- Annulated bacteriochlorins for near-infrared photophysical studies
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Molecules with strong absorption in the near-infrared (NIR) spectral region are of interest for a variety of applications in the photosciences. Nature's NIR absorbers are bacteriochlorophylls, which contain a tetrahydroporphyrin chromophore accentuated by
- Fujita, Hikaru,Jing, Haoyu,Krayer, Michael,Allu, Srinivasarao,Veeraraghavaiah, Gorre,Wu, Zhiyuan,Jiang, Jianbing,Diers, James R.,Magdaong, Nikki Cecil M.,Mandal, Amit K.,Roy, Arpita,Niedzwiedzki, Dariusz M.,Kirmaier, Christine,Bocian, David F.,Holten, Dewey,Lindsey, Jonathan S.
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supporting information
p. 7209 - 7232
(2019/05/24)
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- Diverse ortho-C(sp2)-H functionalization of benzaldehydes using transient directing groups
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Pd-catalyzed C-H functionalizations promoted by transient directing groups remain largely limited to C-H arylation only. Herein, we report a diverse set of ortho-C(sp2)-H functionalizations of benzaldehyde substrates using the transient directing group strategy. Without installing any auxiliary directing group, Pd(II)-catalyzed C-H arylation, chlorination, bromination, and Ir(III)-catalyzed amidation, could be achieved on benzaldehyde substrates. The transient directing groups formed in situ via imine linkage can override other coordinating functional groups capable of directing C-H activation or catalyst poisoning, significantly expanding the scope for metal-catalyzed C-H functionalization of benzaldehydes. The utility of this approach is demonstrated through multiple applications, including late-stage diversification of a drug analogue.
- Liu, Xi-Hai,Park, Hojoon,Hu, Jun-Hao,Hu, Yan,Zhang, Qun-Liang,Wang, Bao-Long,Sun, Bing,Yeung, Kap-Sun,Zhang, Fang-Lin,Yu, Jin-Quan
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supporting information
p. 888 - 896
(2017/05/16)
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Provided are compounds of formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the prog
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Page/Page column 37; 38
(2017/01/23)
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- Efficient three-component synthesis of diversely substituted tetrahydro-1H-cyclopenta[c]quinolines
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The synthesis of highly functionalized substituted tetrahydro-1H-cyclopenta[c]quinoline (I) and its reduced derivatives hexahydro-1H-cyclopenta[c]quinolines (II) via Povarov reaction in high diastereoselectivity and high to moderate yields is described he
- Ni?o, Patricia,Caba, Marta,Aguilar, Nuria,Terricabras, Emma,Albericio, Fernando,Fernàndez, Joan-Carles
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p. 854 - 881
(2017/01/18)
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- Synthesis, radiolabeling and preliminary in vivo evaluation of multimodal radiotracers for PET imaging and targeted radionuclide therapy of pigmented melanoma
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Melanin pigment represents an attractive target to address specific treatment to melanoma cells, such as cytotoxic radionuclides. However, less than half of the patients have pigmented metastases. Hence, specific marker is required to stratify this patient population before proceeding with melanin-targeted radionuclide therapy. In such a context, we developed fluorinated analogues of a previously studied melanin-targeting ligand, N-(2-diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide (ICF01012). These latter can be labeled either with 18F or 131I/125I for positron emission tomography imaging (melanin-positive patient selection) and targeted radionuclide therapy purposes. Here we describe the syntheses, radiosyntheses and preclinical evaluations on melanoma-bearing mice model of several iodo- and fluoro(hetero)aromatic derivatives of the ICF01012 scaffold. After preliminary planar gamma scintigraphic and positron emission tomography imaging evaluations, [125I]- and [18F]-N-[2-(diethylamino)ethyl]-4-fluoro-3-iodobenzamides ([125I]4, [18F]4) were found to be chemically and biologically stable with quite similar tumor uptakes at 1 h p.i. (9.7 ± 2.6% ID/g and 6.8 ± 1.9% ID/g, respectively).
- Billaud, Emilie M.F.,Maisonial-Besset, Aurélie,Rbah-Vidal, Latifa,Vidal, Aurélien,Besse, Sophie,Béquignat, Jean-Baptiste,Decombat, Caroline,Degoul, Fran?oise,Audin, Laurent,Deloye, Jean-Bernard,Dollé, Frédéric,Kuhnast, Bertrand,Madelmont, Jean-Claude,Tarrit, Sébastien,Galmier, Marie-Josèphe,Borel, Michèle,Auzeloux, Philippe,Miot-Noirault, Elisabeth,Chezal, Jean-Michel
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supporting information
p. 818 - 838
(2015/03/05)
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 51
(2013/10/22)
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- A versatile method for the hydrolysis of gem-dibromomethylarenes bearing carboxylate or boronate group into aldehydes
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Hydrolysis of gem-dibromomethylarenes bearing carboxylate or boronate group to corresponding aldehydes without affecting the ester group was successfully accomplished in high yields by subjecting them to refluxing pyridine. Both aromatic and heteroaromatic substrates gave the corresponding aldehydes in good yields. This method was efficiently adapted for the large scale synthesis of 2d and 2f.
- Augustine, John Kallikat,Naik, Y. Arthoba,Mandal, Ashis Baran,Chowdappa, Nagaraja,Praveen, Vinuthan B.
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p. 688 - 695
(2008/04/12)
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