261638-97-5Relevant articles and documents
Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway
Němec, Václav,Hylsová, Michaela,Maier, Luká?,Flegel, Jana,Sievers, Sonja,Ziegler, Slava,Schr?der, Martin,Berger, Benedict-Tilman,Chaikuad, Apirat,Val?íková, Barbora,Uldrijan, Stjepan,Drápela, Stanislav,Sou?ek, Karel,Waldmann, Herbert,Knapp, Stefan,Paruch, Kamil
supporting information, p. 1062 - 1066 (2019/01/04)
Reported is the identification of the furo[3,2-b]pyridine core as a novel scaffold for potent and highly selective inhibitors of cdc-like kinases (CLKs) and efficient modulators of the Hedgehog signaling pathway. Initially, a diverse target compound set was prepared by synthetic sequences based on chemoselective metal-mediated couplings, including assembly of the furo[3,2-b]pyridine scaffold by copper-mediated oxidative cyclization. Optimization of the subseries containing 3,5-disubstituted furo[3,2-b]pyridines afforded potent, cell-active, and highly selective inhibitors of CLKs. Profiling of the kinase-inactive subset of 3,5,7-trisubstituted furo[3,2-b]pyridines revealed sub-micromolar modulators of the Hedgehog pathway.
Copper-catalyzed regioselective hydroboration of terminal alkynes in aqueous medium
Yao, Zi-Jian,Hong, Shibin,Zhang, Wei,Liu, Mengyan,Deng, Wei
supporting information, p. 910 - 913 (2016/02/05)
A mild and environment-friendly copper-catalyzed hydroboration of terminal alkynes in aqueous medium was reported. Regioselectivity control was achieved in the presence of cyclodextrin-bispyridine ligand (CD-1). This protocol was successfully applied to inactivated terminal alkynes. Moreover, the ligand was recovered and reused without any loss of activity over five cycles.
Iridium-catalyzed enantioselective hydrogenation of alkenylboronic esters
Ganic, Adnan,Pfaltz, Andreas
supporting information; experimental part, p. 6724 - 6728 (2012/07/28)
Choose the right ligand: An iridium complex derived from a phosphino-imidazoline ligand is a highly efficient catalyst for the asymmetric hydrogenation of terminal vinyl boronic esters (see scheme). On the other hand, trisubstituted alkenyl-boronates can
SPIROCYCLIC GPR40 MODULATORS
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Page/Page column 194, (2010/04/30)
The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I'A or I'B, where the definitions of the variables are provided herein. The present invention also
CONFORMATIONALLY CONSTRAINED CARBOXYLIC ACID DERIVATIVES USEFUL FOR TREATING METABOLIC DISORDERS
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Page/Page column 173, (2009/10/22)
The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
Palladium-catalyzed cross-coupling reaction of bis(pinacolato)diboron with 1-alkenyl halides or triflates: Convenient synthesis of unsymmetrical 1,3-dienes via the borylation-coupling sequence
Takagi, Jun,Takahashi, Kou,Ishiyama, Tatsuo,Miyaura, Norio
, p. 8001 - 8006 (2007/10/03)
The synthesis of 1-alkenylboronic acid pinacol esters via a palladium-catalyzed cross-coupling reaction of bis(pinacolato)diboron (pin2B2, pin = Me4C2O2) with 1-alkenyl halides or triflates was carrie
A borylcopper species generated from bis(pinacolato)diboron and its additions to α,β-unsaturated carbonyl compounds and terminal alkynes
Takahashi, Kou,Ishiyama, Tatsuo,Miyaura, Norio
, p. 47 - 53 (2007/10/03)
The addition of bis(pinacolato)diboron [(Me4C2O2)B-B(O2C2Me 4)] to α,β-unsaturated carbonyl compounds giving β-boryl carbonyl compounds and the addition to terminal alkynes yielding either 2-boryl-1-alkenes or 1-boryl-1-alkenes were carried out in DMF at room temperature in the presence of CuCl and AcOK. The transmetalation between diboron and [Cu(Cl)OAc]K generating a borylcopper species was proposed as the key step in the reactions because CuOAc similarly mediated both addition reactions to enones and alkynes in the presence of LiCl.
Synthesis of 1-alkenylboronic esters via palladium-catalyzed cross-coupling reaction of bis(pinacolato)diboron with 1-alkenyl halides and triflates
Takahashi, Kou,Takagi, Jun,Ishiyama, Tatsuo,Miyaura, Norio
, p. 126 - 127 (2007/10/03)
The synthesis of 1-alkenylboronic acid pinacol esters via the palladium-catalyzed cross-coupling reaction of 1-alkenyl halides or triflates with bis(pinacolato)diboron [(Me4C2O2)B-B(O2C2Me 4/sub