934-27-0Relevant academic research and scientific papers
Some Observations on the Brunner Reaction
Wolff, Jens,Taddei, Maurizio
, p. 4267 - 4272 (1986)
Elucidation of the stereochemical course of the Brunner reaction is described.A slight modification in the procedure gives better yields and seems very promising for a more general application of this reaction.
Decarboxylative Borylation of mCPBA-Activated Aliphatic Acids
Wei, Dian,Liu, Tu-Ming,Zhou, Bo,Han, Bing
supporting information, p. 234 - 238 (2020/01/02)
A decarboxylative borylation of aliphatic acids for the synthesis of a variety of alkylboronates has been developed by mixing m-chloroperoxybenzoic acid (mCPBA)-activated fatty acids with bis(catecholato)diboron in N,N-dimethylformamide (DMF) at room temperature. A radical chain process is involved in the reaction which initiates from the B-B bond homolysis followed by the radical transfer from the boron atom to the carbon atom with subsequent decarboxylation and borylation.
Synthesis and biological evaluation of new berberine derivatives as cancer immunotherapy agents through targeting IDO1
Wang, Yan-Xiang,Pang, Wei-Qiang,Zeng, Qing-Xuan,Deng, Zhe-Song,Fan, Tian-Yun,Jiang, Jian-Dong,Deng, Hong-Bin,Song, Dan-Qing
, p. 1858 - 1868 (2017/11/17)
To discover small-molecule cancer immunotherapy candidates through targeting Indoleamine 2,3-dioxygenase 1 (IDO1), twenty–five new berberine (BBR) derivatives defined with substituents on position 3 or 9 were synthesized and examined for repression of IFN-γ-induced IDO1 promoter activities. Structure–activity relationship (SAR) indicated that large volume groups at the 9-position might be beneficial for potency. Among them, compounds 2f, 2i, 2n, 2o and 8b exhibited increased activities, with inhibition rate of 71–90% compared with BBR. Their effects on IDO1 expression were further confirmed by protein level as well. Furthermore, compounds 2i and 2n exhibited anticancer activity by enhancing the specific lysis of NK cells to A549 through IDO1, but not cytotoxicity. Preliminary mechanism revealed that both of them inhibited IFN-γ-induced IDO1 expression through activating AMPK and subsequent inhibition of STAT1 phosphorylation. Therefore, compounds 2i and 2n have been selected as IDO1 modulators for small-molecule cancer immunotherapy for next investigation.
NOVEL COMPOUND, RADIATION-SENSITIVE COMPOSITION, CURED FILM AND METHOD FOR FORMING THE SAME
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Paragraph 0168; 0169; 0175; 0176, (2018/05/03)
The invention relates to a novel compound, a radioactive ray sensitivity composition, a solidified film and a forming method thereof. The invention aims to provide a compound, which has a high radiation susceptibility, good dissolvability in a radiation sensitivity composition and good transparency of solidified film when the compound is used as a photo polymerized initiator. A radiation sensitivity compound can obtain the solidified film with good transparency and surface hardness. The invention is a compound expressed in the following formula (1), where R4 is alicyclic alkyl with one part of or the whole hydrogen atoms being replaced by alkyl with 1-12 carbon atoms. The invention is the radiation sensitivity composition having the compound (A) as the photo polymerized initiator and the polymerized compound (B) having ethylene unsaturated double bonds. The radiation sensitivity composition preferably includes alkali soluble resin (C).
Palladium-Catalyzed Alkoxycarbonylation of Unactivated Secondary Alkyl Bromides at Low Pressure
Sargent, Brendon T.,Alexanian, Erik J.
supporting information, p. 7520 - 7523 (2016/07/06)
Catalytic carbonylations of organohalides are important C-C bond formations in chemical synthesis. Carbonylations of unactivated alkyl halides remain a challenge and currently require the use of alkyl iodides under harsh conditions and high pressures of CO. Herein we report a palladium-catalyzed alkoxycarbonylation of secondary alkyl bromides that proceeds at low pressure (2 atm CO) under mild conditions. Preliminary mechanistic studies are consistent with a hybrid organometallic-radical process. These reactions efficiently deliver esters from unactivated alkyl bromides across a diverse range of substrates and represent the first catalytic carbonylations of alkyl bromides with carbon monoxide.
ORGANIC COMPOUNDS WITH A WOODY-PEPPERY ODOUR
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Page/Page column 12, (2016/04/20)
(Z)-Configured 5-substituted 5,6-dimethylhepta-3,6-dien-2-one possessing very characteristic dark woody odour with typical agarwood-like spicy peppery connotation.
Palladium-catalyzed double activation and arylation of 2° and 3° C(sp3)-H bonds of the norbornane system: Formation of a C-C bond at the bridgehead carbon and bridgehead quaternary stereocenter
Parella, Ramarao,Babu, Srinivasarao Arulananda
supporting information, p. 1395 - 1402 (2014/06/23)
Pd-catalyzed activation and direct arylation of both 2° and the bridgehead 3° (sp3) C-H bonds and an unprecedented C-C bond formation at the bridgehead carbon of the norbornane system are reported. The assembly of bridgehead-substituted norbornane frameworks having contiguous stereocenters was accomplished. X-ray crystal structure analysis of representative molecules unambiguously established the stereochemistry.
Hypervalent iodine catalyzed hofmann rearrangement of carboxamides using oxone as terminal oxidant
Yoshimura, Akira,Middleton, Kyle R.,Luedtke, Matthew W.,Zhu, Chenjie,Zhdankin, Viktor V.
, p. 11399 - 11404 (2013/02/23)
Hofmann rearrangement of carboxamides to carbamates using Oxone as an oxidant can be efficiently catalyzed by iodobenzene. This reaction involves hypervalent iodine species generated in situ from catalytic amount of PhI and Oxone in the presence of 1,1,1,3,3,3-hexafluoroisopropanol (HFIP) in aqueous methanol solutions. Under these conditions, Hofmann rearrangement of various carboxamides affords corresponding carbamates in high yields.
POTASSIUM CHANNEL MODULATORS
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Page/Page column 51, (2010/12/26)
Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, X, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described
SUBSTITUTED ARYL PYRIMIDINONES
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Page/Page column 47, (2009/10/09)
Substituted aryl pyrimidinones are provided, of the Formula (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
