1033090-34-4Relevant articles and documents
[...] intermediate and its preparation and [...] preparation (by machine translation)
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Paragraph 0074-0077; 0081-0084; 0088-0091; 0095-0098, (2019/01/08)
The present invention relates to the field of drug synthesis, discloses a [...] key intermediate 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea and its preparation and [...] preparation. The music-cutting of the Buddhist intermediate, its pu
AZOLE-SUBSTITUTED PYRIDINE COMPOUND
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Paragraph 0659; 0660, (2019/01/08)
The present invention provides a compound represented by formula [I'| shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme, wherein the structure represented by formula [III] shown below represents any of the structures represented by formula group [IV] shown below, wherein R1 represents a hydrogen atom, a fluorine atom, methyl, etc.; R2, R3, and R4 each independently represent a hydrogen atom, a fluorine atom, or methyl; W represents a single bond, C1-3alkanediyl, or the formula -O-CH2CH2-; and ring A represents (a) substituted C4-6cycloalkyl, (b) substituted 4- to 6-membered saturated nitrogen-containing heterocyclyl, (c) substituted phenyl, (d) substituted pyridyl, (e) substituted 2,3-dihydrobenzofuran, (f) 4- to 6-membered saturated oxygen-containing heterocyclyl, etc.
Preparation method of lenvatinib
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Paragraph 0032; 0033; 0034; 0035; 0036; 0037, (2017/07/22)
The invention relates to a preparation method of lenvatinib, and concretely relates to a method for preparing lenvatinib through a one-step reaction formation reaction. The preparation method of lenvatinib has the advantages of small amount of generated impurities difficult to remove, easy post-treatment, convenient quality control in the bulk drug production process, and provision of convenience for researches of subsequent preparations.
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1h- pyrazol-1-yl)ethoxy]-6-methylphenyl}-n-(2,2-difluoropropyl)-5, 7-dihydro-6h-pyrrolo[3,4-d]pyrimidine-6-carboxamide
Zehnder, Luke,Bennett, Michael,Meng, Jerry,Huang, Buwen,Ninkovic, Sacha,Wang, Fen,Braganza, John,Tatlock, John,Jewell, Tanya,Zhou, Joe Zhongxiang,Burke, Ben,Wang, Jeff,Maegley, Karen,Mehta, Pramod P.,Yin, Min-Jean,Gajiwala, Ketan S.,Hickey, Michael J.,Yamazaki, Shinji,Smith, Evan,Kang, Ping,Sistla, Anand,Dovalsantos, Elena,Gehring, Michael R.,Kania, Robert,Wythes, Martin,Kung, Pei-Pei
experimental part, p. 3368 - 3385 (2011/06/27)
Figure Presented. A novel class of heat shock protein 90 (Hsp90) inhibitors was discovered by high-throughput screening and was subsequently optimized using a combination of structure-based design, parallel synthesis, and the application of medicinal chemistry principles. Through this process, the biochemical and cell-based potency of the original HTS lead were substantially improved along with the corresponding metabolic stability properties. These efforts culminated with the identification of a development candidate (compound 42) which displayed desired PK/PD relationships, significant efficacy in a melanoma A2058 xenograft tumor model, and attractive DMPK profiles.
Azide monoliths as convenient flow reactors for efficient Curtius rearrangement reactions
Baumann, Marcus,Baxendale, Ian R.,Ley, Steven V.,Nikbin, Nikzad,Smith, Christopher D.
experimental part, p. 1587 - 1593 (2008/10/09)
The preparation and use of an azide-containing monolithic reactor is described for use in a flow chemistry device and in particular for conducting Curtius rearrangement reactions via acid chloride inputs. The Royal Society of Chemistry 2008.