- 3,5-DISUBSTITUTED PYRAZOLES USEFUL AS CHECKPOINT KINASE 1 (CHK1) INHIBITORS, AND THEIR PREPARATIONS AND APPLICATIONS
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Potent inhibitors of Chk1 have the structure formula (I) below. Pharmaceutical compositions comprising the Chk1 inhibitors, uses thereof and their preparation process.
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Paragraph 000147
(2018/02/28)
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- Transition metal-free protodecarboxylation of electron rich aromatic acids under mild conditions
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A mild and practical method for the transition metal-free protodecarboxylation of aromatic acids using readily available and safe sodium persulfate as initiator was described. This environment-friendly decarboxylation approach was performed at 60 °C in ethanol and could easily scale up to the gram level with a good yield. In Particular, the tandem reactions of decarboxylation and halogenation were achieved by the addition of the corresponding halogenating reagents to the reaction system.
- Fang, Jingxian,Wang, Dangui,Deng, Guo-Jun,Gong, Hang
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supporting information
p. 4503 - 4506
(2017/10/30)
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- Rh-Catalyzed Synthesis of Coumarin Derivatives from Phenolic Acetates and Acrylates via C-H Bond Activation
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An efficient annulation strategy involving the reaction of phenolic acetates with acrylates in the presence of [Rh2(OAc)4] as catalyst and formic acid as reducing agent, leading to the high yield synthesis of coumarin derivatives, has been developed. The addition of NaOAc as a base increased the yield of the products. The reaction is quite successful for both electron-rich as well as electron-deficient phenolic acetates, affording coumarins with excellent regioselectivity, and proceeds via C-H bond activation proven by deuterium incorporation studies.
- Gadakh, Sunita K.,Dey, Soumen,Sudalai, Arumugam
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p. 11544 - 11550
(2015/12/04)
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- New approach for the construction of the coumarin frame and application in the total synthesis of natural products
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A new synthetic approach is described for building the coumarin scaffold through the Lewis acid-promoted cyclization of novel aryl 3-(dimethylamino)prop- 2-enoates 2a - 2f. The latter precursors were prepared via aminomethylenation of the corresponding aryl acetates 4a - 4f with the Bredereck reagent. This approach was used for the synthesis of biologically active natural compounds 1a - 1f, through a three-step procedure starting from the corresponding phenols.
- Jerezano, Alberto,Jimenez, Fabiola,Del Carmen Cruz, Maria,Montiel, Luisa E.,Delgado, Francisco,Tamariz, Joaquin
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experimental part
p. 185 - 198
(2011/04/17)
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- Isolation and synthesis of flavonols and comparison of their antioxidant activity
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Phytochemical investigation of the leaves of Astragalus beckari yielded four flavonol aglycones, namely kaempferol, quercetin, 5-deoxy kaempferol and fisitin. These isolated compounds were then synthesised in the laboratory using the Algar-Flyn-Oyamad reaction. Antioxidant activity of both the isolated and synthesised flavonoids was compared using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay method. The isolated flavonoids were found to be more active.
- Hasan, Aurangzeb,Sadiq,Abbas,Mughal,Khan, Khalid M.,Ali, Muhammad
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experimental part
p. 995 - 1003
(2010/09/05)
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- An aryne route to cytosporone B and phomopsin C
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The octaketide cytosporone B has been synthesized in six steps using 1,3,5-trihydroxybenzene as a starting material via aryne insertion reaction into a carbon-carbon σ-bond.
- Yoshida, Hiroto,Morishita, Takami,Ohshita, Joji
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scheme or table
p. 508 - 509
(2010/08/22)
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- Polymer-supported gadolinium triflate as a convenient and efficient Lewis acid catalyst for acetylation of alcohols and phenols
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A polymer-supported gadolinium triflate (CMPS-IM-Gd) catalyst was prepared from chloromethyl polystyrene (CMPS) resin using a simple and convenient procedure. This polymeric catalyst was used as an efficient Lewis acid catalyst for the acetylation of various alcohols and phenols with acetic anhydride, affording high yields under mild conditions. The reaction was completed in a short period of time with small amounts of the catalyst. The catalyst was reused over 10 times without any significant loss of its catalytic activity.
- Yoon, Hyo-Jin,Lee, Sang-Myung,Kim, Jong-Ho,Cho, Hong-Jun,Choi, Jung-Woo,Lee, Sang-Hyeup,Lee, Yoon-Sik
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p. 3165 - 3171
(2008/09/20)
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- Enantioselective synthesis of a fluorinated analogue of the orsellinic acid-type twelve-membered lactone lasiodiplodin
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The chemoenzymatic synthesis of the racemate and the one enantiomer of the fluorinated analogue 8 of the natural cyclooxygenase inhibitor lasiodiplodin is decribed. A lipase-mediated deracemization of the fluorohydrin 18 provided the chiral, nonracemic building block for the enantioselective synthesis of the title compound. The key step was the formation of the 12-membered lactene by a ring-closing metathesis.
- Runge,Haufe
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p. 8737 - 8742
(2007/10/03)
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- Chlorosulfination with Thionyl Chloride of Aromatic Methyl Ethers Containing Other Functional Groups
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Further studies on the direct chlorosulfination with thionyl chloride of aroamtic methyl ethers are described.In some cases (e.g. 1,6-dimethoxynaphthalene, 1,2,4-trimethoxybenzene, ethyl 3,5- and 3,7-dimethoxy-2-naphthoate, 3,5-dimethoxyphenyl benzoate) g
- Bell, Kevin H.,McCaffery, Leslie F.
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p. 1213 - 1224
(2007/10/02)
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