method of or tho -fluorination where an aryl C-H bond is directly replaced by an aryl C-F bond in a palladium-catalyzed reaction is provided. The method includes the ortho -fluorination of a triflamide protected benzylamine, a palladium catalyst, such as Pd(OTf) 2 , a fluorinating reagent such as N-fluoro-2,4,6-trimethylpyridinium triflate, and a ligand to promote the reaction such as N-methylpyrrolidinone (NMP).
摘要翻译：提供了在钯催化的反应中芳基C-H键被芳基C-F键直接替代的新的或其氟化方法。该方法包括三氟甲磺酰胺保护的苄胺，钯催化剂如Pd（OTf）2，氟化试剂如N-氟-2,4,6-三甲基吡啶鎓三氟甲磺酸酯的正氟化和促进反应的配体例如N-甲基吡咯烷酮（NMP）。

2. 发明申请

WO2016123361A1 LIGAND-ENABLED META-C-H ACTIVATION USING A TRANSIENT MEDIATOR 审中-公开
标题翻译：使用瞬态介质的启动META-C-H激活
公开(公告)号：WO2016123361A1
公开(公告)日：2016-08-04
申请号：PCT/US2016/015396
申请日：2016-01-28
申请人： THE SCRIPPS RESEARCH INSTITUTE , YU, Jin-Quan
发明人： YU, Jin-Quan
IPC分类号： C07C233/15 , C07D209/04 , C07D307/77
CPC分类号： C07C233/15 , C07B43/06 , C07C231/12 , C07C233/59 , C07C2602/10 , C07D209/04 , C07D209/42 , C07D209/48 , C07D307/77 , C07D307/84
摘要： An alternative approach to formation of a C-C bond at a meta-position of an aromatic compound is disclosed that employs an ethylenically unsaturated bicyclic compound as a transient mediator to achieve meta-selective C-H activation with a simple and common ortho-directing group. The use of a pyridine-based ligand assists in relaying the palladium catalyst to the meta-position by the unsaturated bicyclic compound following initial ortho-C-H activation.
摘要翻译：公开了在芳族化合物的间位形成C-C键的替代方法，其采用烯键式不饱和双环化合物作为瞬时介体，以简单且常见的正向导向基团实现元选择性C-H活化。使用吡啶基配体有助于在最初的邻C-H活化之后将不饱和双环化合物将钯催化剂中和到间位。

3. 发明申请

WO2021108411A1 MERGING C(SP3)-H ACTIVATION WITH DNA-ENCODING 审中-公开
公开(公告)号：WO2021108411A1
公开(公告)日：2021-06-03
申请号：PCT/US2020/062026
申请日：2020-11-24
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： YU, Jin-Quan
IPC分类号： C12N15/113 , C07D213/56 , B01J23/44
摘要： Palladium-catalyzed C(sp3)-H arylation of aliphatic carboxylic acids, amides and ketones with BNA-encoded aryl iodides in water is disclosed, Furthermore, sequential C-H arylation chemistry enabled the on-DNA synthesis of structurally-diverse scaffolds containing enriched C(sp3) character, chiral centers, cyclopropane, cyclobutane, and heterocycles. That new chemistry permits preparation of a DNA- encoded library (BEL) technology that can dramatically expedite hit identification in drug discovery owing to its ability to perform protein affinity selection with millions or billions of molecules in a single experiment. The sequential functionalization of multiple C-H bonds provides an unique avenue for creating diversity and complexity from simple starting materials. The use of water as solvent, the presence of DMA, and the extremely low concentration of DMA-encoded coupling partners (0.001 M) have previously hampered the development DMA-encoded C(sp3)-H activation reactions, but many of those hurdles have now been overcome.

4. 发明申请

WO2006026053A1 CATALYTICS ASYMMETRIC ACTIVATION OF UNACTIVATED C-H BONDS, AND COMPOUNDS RELATED THERETO 审中-公开
标题翻译：催化剂不对称活化的C-H BONDS及其相关化合物
公开(公告)号：WO2006026053A1
公开(公告)日：2006-03-09
申请号：PCT/US2005/027713
申请日：2005-08-05
申请人： BRANDEIS UNIVERSITY , YU, Jin-Quan , GIRI, Ramesh
发明人： YU, Jin-Quan , GIRI, Ramesh
IPC分类号： C07D417/02
CPC分类号： C07C69/74 , C07C69/65 , C07D207/06 , C07D213/74 , C07D263/10 , C07D263/12 , C07D263/14 , C07D265/32 , C07D307/33 , C07D413/06 , Y02P20/55
摘要： One aspect of the present invention is directed in part to catalytic and stereoselective functionalization of unactivated C-H bonds of simple organic substrates. The compounds and methods provided herein allow one to control the stereochemistry in a C-H activation step, activate substrates containing α-hydrogens next to the directing group, and remove a directing group under mild conditions. One aspect of the present invention relates to a transition-metal-catalyzed method for selective and asymmetric oxidation of carbons located in a β- or γ-position relative to an auxiliary. Another aspect of the invention relates to the enantiomerically-enriched substrates and the enantiomerically-enriched products formed via said method. In certain embodiments, oxazoline and oxazinone directing groups are used. In addition, the Boc protecting group has been identified as a directing group which does not necessitate removal.
摘要翻译：本发明的一个方面部分地涉及简单有机底物的未活化C-H键的催化和立体选择性官能化。本文提供的化合物和方法允许控制C-H活化步骤中的立体化学，活化在指导基团旁边含有α-氢的底物，并在温和条件下除去引导基团。本发明的一个方面涉及用于相对于辅助剂位于β或β-位的碳的选择性和不对称氧化的过渡金属催化方法。本发明的另一方面涉及通过所述方法形成的对映异构体富集的底物和对映异构体富集的产物。在某些实施方案中，使用恶唑啉和恶嗪酮指导基团。此外，Boc保护基被鉴定为不需要去除的引导基团。

5. 发明申请

WO2020243754A1 LIGAND-ENABLED ß-C(sp3)–H LACTONIZATION FOR ß-C–H FUNCTIONALIZATIONS 审中-公开
公开(公告)号：WO2020243754A1
公开(公告)日：2020-12-03
申请号：PCT/US2020/070100
申请日：2020-05-29
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： YU, Jin-Quan , ZHUANG, Zhe
IPC分类号： C07D305/12 , C07D401/06 , C07D407/04 , C07D407/06 , C07C51/09
摘要： Provided herein is a method of forming a beta-lactone from a carboxylic acid having a beta-carbon with a hydrogen atom disposed thereon. The method comprises contacting a carboxylic acid of formula (1) as described herein with an effective amount of a palladium(II) catalyst, an effective amount of an N-protected aminoacid ligand, and t-butylhydroperoxide in a solvent comprising hexafluoroisopropanol (HFIP), at about 60˚C to provide a beta-lactone of formula (2) as described herein.

6. 发明申请

WO2018080897A1 PD-CATALYZED γ-C(SP3)-H ARYLATION / HETEROARYLATION OF FREE AMINES 审中-公开
标题翻译： PD-CATALYZEDγ-C（SP3）-H芳基化/杂原子自由胺
公开(公告)号：WO2018080897A1
公开(公告)日：2018-05-03
申请号：PCT/US2017/057434
申请日：2017-10-19
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： YU, Jin-Quan
IPC分类号： C07C209/68 , C07B37/00
CPC分类号： C07C269/04 , B01J31/2239 , B01J2231/44 , B01J2531/824 , C07B37/04 , C07C209/68 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D213/40 , C07D213/61 , C07D213/64 , C07D215/12 , C07D241/42 , C07D319/18 , C07D333/22 , C07D471/04 , C07C211/40 , C07C271/22
摘要： Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldenyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
摘要翻译： Pd（II）催化的g-G（sp3）-H芳基化或伯胺的杂芳基化通过使用2-羟基烟酰基腺苷作为催化瞬时指导基团来实现。重要的是，催化剂和引导基团的负载量可以分别降低到2％和4％，从而表现出这种新设计的瞬态引导组的高效率。杂环芳基碘化物也与该反应相容。此外，使用该反应可快速合成1,2,3,4-四氢萘啶衍生物。

7. 发明申请

WO2017165304A3 Pd(II)-CATALYZED ENANTIOSELECTIVE BETA-METHYLENE C(sp3)-H BOND ACTIVATION 审中-公开
标题翻译： Pd（II） - 定性对映选择性亚甲基C（sp3）-H键活化
公开(公告)号：WO2017165304A3
公开(公告)日：2017-09-28
申请号：PCT/US2017/023229
申请日：2017-03-20
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： YU, Jin-Quan
IPC分类号： C07D215/04 , C07D401/06 , C07D491/048 , C07D491/052
摘要： Chiral acetyl-protected aminoethyl quinoline (APAQ), pyridine and imazoline ligands are disclosed that enable Pd (II)-catalyzed enantioselective arylation or heteroarylation of ubiquitous prochiral β-methylene C-H bonds of aliphatic amides offers an alternative disconnection for constructing β-chiral centers. Systematic tuning of the ligand structure reveals that a six-membered instead of a five-membered chelation of these types of ligands with the Pd(II) is important for accelerating the C(sp 3 )-H activation thereby achieving enantioselectivity for quinoline and pyridine ligands.
摘要翻译：手性乙酰基保护的氨基乙基喹啉（APAQ），吡啶和咪唑啉配体公开了使Pd（II）催化的脂肪族酰胺的普遍存在的前手性β-亚甲基CH键的对映选择性芳基化或杂芳基化提供替代断开构建β-手性中心。配体结构的系统调节揭示了六元而不是这些类型的配体与Pd（II）的五元螯合对于加速C（sp 3 -s）-H活化是重要的从而实现喹啉和吡啶配体的对映体选择性。

8. 发明申请

WO2017165304A2 Pd(II)-CATALYZED ENANTIOSELECTIVE BETA-METHYLENE C(sp3)-H BOND ACTIVATION 审中-公开
公开(公告)号：WO2017165304A2
公开(公告)日：2017-09-28
申请号：PCT/US2017/023229
申请日：2017-03-20
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： YU, Jin-Quan
IPC分类号： C07D215/04 , C07D401/06 , C07D491/048 , C07D491/052
摘要： Chiral acetyl-protected aminoethyl quinoline (APAQ), pyridine and imazoline ligands are disclosed that enable Pd (II)-catalyzed enantioselective arylation or heteroarylation of ubiquitous prochiral β-methylene C-H bonds of aliphatic amides offers an alternative disconnection for constructing β-chiral centers. Systematic tuning of the ligand structure reveals that a six-membered instead of a five-membered chelation of these types of ligands with the Pd(II) is important for accelerating the C(sp 3 )-H activation thereby achieving enantioselectivity for quinoline and pyridine ligands.

9. 发明申请

WO2023287964A1 LIGAND-CONTROLLED DIVERGENT DEHYDROGENATIVE REACTIONS OF ALIPHATIC ACIDS 审中-公开
公开(公告)号：WO2023287964A1
公开(公告)日：2023-01-19
申请号：PCT/US2022/037089
申请日：2022-07-14
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： YU, Jin-Quan , WANG, Zhen , HU, Liang
IPC分类号： C07C5/333 , C07C5/42 , C07C5/32 , B01J23/44
摘要： Disclosed herein are palladium-catalyzed dehydrogenation processes of carboxylic acids to make α, β-unsaturated carboxylic acids or γ-alkylidene butenolides. The processes allow the chemoselective dehydrogenation of carboxylic acids in the presence of other enolizable functionalities such as ketones, providing reactivity that is inaccessible with existing carbonyl desaturation protocols.

10. 发明申请

WO2022125736A1 A TAUTOMERIC LIGAND ENABLES BIOMIMETIC C-H HYDROXYLATION WITH MOLECULAR OXYGEN 审中-公开
公开(公告)号：WO2022125736A1
公开(公告)日：2022-06-16
申请号：PCT/US2021/062538
申请日：2021-12-09
申请人： THE SCRIPPS RESEARCH INSTITUTE [US]/[US]
发明人： YU, Jin-Quan , WANG, Zhen , LI, Zhen
IPC分类号： B01J23/40 , B01J23/44 , C07C37/58 , C07C51/347 , C07C51/367
摘要： Disclosed herein is a process for making a compound of formula (2) by (hetero)aromatic C-H hydroxylation of a compound of formula (1): catalyzed by palladium(II) and a bidentate ligand in the presence of O2. The process is useful for instance, in the late-stage modification of medicinally important heterocycles.

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