441784-82-3Relevant articles and documents
A novel class of phosphonate nucleosides. 9-[(1-phosphonomethoxycyclopropyl)methyl]guanine as a potent and selective anti-HBV agent
Choi, Jong-Ryoo,Cho, Dong-Gyu,Roh, Kee Y.,Hwang, Jae-Taeg,Ahn, Sinbyoung,Jang, Hyun S.,Cho, Woo-Young,Kim, Kyong W.,Cho, Young-Gyo,Kim, Jeongmin,Kim, Yong-Zu
, p. 2864 - 2869 (2004)
9-[1-(Phosphonomethoxycyclopropyl)methyl]guanine (PMCG, 1), representative of a novel class of phosphonate nucleosides, blocks HBV replication with excellent potency (EC50 = 0.5 μM) in a primary culture of HepG2 2.2.15 cells. It exhibits no sig
SUBSTITUTED IMIDAZOLECARBOXYLATE DERIVATIVES AND THE USE THEREOF
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Paragraph 0311; 0314-0315, (2020/12/08)
A compound is shown in formula (I). The derivatives of the compound include a stereoisomer, a pharmaceutically acceptable salt, a solvate, a prodrug, a metabolite, a deuterated derivative. The compound is a structurally novel substituted imidazole formate derivative. Substituted imidazole formate derivatives are used in preparing a drug with sedative, hypnotic and/or anesthetic effects, as well as a drug that can control the state of epilepsy. The compound has a good inhibitory effect on the central nervous system, and provides a new option for clinical screening of and/or preparation of a drug with sedative, hypnotic and/or anesthetic effects and controlling the state of epilepsy.
Method for preparing Besifovir
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Paragraph 0050; 0051, (2019/01/06)
The invention relates to a method for preparing P-[[[1-[(2-amino-9H-purine-9-yl) methyl] cyclopropyl] oxy] methyl]-phosphoric acid (Besifovir). The method comprises the following steps: 1) enabling acompound of formula (1) as shown in the specification to react with tertiary butyl diphenylchlorosilane so as to prepare a compound of formula (2) as shown in the specification; 2) enabling the compound of formula (2) to react with ethyl magnesium bromide so as to prepare a compound of formula (3) as shown in the specification; 3) enabling the compound of the formula (3) to react with p-toluenesulfonyl oxymethyldiethoxyphosphine under a condition that tertiary butanol lithium is adopted as an alkali so as to prepare a compound of formula (23) as shown in the specification; 4) carrying out ammonium fluoride hydrolysis on the compound of formula (23) so as to prepare a compound of formula (24) as shown in the specification; 5) enabling the compound of formula (24) to react with a compound offormula (28) as shown in the specification so as to prepare a compound as a solid of formula (22) as shown in the specification; 6) carrying out reduction dechloridation on the compound of formula (22) as shown in the specification under a condition of a catalyst and a hydrogen supplier so as to prepare a compound as a solid of formula (25) as shown in the specification; 7) carrying out trimethylbromide silane hydrolysis on the compound of formula (25), so as to obtain Besifovir as shown in the specification. The method is cheap in raw material and intermediate material, easy in raw materialand intermediate material obtaining, low in cost, high in yield, gentle in condition and good in security.
NON-FUSED TRICYCLIC COMPOUNDS
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Paragraph 00638, (2018/11/26)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Two-step conversion of carboxylic esters into distally fluorinated ketones: Via ring cleavage of cyclopropanol intermediates: Application of sulfinate salts as fluoroalkylating reagents
Konik, Yulia A.,Kudrjashova, Marina,Konrad, Nele,Kaabel, Sandra,J?rving, Ivar,Lopp, Margus,Kananovich, Dzmitry G.
supporting information, p. 4635 - 4643 (2017/07/10)
Tertiary cyclopropanols easily available from carboxylic esters have been used in the synthesis of distally fluorinated ketones. Cyclopropane ring cleavage reactions in methanol with aqueous tert-butyl hydroperoxide in the presence of a copper(ii) acetate catalyst and sodium triflinate (Langlois reagent) afford β-trifluoromethyl ketones in 16-74% isolated yields. Sodium triflinate serves as a precursor of reactive trifluoromethyl copper species, enabling ring-opening trifluoromethylation, as evidenced by mechanistic studies. We also demonstrate here that other sulfinate salts, such as sodium 1,1-difluoroethanesulfinate, sodium 2-(4-bromophenyl)-1,1-difluoroethanesulfinate and sodium 1-(trifluoromethyl)cyclopropanesulfinate, can be used as fluoroalkylation reagents, resulting in the corresponding fluorinated ketones.
Simple access to β-trifluoromethyl-substituted ketones via copper-catalyzed ring-opening trifluoromethylation of substituted cyclopropanols
Kananovich, Dzmitry G.,Konik, Yulia A.,Zubrytski, Dzmitry M.,J?rving, Ivar,Lopp, Margus
supporting information, p. 8349 - 8352 (2015/05/13)
Tertiary cyclopropanols react rapidly with Togni reagent in methanol at room temperature in the presence of catalytic amounts (3 mol%) of CuCl affording β-trifluoromethyl ketones in 65-73% isolated yields. Ring opening in 1,2-dialkylsubstituted cyclopropanols gives a mixture of isomeric β-trifluoromethyl ketones in about 50% combined yield.
NUCLEOSIDE PHOSPHONATE DERIVATIVES USEFUL IN THE TREATMENT OF HIV INFECTIONS
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Page/Page column 38-39, (2008/06/13)
The present invention relates to a method of treating HIV infections by administering a nucleoside phosphonate derivative represented by formula (I).
