1160293-22-0

Usage

Uses

Used in Pharmaceutical Industry:
2,3-Dihydro-3-(MethoxyphenylMethylene)-2-oxo-1H-indole-6-carboxylic acid Methyl ester is used as an intermediate for the synthesis of (E)-Intedanib (I666670), which is a pharmaceutical compound with potential applications in the treatment of various types of cancer.
Used in the Preparation of Deuterated Derivatives:
In the field of drug development, 2,3-Dihydro-3-(MethoxyphenylMethylene)-2-oxo-1H-indole-6-carboxylic acid Methyl ester is used as a reactant in the preparation of deuterated derivatives of Nintedanib (N478290). Nintedanib is an angiokinase inhibitor with antitumor activity, and the deuterated derivatives may offer improved pharmacokinetic properties and enhanced therapeutic effects.
Overall, 2,3-Dihydro-3-(MethoxyphenylMethylene)-2-oxo-1H-indole-6-carboxylic acid Methyl ester plays a crucial role in the pharmaceutical industry, particularly in the development of antitumor drugs and the synthesis of novel drug candidates with improved therapeutic potential.

Upstream product

• 1160293-24-2 N-chloroacetyl-3-[methoxy(phenyl)methylene]-2-oxoindoline-6-carboxylic acid methyl ester 
• 334952-07-7 4-methoxycarbonylmethyl-3-nitrobenzoic acid methyl ester 
• 14192-26-8 2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester 
• 121-92-6 3-nitrobenzoic acid 
• 618-95-1 methyl 3-nitrobenzoate 
• 1160293-25-3 methyl 1-(2-chloroacetyl)-2-oxoindoline-6-carboxylate 
• 14719-83-6 methyl 3-nitro-4-chlorobenzoate 
• 1160293-27-5 [4-(methoxycarbonyl)-2-nitrophenyl]malonic acid dimethyl ester 
• 96-99-1 4-chloro-3-nitrobenzoate 
• 1235004-99-5 methyl 2-oxoindole-6-carboxylate 
• 707-07-3 orthobenzoic acid trimethyl ester 

Downstream Products

• 656247-17-5 nintedanib 
• 1987887-92-2 methyl (Z)-3-(((4-(methylamino)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate 
• 1160294-26-7 nintedanib 

Relevant academic research and scientific papers

Potential impurity compound of Nintedanib, as well as preparation method, application and detection method of potential impurity compound

The invention relates to a potential impurity compound of Nintedanib, and a preparation method, application and detection method of the potential impurity compound. The structure of the potential impurity compound is shown in the formula (as shown in the specification). The invention aims to improve the quality standard of Nintedanib through study on impurities to guarantee the safe medication of Nintedanib. According to the preparation method disclosed by the invention, the pure potential impurity compound of Nintedanib is obtained, so that a reference substance for qualitative and quantitative analysis is provided for the detection of a finished Nintedanib product.

Impurity compound of Nintedanib, as well as preparation method, application and detection method of impurity compound

The invention relates to an impurity compound of Nintedanib, as well as a preparation method, application and detection method of the impurity compound. The structure of the impurity compound is shown in the following formula I (as shown in the specification), or in the following formula II (as shown in the specification). The invention aims to improve the quality standard of Nintedanib through study on impurities to guarantee the safe medication of Nintedanib. According to the preparation method disclosed by the invention, the pure impurity compound of Nintedanib is obtained, so that a reference substance for qualitative and quantitative analysis is provided for the detection of a finished Nintedanib product.

nepal reaches Neeb process and intermediates for the synthesis of (by machine translation)

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)

Design, synthesis and biological evaluation of deuterated nintedanib for improving pharmacokinetic properties

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.

INDOLINONE DERIVATIVES AND PROCESS FOR THEIR MANUFACTURE

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.

PROCESS FOR THE MANUFACTURE OF AN INDOLINONE DERIVATIVE

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.