- METHOD FOR MANUFACTURING CYANOPYRIDINE COMPOUND
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PROBLEM TO BE SOLVED: To provide a novel method for manufacturing a cyanopyridine compound. SOLUTION: There is provided a method for manufacturing a cyanopyridine compound represented by the formula (1) by reacting a compound represented by the formula (4) and a cyanating agent. (4), (1), where R1 represents an alkyl group having 1 to 6 carbon atoms or a phenyl group which may have an alkyl group having 1 to 6 carbon atoms, the alkyl group having 1 to 6 carbon atoms may have a halogen atom, R2, R3 and R4 represent each independently a hydrogen atom or an alkyl group having 1 to 6 carbon atoms which may have a halogen atom, X2 represents a halogen atom and n represents an integer of 0 to 2. COPYRIGHT: (C)2016,JPO&INPIT
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Paragraph 0025
(2016/12/26)
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- Synthesis and biological evaluation of triazolothienopyrimidine derivatives as novel HIV-1 replication inhibitors
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We identified a novel class of triazolothienopyrimidine (TTPM) compounds as potent HIV-1 replication inhibitors during a high-throughput screening campaign that evaluated more than 200,000 compounds using a cell-based full replication assay. Herein, we report the optimization of the antiviral activity in a cell-based assay system leading to the discovery of aryl-substituted TTPM derivatives (38, 44, and 45), which exhibited significant inhibition of HIV-1 replication with acceptable safety margins. These novel and potent TTPMs could serve as leads for further development.
- Kim, Junwon,Kwon, Jeongjin,Lee, Doohyun,Jo, Suyeon,Park, Dong-Sik,Choi, Jihyun,Park, Eunjung,Hwang, Jong Yeon,Ko, Yoonae,Choi, Inhee,Ju, Moon Kyeong,Ahn, Jiye,Kim, Junghwan,Han, Sung-Jun,Kim, Tae-Hee,Cechetto, Jonathan,Nam, Jiyoun,Ahn, Sujin,Sommer, Peter,Liuzzi, Michel,No, Zaesung,Lee, Jinhwa
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p. 153 - 157
(2013/02/23)
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- Selective oxidation of sulfides to sulfoxides/sulfones by 30% hydrogen peroxide
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A selective and efficient procedure for the oxidation of various sulfides with sodium tungstate dihydrate with 30% hydrogen peroxide in the presence of trioctylmethylammonium dihydrogen phosphate, respectively, to the corresponding sulfoxides and sulfones is reported. The oxidation reaction is carried out at -5 to 0 °C in the presence of hydroxypropyl -β cyclodextrins for sulfoxides or at 50-60 °C for sulfones. The mild reaction conditions, easy workup, and good yields of the products are the major advantages of this method. Copyright Taylor and Francis Group, LLC 2012.
- He, Ying,Ma, Xiaoyun,Ji, Hai Feng,Zha, Xin Bing,Jiang, Hongliang,Lu, Ming
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experimental part
p. 822 - 830
(2012/08/07)
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