- nepal reaches Neeb process and intermediates for the synthesis of (by machine translation)
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The invention discloses a method for synthesizing nepal reaches Neeb and intermediates thereof, the synthesis method comprises: under acidic conditions, the compound of formula (II) reaction of a compound of the formula (I) compound of formula (III); compound (III) of the detached with acid uncle Ding Zhiji carbonate, adding alkali reaction of the compound of formula (V); the compound of formula (V) reaction with chloroacetic acid derivatives of formula (VI) the activation of the compound, then the reaction-methyl piperazine N, obtain nepal reaches Neeb. The present invention provides a mild reaction conditions of a new method for synthesizing nepal reaches Neeb, the invention also provides synthetic intermediates nepal reaches Neeb. (by machine translation)
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- Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties
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Nintedanib is a novel triple angiokinase inhibitor that inhibits three growth factors simultaneously. Deuterated derivatives of nintedanib at certain metabolically active sites were prepared and evaluated in vitro and in vivo. In particular, deuterated compound SKLB-C2202 had significantly improved pharmacokinetic properties compared with nintedanib. These efforts lay the foundation for further investigating the druggability of SKLB-C2202. Deuterated derivatives of nintedanib at certain metabolically active sites were prepared and evaluated in vitro and in vivo. Deuterated compound SKLB-C2202 had significantly improved pharmacokinetic properties compared with nintedanib. Further research is underway.
- Xu, Ruixue,Zhan, Miao,Peng, Lingling,Pang, Xuehai,Yang, Jun,Zhang, Tao,Jiang, Hongxia,Zhao, Lifeng,Chen, Yuanwei
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p. 308 - 312
(2015/06/25)
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- INDOLINONE DERIVATIVES AND PROCESS FOR THEIR MANUFACTURE
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The present invention relates to specific indolinone derivatives, namely the compounds of formula, in which R1 represents an hydrogen atom or a group, and R2 and R3 each represent an hydrogen atom or R2 and R3 taken together represent a group, with the proviso that when R1 represents an hydrogen atom R2 and R3 taken together represent a group, and to a process for their manufacture.
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Page/Page column 17-18; 3; 13
(2009/07/17)
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- PROCESS FOR THE MANUFACTURE OF AN INDOLINONE DERIVATIVE
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The present invention relates to a process for the manufacture of a specific indolinone derivative and a pharmaceutically acceptable salt thereof, namely 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone and its monoethanesulfonate, to new manufacturing steps and to new intermediates of this process.
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Page/Page column 4; 19
(2009/07/17)
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