361-73-9Relevant academic research and scientific papers
2-oxadiazole-3-aminothiophene thieno-[2,3-b] pyridine derivative and preparing method and application thereof
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Paragraph 0069-0071; 0075-0077, (2017/09/01)
The invention belongs to the field of chemical pharmaceuticals, and particularly relates to a 2-oxadiazole-3-aminothiophene thieno-[2,3-b] pyridine derivative and a preparing method and application thereof. The structure of the 2-oxadiazole-3-aminothiophene thieno-[2,3-b] pyridine derivative is shown in the formula I. A compound of the 2-oxadiazole-3-aminothiophene thieno-[2,3-b] pyridine derivative has the good HCV inhibitory effect, and meanwhile shows the low cytotoxicity, and a new method is provided for development of an anti-HCV inhibitor. The general formula is defined in the description.
A new series of HCV inhibitors based on a 2-(thieno[2,3B]pyridin-2-yl)-1,3,4-oxadiazole scaffold
Zuo, Wei-Qiong,Wang, Ning-Yu,Zhu, Yong-Xia,Liu, Li,Xiao, Kun-Jie,Zhang, Li-Dan,Gao, Chao,Liu, Zhi-Hao,You, Xin-Yu,Shi, Yao-Jie,Peng, Cui-Ting,Ran, Kai,Tang, Hong,Yu, Luo-Ting
, p. 40277 - 40286 (2016/05/24)
A new series of HCV inhibitors based on a 2-(thieno[2,3-b]pyridin-2-yl)-1,3,4-oxadiazole scaffold was developed. Detailed SAR investigations revealed the HCV inhibitory activity was sensitive to the size of C5, the C6-fused ring, and the size and flexibility of C5′ cycloalkane, which led to the identification of several compounds with potent inhibitory activity against HCV genotype 1b replicon. The most potent compound 10d showed ~100-fold improvement in potency compared with compound 1, with an EC50 of 0.039 μM, but without obvious cytotoxicity in vitro.
Highly selective trifluoroacetic ester/ketone metathesis: An efficient approach to trifluoromethyl ketones and esters
Zhou, Yuhan,Yang, Dongmei,Luo, Gen,Zhao, Yilong,Luo, Yi,Xue, Na,Qu, Jingping
, p. 4668 - 4674 (2014/06/23)
A highly selective and atom efficient 'trifluoroacetic ester/ketone metathesis' has been sincerely witnessed. Enolizable alkyl (at least two non-hydrogen atoms) aryl ketones were found to react readily with ethyl trifluoroacetate under the promotion of NaH to afford trifluoroacetic ester/ketone exchange products, trifluoromethyl ketones (TFMKs), and aromatic acid esters, which were quite different from the general Claisen condensation products, 1,3-diketones. The outcome of the reaction between ketone and ethyl trifluoroacetate is strongly related to the structures of substrates, the steric congestion caused by alkyl group is in favor of the C-C bond cleavage. DFT investigation further disclosed that the metathesis reaction was a kinetically favored pathway. Using only a slight excess of cheap trifluoromethylation reagent, simple operation and mild conditions make it a practical method for preparation of TFMKs on large scale, as well as a new choice of converting aryl alkyl ketones to aromatic acid esters.
COMPOUNDS FOR THE TREATMENT OF HIV
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Page/Page column 275, (2013/03/26)
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
Metal and boron derivatives of fluorinated cyclic 1,3-dicarbonyl compounds
Sevenard, Dmitri V.,Khomutov, Oleg G.,Boltachova, Nadezhda S.,Filyakova, Vera I.,Vogel, Vera,Lork, Enno,Vyacheslav Ya. Sosnovskikh,Iaroshenko, Viktor O.,Roeschenthalerc, Gerd-Volker
experimental part, p. 541 - 550 (2009/09/07)
Starting from the corresponding cyclic 1,3-diketones or other precursors (cyclic ketones as well as lactones), several new salts and chelate complexes of fluorinated 1,3-dicarbonyls were obtained. Their preparative significance was demonstrated by straigh
COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEROF IN MEDICINE
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Page/Page column 30, (2009/01/24)
Compound of formula (I) and salts thereof are provided: wherein X, Y, Z, R1, R2 and R3 are as defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
