- δ-Selective functionalization of alkanols enabled by visible-light-induced ligand-to-metal charge transfer
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We demonstrate the application of ligand-to-metal charge transfer (LMCT) excitation to the direct catalytic generation of energetically challenging alkoxy radicals from alcohols through a coordination-LMCT-homolysis process with an abundant and inexpensive cerium salt as the catalyst. This catalytic manifold provides a simple and efficient way to utilize the characteristic reactivity and selectivity of transient alkoxy radicals for δ-selective C-H bond functionalization. Under mild redox-neutral conditions without the need for prefunctionalization, this method provides a versatile platform to access molecular complexity from simple and abundant alcohols.
- Hu, Anhua,Guo, Jing-Jing,Pan, Hui,Tang, Haoming,Gao, Zhaobo,Zuo, Zhiwei
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Read Online
- A divergent synthetic pathway for pyrimidine-embedded medium-sized azacycles through an N-quaternizing strategy
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Medium-sized heterocycles have recently received significant attention because of their potential roles as modulators of protein-protein interactions, but their molecular diversity and synthetic availability are still inadequate to meet the demand. To address these issues, we developed a new divergent synthetic pathway for skeletally distinct pyrimidine-containing medium-sized azacycles. We introduced N-quaternized pyrimidine-containing polyheterocycles as novel key intermediates for diversity-generating reactions via selective bond cleavages or migrations and prepared 14 discrete core skeletons in an efficient manner. The skeletal diversity of the resulting molecular frameworks was confirmed by chemoinformatic analysis.
- Choi, Yoona,Kim, Heejun,Park, Seung Bum
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p. 569 - 575
(2019/01/10)
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- HERBICIDAL BENZOXAZINONES
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The present invention provides benzoxazinones of formula I wherein R1 is hydrogen or halogen; R2 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, C3/
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Page/Page column 87; 88
(2012/04/17)
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- Substituted Pyrazalones
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The invention is related to compounds of formula (I) as antagonists of the TGFβ family type I receptors, Alk5 and/or AIk 4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such a
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Page/Page column 31
(2010/04/23)
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- Ruthenium tetroxide oxidation of N,N'-Diboc hexahydropyridazines
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The ruthenium tetroxide (RuO4) oxidation of the 3-substituted N,N'-diBochexahydropyridazines gave the 6-oxohexahydropyridazines in good to high yields, whereas the oxidation of the unsubstituted ones also gave the 3,6-dioxo derivatives. The 3,6
- Kaname, Mamoru,Yoshifuji, Shigeyuki,Sashida, Haruki
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experimental part
p. 647 - 658
(2009/12/26)
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- Development of cyclic hydrazine and hydrazide type organocatalyst-mechanistic aspects of cyclic hydrazine/hydrazide-catalyzed diels-alder reactions
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Some hydrazines and hydrazides were prepared and screened for their catalytic efficiencies in Diels-Alder reactions. 1H-NMR studies and ab initio calculations revealed that catalytic efficiencies of these catalysts are greatly dependent on the release of the catalysts from the Diels-Alder adducts.
- Suzuki, Ichiro,Hirata, Ai,Takeda, Kei
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scheme or table
p. 851 - 863
(2009/12/01)
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- Biginelli reactions catalyzed by hydrazine type organocatalyst
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Pyrazolidine dihydrochloride can be used in the acceleration of Biginelli reactions between urea, ethyl acetoacetate and various aldehydes to provide DHPMs in good to excellent yields.
- Suzuki, Ichiro,Iwata, Yukari,Takeda, Kei
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p. 3238 - 3241
(2008/09/21)
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- Synthesis, biological evaluation and structural determination of β-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors
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Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of β-aminoacyl-containing cyclic hydrazine derivatives were synthesized and evaluated as DPP-IV inhibitors. One member of this series, (R)-3-amino-1-(2-benzoyl-1,2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)but an-1-one (10f), showed potent in vitro activity, good selectivity and in vivo efficacy in mouse models. Also, the binding mode of compound 10f was determined by X-ray crystallography.
- Ahn, Jin Hee,Shin, Mi Sik,Jun, Mi Ae,Jung, Sun Ho,Kang, Seung Kyu,Kim, Kwang Rok,Rhee, Sang Dal,Kang, Nam Sook,Kim, Sun Young,Sohn, Sang-Kwon,Kim, Sung Gyu,Jin, Mi Sun,Lee, Jie Oh,Cheon, Hyae Gyeong,Kim, Sung Soo
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p. 2622 - 2628
(2008/02/11)
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- Composition for dyeing keratin fibers, comprising at least one diamino-N,N-dihydropyrazolone derivative, at least one coupler, and at least one heterocyclic direct dye
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Disclose herein is a composition for dyeing keratin fibers, for example, human keratin fibers such as the hair, comprising at least one oxidation base chosen from diamino-N,N-dihydropyrazolones and addition salts thereof, at least one coupler, and at least one heterocyclic direct dye. Also disclosed herein is a method for dyeing keratin fibers comprising applying a composition of the present disclosure to the keratin fibers. The compositions and methods of the present disclosure may make it possible to obtain fast coloration of keratin fibers that is resistant to light and/or to washing.
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Page/Page column 25; 26
(2008/06/13)
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- Composition for dyeing keratin fibers, comprising at least one diamino-N,N-dihydropyrazolone derivative, at least one coupler and at least one associative polyurethane polymer
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The present disclosure relates to a composition for dyeing keratin fibers, for example, human keratin fibers such as the hair, comprising at least one oxidation base chosen from diamino-N,N-dihydropyrazolone compounds and addition salts thereof, at least one coupler and at least one associative polyurethane polymer, and also to a dyeing process and kit using such a composition. The present disclosure makes it possible, for instance, to obtain fast coloration of keratin fibers that is resistant to light and to washing.
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Page/Page column 23-24
(2008/06/13)
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- Composition for dyeing keratin fibers, comprising at least one diamino-N,N-dihydropyrazolone derivative, at least one coupler, and at least one surfactant
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Disclosed herein is a composition for dyeing keratin fibers, for example, human keratin fibers such as the hair, comprising at least one oxidation base chosen from diamino-N,N-dihydropyrazolones and the addition salts thereof, at least one coupler, and at least one surfactant chosen from (C8-C30)alkyl ether carboxylic acids and salts thereof, (C12-C30)alkyl polyglucosides, monoglycerolated surfactants, and polyglycerolated surfactants. Also disclosed herein is a method for dyeing keratin fibers comprising applying a composition in accordance with the present disclosure to the keratin fibers. The compositions and methods of the present disclosure may makes it possible to obtain fast coloration of keratin fibers that is resistant to light and/or to washing.
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Page/Page column 22
(2008/06/13)
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- Composition for dyeing keratin fibers, comprising a diamino-N,N-dihydropyrazolone compound, a coupler, and a polyol
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The present disclosure relates to a composition for dyeing keratin fibers, for instance human keratin fibers such as the hair, comprising at least one oxidation base chosen from diamino-N,N-dihydropyrazolone compounds and addition salts thereof, at least one coupler and at least one C4-C30 polyol. The present disclosure also relates to the dyeing process and kit using the composition as presently disclosed. Use of the present disclosure makes it, for example, possible to obtain fast coloration of keratin fibers that is resistant to light and to washing.
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Page/Page column 20-21
(2008/06/13)
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- NOVEL CATHEPSIN C INHIBITORS AND THEIR USE
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The invention is directed to novel cathepsin C inhibitors and their use in the treatment of diseases mediated by the cathepsin C enzyme. Specifically, the invention is directed to compounds according to Formula (I): wherein X and n are defined below, and
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Page/Page column 22
(2010/11/23)
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- Composition for dyeing keratinous fibers comprising at least one diamino-N,N-dihydropyrazolone derivative
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Disclosed herein are a composition for dyeing keratinous fibers, for example, human keratinous fibers such as hair, comprising at least one oxidation base chosen from diamino-N,N-dihydropyrazolone derivative and a method using the composition. Further disclosed herein are amino-N,N-dihydropyrazolone derivatives and the addition salts thereof and diamino-N,N-dihydropyrazolone derivatives and the addition salts thereof, as well as the methods for preparing these compounds.
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Page/Page column 20
(2008/06/13)
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- Synthesis, molecular modeling and biological evaluation of aza-proline and aza-pipecolic derivatives as FKBP12 ligands and their in vivo neuroprotective effects
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Nonimmunosuppressant ligands, exemplified by GPI 1046 (1), for the peptidyl-prolyl isomerase FKBP12 have been found to unexpectedly possess powerful neuroprotective and neuroregenerative effects in vitro and in vivo. We have extensively explored the thera
- Wilkinson, Douglas E.,Thomas IV, Bert E.,Limburg, David C.,Holmes, Agnes,Sauer, Hansjorg,Ross, Douglas T.,Soni, Raj,Chen, Yi,Guo, Hong,Howorth, Pamela,Valentine, Heather,Spicer, Dawn,Fuller, Mike,Steiner, Joseph P.,Hamilton, Gregory S.,Wu, Yong-Qian
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p. 4815 - 4825
(2007/10/03)
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