- HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
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The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.
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Paragraph 0066-0067
(2021/02/25)
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- A Ba/Pd Catalytic System Enables Dehydrative Cross-Coupling and Excellent E-Selective Wittig Reactions
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A Ba/Pd cooperative catalysis system was developed to enable the dehydrative cross-coupling of allylic alcohols with P-ylides to occur directly and promote a subsequent Wittig reaction in one pot. A variety of multisubstituted 1,4-dienes were isolated in good to excellent yields with broad P-ylides (stabilized by both ester and ketone carbonyl groups) and aldehyde (aliphatic and aromatic) substrates with excellent E selectivity.
- Xie, Peizhong,Fu, Weishan,Cai, Xinying,Sun, Zuolian,Wu, Ying,Li, Shuangshuang,Gao, Cuiqing,Yang, Xiaobo,Loh, Teck-Peng
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supporting information
p. 7055 - 7059
(2019/09/12)
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- Method for preparing cyclopropyl carbonyl methylene triphenyl phosphine
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The invention relates to a method for preparing cyclopropyl carbonyl methylene triphenyl phosphine. The method comprises the following steps: (1) enabling cyclopropyl methyl ketone to react with bromine so as to obtain cyclopropyl bromomethyl ketone; (2) enabling the cyclopropyl bromomethyl ketone to react with triphenyl phosphine so as to obtain brominized triphenyl phosphine cyclopropyl carbonylmethyl; and (3) enabling the brominized triphenyl phosphine cyclopropyl carbonyl methyl to react with sodium hydroxide, thereby obtaining cyclopropyl carbonyl methylene triphenyl phosphine. The content of a cyclopropyl carbonyl methylene triphenyl phosphine product prepared by using the method provided by the invention is up to 98.4% or above, the product quality is good, and the defect that a product prepared by using a conventional preparation method is low in content is overcome. In addition, the preparation method provided by the invention is simple to operate, simple in step, easy in product impurity separation and removal, and beneficial to large-scale industrial production.
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Paragraph 0019; 0027; 0034-0037; 0044-0047; 055-0056
(2019/09/14)
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- Tandem Wittig Reaction-Ring Contraction of Cyclobutanes: A Route to Functionalized Cyclopropanecarbaldehydes
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An original tandem reaction consisting of a Wittig reaction-ring contraction process between α-hydroxycyclobutanone and phosphonium ylides has been developed. Highly functionalized cyclopropanecarbaldehydes are obtained in good to high yield.
- Aitken, David J.,Caboni, Pierluigi,Cuccu, Federico,Frongia, Angelo,Luridiana, Alberto,Secci, Francesco,Serusi, Lorenzo
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supporting information
(2019/10/08)
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- PYRROLOTRIAZINE COMPOUNDS AS TAM INHIBITORS
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This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
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Paragraph 1301; 1302
(2017/10/13)
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- Synthesis of Polysubstituted Pyridines via a One-Pot Metal-Free Strategy
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An efficient strategy for the one-pot synthesis of polysubstituted pyridines via a cascade reaction from aldehydes, phosphorus ylides, and propargyl azide is reported. The reaction sequence involves a Wittig reaction, a Staudinger reaction, an aza-Wittig reaction, a 6π-3-azatriene electrocyclization, and a 1,3-H shift. This protocol provides quick access to the polysubstituted pyridines from readily available substrates in good to excellent yields.
- Wei, Hongbo,Li, Yun,Xiao, Ke,Cheng, Bin,Wang, Huifei,Hu, Lin,Zhai, Hongbin
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supporting information
p. 5974 - 5977
(2016/01/09)
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