- A Highly Efficient Dimeric Manganese-Catalyzed Selective Hydroarylation of Internal Alkynes
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We have developed a general and site-predictable manganese-catalyzed hydroarylation of internal alkynes in the presence of water, under an air atmosphere without the involvement of ligand. The unique catalytic feature of this reaction is highlighted by comparison with other widely used transition metal catalysts including palladium, rhodium, nickel, or copper. The simple operation, high efficiency and excellent functional group compatibility make this protocol practical for more than 90 structurally diverse internal alkynes, overcoming the influence of both electronic and steric effect of alkynes. Its exclusive regio- and chemoselectivity originates from the unique reactivity of the manganese-based catalyst towards an inherent double controlled strategy of sterically hindered propargyl alcohols without the installing of external directing groups. Its synthetic robustness and practicality have been illustrated by the concise synthesis of bervastatin, a hypolipidemic drug, and late-stage modification of complex alkynes with precise regioselectivity.
- Huang, Congcong,Li, Weipeng,Liu, Gengtu,Pang, Yubo,Xie, Jin,Yuan, Xiang-Ai
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supporting information
p. 12789 - 12794
(2020/06/02)
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- SUBSTITUTED IMIDAZOLECARBOXYLATE DERIVATIVES AND THE USE THEREOF
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A compound is shown in formula (I). The derivatives of the compound include a stereoisomer, a pharmaceutically acceptable salt, a solvate, a prodrug, a metabolite, a deuterated derivative. The compound is a structurally novel substituted imidazole formate derivative. Substituted imidazole formate derivatives are used in preparing a drug with sedative, hypnotic and/or anesthetic effects, as well as a drug that can control the state of epilepsy. The compound has a good inhibitory effect on the central nervous system, and provides a new option for clinical screening of and/or preparation of a drug with sedative, hypnotic and/or anesthetic effects and controlling the state of epilepsy.
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Paragraph 0753-0755
(2020/12/08)
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- COMPOUNDS AND USES THEREOF
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The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
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Paragraph 0820
(2019/11/11)
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- Trialkylborane-Mediated Multicomponent Reaction for the Diastereoselective Synthesis of Anti-δ,δ-Disubstituted Homoallylic Alcohols
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The trialkylborane/O2-mediated reaction of propargyl acetates having a tributylstannyl group at an alkyne terminus with aldehydes in a THF-H2O solvent system gave anti-δ,δ-disubstituted homoallylic alcohols with good to high diastereoselectivity. Intriguingly, two alkyl groups derived from trialkylborane were embedded into the reaction product. The trialkylborane plays a key role not only as a radical initiator but also as a source of alkyl radicals.
- Horino, Yoshikazu,Murakami, Miki,Aimono, Ataru,Lee, Jun Hee,Abe, Hitoshi
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supporting information
p. 476 - 480
(2019/01/14)
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- SUBSTITUTED PYRAZOLYL[4,3-C]PYRIDINECOMPOUNDS AS RET KINASE INHIBITORS
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Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2 and R3 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
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Paragraph 00547
(2019/08/08)
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- Synthesis of 2-(2-Oxo-2-phenylethyl)cyclopentanone by Rhodium-Catalyzed Tandem Alkynyl Cyclobutanols Hydroacylation and Semipinacol Rearrangement
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A rhodium-catalyzed tandem reaction of alkynyl cyclobutanols with salicylaldehydes has been developed. The reaction offers a new and atom-economical approach for the selective preparation of multisubstituted 2-(2-oxo-2-phenylethyl)cyclopentanone in high y
- Guo, Rui,Mo, Xueling,Zhang, Guozhu
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supporting information
p. 1263 - 1267
(2019/02/26)
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- HPK1 INHIBITORS, PREPARATION METHOD AND APPLICATION THEREOF
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Disclosed are HPK-1 inhibitors having a structure represented by Formula (X), pharmaceutical compositions comprising the HPK-1 inhibitors, methods of using the HPK-1 inhibitors, such as treating cancers, methods of preparing the HPK-1 inhibitors, and the synthetic intermediates.
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Page/Page column 115
(2019/11/12)
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- Structure-based design of tricyclic NF-κB inducing kinase (NIK) inhibitors that have high selectivity over phosphoinositide-3-kinase (PI3K)
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We report here structure-guided optimization of a novel series of NF-κB inducing kinase (NIK) inhibitors. Starting from a modestly potent, low molecular weight lead, activity was improved by designing a type 11/2 binding mode that accessed a back pocket past the methionine-471 gatekeeper. Divergent binding modes in NIK and PI3K were exploited to dampen PI3K inhibition while maintaining NIK inhibition within these series. Potent compounds were discovered that selectively inhibit the nuclear translocation of NF-κB2 (p52/REL-B) but not canonical NF-κB1 (REL-A/p50).
- Castanedo, Georgette M.,Blaquiere, Nicole,Beresini, Maureen,Bravo, Brandon,Brightbill, Hans,Chen, Jacob,Cui, Hai-Feng,Eigenbrot, Charles,Everett, Christine,Feng, Jianwen,Godemann, Robert,Gogol, Emily,Hymowitz, Sarah,Johnson, Adam,Kayagaki, Nobuhiko,Kohli, Pawan Bir,Knüppel, Kathleen,Kraemer, Joachim,Krüger, Susan,Loke, Pui,McEwan, Paul,Montalbetti, Christian,Roberts, David A.,Smith, Myron,Steinbacher, Stefan,Sujatha-Bhaskar, Swathi,Takahashi, Ryan,Wang, Xiaolu,Wu, Lawren C.,Zhang, Yamin,Staben, Steven T.
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supporting information
p. 627 - 640
(2017/02/05)
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- ANTIRETROVIRAL AGENTS
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Compounds of formula I or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
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Paragraph 0360
(2016/03/22)
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- PIPERIDINE ISOXAZOLE AND ISOTHIAZOLE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to piperidine isoxazole and isothiazole orexin compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 67-68
(2016/05/19)
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- CHROMENE AND 1,1 A,2,7B-TETRAHYDROCYCLOPROPA[C]CHROMENE PYRIDOPYRAZINEDIONES AS GAMMA-SECRETASE MODULATORS
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Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b/su
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Page/Page column 102; 103
(2015/12/30)
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- Stereoselective One-Pot synthesis of 1-Aminoindanes and 5,6-Fused azacycles using a Gold-Catalyzed Redox-Pinacol-Mannich-Michael cascade
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"Chemical Equation Presented" Just another Mannich Monday: A cascade intramolecular redox-pinacol-Mannich-Michael reaction sequence catalyzed by gold complexes can be used to generate a variety of structures including spirocycles, 1-aminoindanes, and 5,6-fused azabicycles that have a quaternary carbon center. The reaction is characterized by complete atom-economy, high diastereoselectivity, and remarkable efficiency through tandem reactions.
- Yeom, Hyun-Suk,Lee, Youngun,Jeong, Jaewon,So, Eunsoo,Hwang, Soojin,Lee, Ji-Eun,Lee, Shim Sung,Shin, Seunghoon
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supporting information; experimental part
p. 1611 - 1614
(2010/06/15)
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- Synthesis of alkyne derivatives of a novel triazolopyrazine as A 2A adenosine receptor antagonists
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A novel [1,2,4]triazolo[1,5-a]pyrazine core was synthesized and coupled with terminal acetylenes. The structure-activity relationship of the alkynes from this novel template was studied for their in vitro and in vivo adenosine A2A receptor antagonism. Selected compounds from this series were shown to have potent in vitro and in vivo activities against adenosine A 2A receptor. Compound 12, in particular, was found to be orally active at 3 mg/kg in both a mouse catalepsy model and a 6-hydroxydopamine- lesioned rat model.
- Yao, Gang,Haque, Serajul,Sha, Li,Kumaravel, Gnanasambandam,Wang, Joy,Engber, Thomas M.,Whalley, Eric T.,Conlon, Patrick R.,Chang, Hexi,Kiesman, William F.,Petter, Russell C.
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p. 511 - 515
(2007/10/03)
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- Antiulcer compounds having a substituted alkynyl or quinoxaline nucleus and methods of making thereof
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This invention relates to a novel compound which is useful as a drug in preventing and/or treating peptic ulcer-related diseases, to a production process thereof and to a pharmaceutical composition containing the same. Particularly, it provides a compound which has a specified substituted alkynylpyrazine nucleus or a specified substituted alkynylquinoxaline nucleus, represented by the following formula (I) STR1 wherein A is represented by the following formula (II) or (III) STR2 and R1 is represented by the following formula (IV), STR3 and the salts thereof, a production process thereof and a pharmaceutical composition containing the same. The inventive compound is useful as a drug in preventing and/or treating peptic ulcer-related diseases.
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