33603-87-1Relevant articles and documents
Di-tert-Butyl Peroxide-Mediated Atom-Transfer Radical Addition of 2-Chlorodithiane to Aryl Alkynes under Mild Conditions
Lai, Junshan,Tian, Lixia,Liang, Yongping,Zhang, Yuan,Xie, Xingang,Fang, Bowen,Tang, Shouchu
, p. 14328 - 14331 (2015)
Atom transfer radical addition (ATRA) of 2-chlorodithiane onto aryl alkynes through the use of di-tert-butyl peroxide as an oxidant at room temperature directly affords a variety of synthetically valuable β-chloro-(Z)-vinyl dithianes in good yields with high regioselectivities and without the assistance of any transition metals. It provides an operationally simple pathway to access vinyl dithianes with controlled formation of a new C(sp2) - C bond and a C(sp2) - Cl bond.
Novel benzenesulfonamide-bearing pyrazoles and 1,2,4-thiadiazoles as selective carbonic anhydrase inhibitors
Kumar, Rajiv,Kumar, Amit,Ram, Sita,Angeli, Andrea,Bonardi, Alessandro,Nocentini, Alessio,Gratteri, Paola,Supuran, Claudiu T.,Sharma, Pawan K.
, (2021/10/05)
Two series comprising 20 novel benzenesulfonamides bearing thioureido-linked pyrazole 8 and amino-1,2,4-thiadiazole 10 were synthesized and assayed as human carbonic anhydrase (hCA) inhibitors against isoforms I and II as well as the tumor-associated isof
MTA-Cooperative PRMT5 Inhibitors
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Paragraph 0235-0236, (2021/03/19)
The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
Palladium-Catalyzed Allyl-Allyl Reductive Coupling of Allylamines or Allylic Alcohols with H2as Sole Reductant
Zhou, Xibing,Zhang, Guoying,Huang, Renbin,Huang, Hanmin
, p. 365 - 369 (2021/01/26)
Catalytic carbon-carbon bond formation building on reductive coupling is a powerful method for the preparation of organic compounds. The identification of environmentally benign reductants is key for establishing an efficient reductive coupling reaction. Herein an efficient strategy enabling H2 as the sole reductant for the palladium-catalyzed allyl-allyl reductive coupling reaction is described. A wide range of allylamines and allylic alcohols as well as allylic ethers proceed smoothly to deliver the C-C coupling products under 1 atm of H2. Kinetic studies suggested that the dinuclear palladium species was involved in the catalytic cycle.
Regiodivergent Synthesis of Bis(4-oxycoumarin)-based Dioxabicycles: Exploration of [4 + 4] (Heterocyclo)reversion/addition and 1,5-Hydrogen Shift Photochromism
Vyasamudri, Sameer,Yang, Ding-Yah
, (2020/04/20)
Two isomeric dioxabicyclic molecular skeletons were constructed by employing the concepts of divergent synthesis. A base-mediated and an acid-catalyzed pseudo-three-component reaction of two equivalents of 4-hydroxycoumarin and (Z)-3-chloro-3-phenylacryla
Superacid-promoted synthesis of quinoline derivatives
Klumpp, Douglas A.,Stentzel, Michael R.,Vuong, Hein
supporting information, (2020/01/24)
A series of vinylogous imines have been prepared from anilines and cinnamaldehydes. These substrates react in superacidic media to provide quinolines and related compounds. A mechanism for the conversion is proposed which involves the cyclization of dicationic superelectrophilic intermediates. Aromatization of the quinoline ring is thought to occur by superacid-promoted elimination of benzene.
Pendant Alkoxy Groups on N-Aryl Substitutions Drive the Efficiency of Imidazolylidene Catalysts for Homoenolate Annulation from Enal and Aldehyde
Kyan, Ryuji,Mase, Nobuyuki,Narumi, Tetsuo,Sato, Kohei
supporting information, p. 19031 - 19036 (2020/08/25)
Hydrogen-transfer in the tetrahedral intermediate generated from an imidazolylidene catalyst and α,β-unsaturated aldehyde forms a conjugated Breslow intermediate. This is a critical step affecting the efficiency of the NHC-catalyzed γ-butyrolactone formation via homoenolate addition to aryl aldehydes. A novel type of imidazolylidene catalyst with pendant alkoxy groups on the ortho-N-aryl groups is described. Catalyst of this sort facilitates the formation of the conjugated Breslow intermediate. Studies of the rate constants for homoenolate annulation affording γ-butyrolactones, reveal that introduction of the oxygen atoms in the appropriate position of the N-aryl substituents can increase the efficiency of imidazolylidene catalysts. Structural and mechanistic studies revealed that pendant alkoxy groups can be located close to the proton of the tetrahedral intermediate, thereby facilitating the proton transfer.
Β - chloro - α, β - unsaturated - 1, 3 - dithiane compound preparation method and application of
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, (2018/04/27)
The invention provides a beta-chloro-alpha, beta-nonsaturated-1,3-dithiane compound preparation method and use. The preparation method comprises that a solvent, 2-chloro-1,3-dithiane, an alkyne compound and iodine and/or di-tert-butyl peroxide are added into a reactor, the mixture undergoes a reaction at a certain temperature and the reaction product is separated and purified so that the corresponding beta-chloro-alpha, beta-nonsaturated-1,3-dithiane compound is obtained. The preparation method utilizes cheap and easily available raw materials and realizes high efficiency preparation of the beta-chloro-alpha, beta-nonsaturated-1,3-dithiane compound by simple mixing and stirring. The preparation method has the advantages of mild reaction conditions, high yield, environmental friendliness and atom economy. The beta-chloro-alpha, beta-nonsaturated-1,3-dithiane compound can be used for preparation of a plurality of useful compound skeletons and especially for preparation of pyrazole, acridine and phenyl hydrazone compounds, a beta-chloro-alpha, beta-nonsaturated aldehyde compound, a beta-carbonyl or alpha, beta-nonsaturated-1,3-dithiane compound and an allene compound.
Oxazolidinone compound containing piperazine hydrazone structure
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Paragraph 0153; 0154, (2017/09/02)
The invention discloses an oxazolidinone compound containing a piperazine hydrazone structure. The oxazolidinone compound comprises a compound shown as a general formula (I), or stereisomer thereof, or pharmaceutically-acceptable salt thereof, or solvate thereof or prodrug thereof, wherein R1 is hydrogen, fluorine, chlorine or trifluoromethyl, R2 is -NHCOCH3 or -OH, R3 is Ar which is C5-C10 aryl substituted by any 1-3 R4 and heteroaryl, and R4 is hydrogen, hydroxyl, halogen, nitro, amino, cyan, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkyl substituted by hydroxyl, amino or halogen, C1-C6 alkoxy substituted by hydroxyl, amino or halogen, amino substituted by mono- or bi-(C1-C6 alkyl), C1-C6 alkyl amido, free, salty, esterified and amidated hydroxyl, C1-C6 alkyl sulfinyl, C1-C6 alkyl sulfonyl, C1-C6 alkyl acyl and carbamoyl. The oxazolidinone compound can be used for preparing drug for treating microbial infection.
Ugi Reaction Followed by Intramolecular Diels–Alder Reaction and Elimination of HCl: One-Pot Approach to Arene-Fused Isoindolinones
Huang, Jianjun,Du, Xiaochen,Van Hecke, Kristof,Van der Eycken, Erik V.,Pereshivko, Olga P.,Peshkov, Vsevolod A.
supporting information, p. 4379 - 4388 (2017/08/23)
A one-pot procedure involving a four-component Ugi reaction followed by an intramolecular Diels–Alder reaction/HCl elimination cascade has been developed to provide rapid access to the isoindolinone framework in a diversity-oriented fashion. The scope of
