153874-43-2Relevant academic research and scientific papers
CuII/TEMPO-Catalyzed Enantioselective C(sp3)–H Alkynylation of Tertiary Cyclic Amines through Shono-Type Oxidation
Chen, Zhi-Hao,Gao, Pei-Sen,Mei, Tian-Sheng,Sun, Bing,Wang, Zhen-Hua,Weng, Xin-Jun,You, Shu-Li,Zheng, Chao
supporting information, p. 15254 - 15259 (2020/06/23)
A novel strategy for asymmetric Shono-type oxidative cross-coupling has been developed by merging copper catalysis and electrochemistry, affording C1-alkynylated tetrahydroisoquinolines with good to excellent enantioselectivity. The use of TEMPO as a co-catalytic redox mediator is crucial not only for oxidizing a tetrahydroisoquinoline to an iminium ion species but also for decreasing the oxidation potential of the reaction. A novel bisoxazoline ligand is also reported.
Spiro[pyrrolidine-3, 3′-oxindoles] and their indoline analogues as new 5-HT6 receptor chemotypes
Kelemen, ádám A.,Satala, Grzegorz,Bojarski, Andrzej J.,Keseru, Gy?rgy M.
, (2018/01/17)
Synthetic derivatives of spiro[pyrrolidinyl-3, 3′-oxindole] alkaloids (coerulescine analogues) were investigated as new ligands for aminergic G-protein coupled receptors (GPCRs). The chemical starting point 2′-phenylspiro[indoline-3, 3′-pyrrolidin]-2-one scaffold was identified by virtual fragment screening utilizing ligand- and structure based methods. As a part of the hit-to-lead optimization a structure-activity relationship analysis was performed to explore the differently substituted 2′-phenyl-derivatives, introducing the phenylsulphonyl pharmacophore and examining the corresponding reduced spiro[pyrrolidine-3, 3′-indoline] scaffold. The optimization process led to ligands with submicromolar affinities towards the 5-HT6 receptor that might serve as viable leads for further optimization.
Aqueous Titanium Trichloride Promoted Reductive Cyclization of o-Nitrostyrenes to Indoles: Development and Application to the Synthesis of Rizatriptan and Aspidospermidine
Tong, Shuo,Xu, Zhengren,Mamboury, Mathias,Wang, Qian,Zhu, Jieping
, p. 11809 - 11812 (2015/10/05)
Treatment of o-nitrostyrenes with aqueous TiCl3 solution at room temperature afforded indoles through a formal reductive C(sp2)-H amination process. A range of functions such as halides (Cl, Br), carbonyl (ester, carbamate), cyano, hydroxy, and amino groups were tolerated. From β,β-disubstituted o-nitrostyrenes, 2,3-disubstituted indoles were formed by a domino reduction/cyclization/migration process. Mild conditions, simple experimental procedure, ready accessibility of the starting materials and good to excellent yields characterize the present transformation. The methodology was used as a key step in a concise synthesis of rizatriptan and a formal total synthesis of aspidospermidine. Mild and efficient treatment of o-nitrostyrenes with aqueous TiCl3 solution at room temperature afforded indoles through a formal reductive C(sp2)-Hamination process. A concise synthesis of a marketed drug (rizatriptan) and a formal total synthesis of aspidospermidine featuring this novel N-heterocyclization process are reported.
Development of a Suzuki cross-coupling reaction between 2-azidoarylboronic pinacolate esters and vinyl triflates to enable the synthesis of [2,3]-fused indole heterocycles
Jana, Navendu,Nguyen, Quyen,Driver, Tom G.
, p. 2781 - 2791 (2014/04/17)
The scope and limitations of a Suzuki reaction between 2-azidoarylboronic acid pinacolate esters and vinyl triflates are reported. This cross-coupling reaction enables the regioselective synthesis of indoles after a subsequent RhII2-catalyzed sp2-C-H bond amination reaction.
Hydroxymethylcyclohexylamines
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Page/Page column 19, (2011/04/18)
The invention relates to compounds which have an affinity for the μ opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
NOVEL TRICYCLIC HETEROCYCLE COMPOUND
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Page/Page column 57, (2008/06/13)
―The present invention relates to the compound represented by formula (I) ????????A―X―Y―Z―B?????(I) (wherein A is a cyclic group which may have a substituent(s); X is a single bond or a spacer; Y is a single bond or a spacer; Z is a single bond or a spacer; B is a hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s)), a salt thereof, a solvate thereof or a prodrug thereof. The compound represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for preventive and/or therapeutic agent for a disease caused by stress.
Antibacterial compounds
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, (2008/06/13)
Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment bacterial infections: wherein: R1is Ar or Het; R2is H, C1-6alkyl or Ar—C0-6alkyl; X is H, C1-4alkyl
Inhibitors of bacterial enoyl acyl carrier protein reductase (FabI): 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as potential antibacterial agents
Seefeld, Mark A,Miller, William H,Newlander, Kenneth A,Burgess, Walter J,Payne, David J,Rittenhouse, Stephen F,Moore, Terrance D,DeWolf Jr., Walter E,Keller, Paul M,Qiu, Xiayang,Janson, Cheryl A,Vaidya, Kalindi,Fosberry, Andrew P,Smyth, Martin G,Jaworski, Deborah D,Slater-Radosti, Courtney,Huffman, William F
, p. 2241 - 2244 (2007/10/03)
An SAR study of a screening lead has led to the identification of 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as inhibitors of Staphylococcus aureus enoyl acyl carrier protein reductase (FabI).
Benzodiazonine derivatives binding to cholecystokinin or gastrin receptors
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, (2008/06/13)
PCT No. PCT/GB97/00632 Sec. 371 Date Oct. 26, 1998 Sec. 102(e) Date Oct. 26, 1998 PCT Filed Mar. 7, 1997 PCT Pub. No. WO97/32860 PCT Pub. Date Sep. 12, 1997Compounds of the formula wherein one of U and V is -CHR2-, and the other of U and V is selected fro
