- Syntheses of stable-isotope labeled [M + 7] and [M + 6] 2-(methylamino)imidazole
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Stable isotope-labeled 2-methylaminoimidazole (M + 7 and M + 6) was required as an intermediate in the synthesis of mass labeled drug candidates. These two isotopomers were synthesized with total yields of 24 and 36%, respectively. Labeled 2-aminoimidazol
- Zhang, Yinsheng
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- COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
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The invention relates to a compound of Formula I, pharmaceutical compositions comprising a compound of Formula I, and pharmaceutically acceptable slats thereof, pharmaceutical compositions comprising such compounds and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to a subject in need thereof.
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Page/Page column 160-161
(2020/08/22)
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- Keto-imidazoline-2-imine ligand [N,O] bidentate nickel and palladium complex as well as preparation method and application thereof
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The invention relates to a keto-imidazoline-2-imine [N,O] bidentate nickel and palladium complex as well as a preparation method and application thereof. The preparation method comprises the followingsteps: reacting a keto-imidazoline-2-imine ligand with a hydrogen withdrawing reagent and a metal precursor in sequence to prepare a keto-imidazoline-2-imine [N,O] bidentate nickel and palladium complex; and the structural formula of the prepared complex is one of formulas shown in the specification. The complex and a cocatalyst form a catalyst composition, the complex or the catalyst compositionis used for catalyzing homopolymerization or copolymerization of olefin monomers, and the specific process is as follows: under the protection of nitrogen, firstly dissolving the complex or the catalyst composition in a solvent, then adding an olefin monomer, and conducting reacting for a period of time at a certain temperature and under a certain pressure to prepare the olefin polymer. The complex and the catalyst composition provided by the invention have relatively high catalytic activity, high tolerance to polar monomers and relatively low application cost.
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Paragraph 0154; 0159
(2019/11/13)
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- Metal-free C(sp2)-H functionalization of azoles: K2CO3/I2-mediated oxidation, imination, and amination
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The direct C2-H oxidation and imination of a wide variety of azoles was achieved by using a commercially available simple K2CO3/I2 reagent combination. The iodinated azole adduct, produced via the in situ generation of N-heterocyclic carbene, is the key intermediate for C2-H oxidation, imination, and amination of azoles. Significantly, these reactions proceed under mild conditions with high to excellent yields, are scalable to large quantity and exhibit a broad substrate scope. Interestingly, this direct C2-H imination method allowed us to access various pharmacologically active N6-alkyl or N6-aryl substituted benzimidazoquinazolinone scaffolds through intramolecular C-H imination in a sequential one-pot reaction.
- Das, Ranajit,Banerjee, Mainak,Rai, Rakesh Kumar,Karri, Ramesh,Roy, Gouriprasanna
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p. 4243 - 4260
(2018/06/22)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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Paragraph 00799
(2016/01/25)
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- Synthesis and evaluation of 6-methylene-bridged uracil derivatives. Part 2: Optimization of inhibitors of human thymidine phosphorylase and their selectivity with uridine phosphorylase
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A series of novel 6-methylene-bridged uracil derivatives have been optimized for clinical use as the inhibitors of human thymidine phosphorylase (TP). We describe their synthesis and evaluation. Introduction of a guanidino or an amidino group enhanced the in vitro inhibitory activity of TP comparing with formerly reported inhibitor 1. Their selectivity for TP based on uridine phosphorylase inhibitory activity was also evaluated. Compound 2 (TPI) has been selected for clinical evaluation based on its strong TP inhibition and excellent modulation of 2′-deoxy-5-(trifluoromethyl)uridine (F3dThd) pharmacokinetics. As a result, TAS-102 (a combination of F3dThd and TPI) is currently in phase 1 clinical studies.
- Yano, Shingo,Kazuno, Hideki,Sato, Tsutomu,Suzuki, Norihiko,Emura, Tomohiro,Wierzba, Konstanty,Yamashita, Jun-Ichi,Tada, Yukio,Yamada, Yuji,Fukushima, Masakazu,Asao, Tetsuji
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p. 3443 - 3450
(2007/10/03)
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- A NOVEL AMINATION OF AROMATIC AND HETEROAROMATIC COMPOUNDS
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Vinyl azides act as NH2(+) equivalents in reaction with aromatic or heteroaromatic lithium derivatives thus providing a direct method for amination of such compounds.
- Hassner, Alfred,Munger, Paul,Belinka, A. Benjamin, Jr
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p. 699 - 702
(2007/10/02)
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