34782-60-0Relevant academic research and scientific papers
Synthesis of thiadiazoles and 1,2,4-triazoles derived from cyclopropane dicarboxylic acid
Sharba, A. Hussain K.,Al-Bayati, Rida H.,Rezki, Nadjet,Aouad, Mohammed R.
, p. 1153 - 1160 (2005)
New heterocyclic derivatives of cyclopropane dicarboxylic acid comprising thiadiazole and 1,2,4-triazole moieties are reported. Reaction of 1,1-cyclopropane dicarboxylic acid (1) with thiosemicarbazide and phosphorous oxychloride resulted in 1,1-bis (2-am
Studies of copper-bisoxazoline-catalyzed asymmetric cyclopropanation of 2,5-dimethyl-2,4-hexadiene
Itagaki, Makoto,Masumoto, Katsuhisa,Suenobu, Katsuhiro,Yamamoto, Yohsuke
, p. 245 - 250 (2006)
In the [bis{(4R)-(1-naphthyl)-5,5-dimethyloxazoline}/copper]-catalyzed asymmetric cyclopropanation of 2,5-dimethyl-2,4-hexadiene with tert-butyl diazoacetate, the effects of a counterion of the copper complex were studied. The[CuCl/bisoxazoline/ Ph3CPF6] catalyst was found to enhance both the catalytic efficiency and the stereoselectivity (the catalyst 0.2 mol %, yield 92%, trans/cis = 88/12, 96% ee for the trans product), compared to our previously reported CuOTf/bisoxazoline catalyst. The density functional calculations were performed to elucidate the effects of the counterion as well as the effects of the gem-dimethyl groups at the 5-position on the bisoxazoline ligand.
Catalytic Asymmetric Homologation of 4-Substituted Cyclohexanones with CF3CHN2: Enantioselective Synthesis of α-Trifluoromethyl Cycloheptanones
Li, Shu-Sen,Sun, Shuo,Wang, Jianbo
supporting information, (2021/12/27)
Introduction of the trifluoromethyl group (CF3) into organic molecules in an enantioselective manner has attracted significant attention, but still remains a challenging problem. We herein report a catalytic asymmetric trifluoromethylation of cyclic ketones via a ScIII/chiral bisoxazoline-catalyzed homologation reaction by employing 2,2,2-trifluorodiazoethane (CF3CHN2) as the CF3 source. This desymmetrization process is highly efficient and generates two chiral centers with excellent diastereoselectivity and enantioselectivity, affording chiral α-trifluoromethyl cyclic ketones in a straightforward manner.
Preparation method of cabozantinib defluorination impurity
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Paragraph 0019; 0031-0032, (2020/08/25)
The invention discloses a preparation method of a cabozantinib defluorination impurity. The method comprises the following steps: preparing an intermediate 1, preparing 4-chloro-6, 7-dimethoxyquinoline, preparing an intermediate 2, and removing fluorine i
Catalytic Desymmetric Cycloaddition of Diaziridines with Metalloenolcarbenes: The Role of Donor–Acceptor Cyclopropenes
Zheng, Haifeng,Doyle, Michael P.
supporting information, p. 12502 - 12506 (2019/08/16)
A chiral copper(I) complex catalyzes reactions of symmetric diaziridines with enol diazo compounds, which react through N?N bond ring opening in a formal [3+3] cycloaddition to form four chiral centers with high stereocontrol. A broad spectrum of bridged dinitrogen heterocycles were obtained in high yields and excellent diastereo- and enantioselectivities from γ-substituted enol diazoacetates, while their geometrical isomers gave different enantioselectivities. Donor–acceptor cyclopropenes formed from the geometrical isomers of the γ-substituted enol diazoacetates underwent catalytic ring opening to give only the Z isomer of the metalloenolcarbene intermediate, provided excellent yields and selectivities for the 1,5-diazabicyclo[n.3.1]non-2-ene derivatives.
Design and synthesis of malonamide derivatives as antibiotics against methicillin-resistant staphylococcus aureus
Su, Jung-Chen,Huang, Yu-Ting,Chen, Chang-Shi,Chiu, Hao-Chieh,Shiau, Chung-Wai
, (2018/01/03)
Methicillin-resistant Staphylococcus aureus (MRSA) is a serious threat to humans. Most existing antimicrobial drugs, including the β-lactam and quinoxiline classes, are not effective against MRSA. In this study, we synthesized 24 derivatives of malonamide, a new class of antibacterial agents and potentiators of classic antimicrobials. A derivative that increases bacterial killing and biofilm eradication with low cell toxicity was created.
A deuterium generation of card abundantly for nepal derivatives, preparation method thereof, and wherein the intermediate application
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Paragraph 0146; 0147, (2018/03/26)
The invention belongs to the technical field of pharmaceutical chemistry, and discloses a deuterated cabozantinib derivative, a preparation method and an application thereof, and an intermediate of the deuterated cabozantinib derivative. The deuterated ca
Cu-Catalyzed Enantioselective Ring Opening of Cyclic Diaryliodoniums toward the Synthesis of Chiral Diarylmethanes
Li, Bin,Chao, Zengyin,Li, Chunyu,Gu, Zhenhua
supporting information, p. 9400 - 9403 (2018/07/30)
A Cu-catalyzed enantioselective desymmetrizing ring-opening reaction of six-membered cyclic diaryliodonium salts with carboxylic acids or thioacids is reported for the facile access to chiral diarylmethanes. A Cu/[cyclopropyl bis(oxazoline)] catalyst well
Novel anti-PD-L1 compound, application thereof and composition containing same
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Paragraph 0076; 0078-0080, (2019/01/16)
The invention discloses a novel anti-PD-L1 compound, application thereof and a composition containing the same. The compound is a compound as shown in the formula I or medically acceptable salt or hydrate or solvate or metabolite or stereisomer or tautome
SUBSTITUTED MALONAMIDES AND THEIR USE AS ANTIBACTERIAL DRUGS
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Page/Page column 19; 20, (2017/03/14)
Disclosed are a series of malonamide derivatives having a chemical structure(I), their synthesis, and evaluation of their bioactivities against bacterial cell, bacterial-infected C.elegans and mice.
