138229-59-1Relevant academic research and scientific papers
Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule
Zhao, Qiuye,Lan, Tianlong,Su, Shang,Rao, Yu
, p. 369 - 372 (2019)
Poly (ADP-ribose) polymerase-1 (PARP1) is a major member of the PARP superfamily that is involved in DNA damage signalling and other important cellular processes. Here we report the development of a small molecule targeting PARP1 based on the PROTAC strategy. In the MDA-MB-231 cell line, the representative compound 3 can induce significant PARP1 cleavage and programmed cell death.
Indazole formamide compound as well as preparation method and application thereof
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, (2021/02/16)
The invention belongs to the field of chemical medicines, and particularly relates to an indazole formamide compound as well as a preparation method and application thereof. The invention provides anindazole carboxamide compound or a pharmaceutically acce
Synthesis method of methyl 3-formyl-2-nitrobenzoate
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Paragraph 0024; 0026; 0027; 0029, (2019/11/20)
The invention provides a synthesis method of methyl 3-formyl-2-nitrobenzoate. Firstly, methyl 3-methyl-2-nitrobenzoate is subjected to a substitution reaction with chlorine to obtain methyl 3-(dichloromethyl)-2-nitrobenzoate; the methyl 3-(dichloromethyl)
PROCESSES FOR THE PREPARATION OF NIRAPARIB AND INTERMEDIATES THEREOF
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Paragraph 00181; 00182, (2019/03/05)
The present invention relates to novel procedures and novel intermediates useful in the synthesis of Niraparib or any salt thereof.
Derivative based on PARP inhibitor Niraparib and a preparation method and use thereof
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, (2019/10/29)
The invention discloses a derivative based on a PARP inhibitor Niraparib. The derivative has a structure shown in a formula I as shown in the description, wherein R1 is selected from alkyl, alkoxy, cycloalkyl, aryl alkyl, cycloalkyl alkyl, heterocyclyl, a
SINGLE MOLECULE COMPOUNDS PROVIDING MULTI-TARGET INHIBITION OF PARP AND OTHER PROTEINS AND METHODS OF USE THEREOF
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, (2019/01/10)
The invention relates to compounds useful for inhibiting PARP and at least one other protein and to methods of treating diseases including cancer by administration of a compound(s) of Formula I-V (or pharmaceutically acceptable salts thereof) as defined herein.
Niraparib synthesis method
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, (2017/04/28)
The invention discloses a Niraparib synthesis method. The method comprises that through esterification, 3-methyl hydroformylation, 3-schiff base reaction, cyclization, amidation, BOC removal and chiral resolution, optically pure Niraparib with purity of 91% or more is prepared from 3-methyl-2-nitrobenzoic acid. The method has the advantages of simple process, high efficiency, easy operation and less equipment requirement, and is a method suitable for industrial production.
A prepares Nepal to pull handkerchief Nepal method (by machine translation)
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Paragraph 0055; 0056, (2017/07/23)
The invention discloses a compound 2 - [4 - ((3S) - 3 - piperidinyl) phenyl] - 2H - indazole - 7 - carboxamide preparation method, through the 4 - nitro phenylpyridyl with reaction produced animal pen halogenphenmethyl season ammonium salt, by sodium borohydride reduction of the pyridine quaternary ammonium salt, in the palladium reagent obtained under the action of the 3 - (4 - aminophenyl) piperidine, in the chiral reagent obtained under the action of the (S)- 3 - (4 - halophenyl) piperidine, with 3 - formyl - 2 - nitro-benzoic acid methyl ester condensation and in sodium azide formed under the action of powder medicine, after preparing the amine Niraparib (molecular entity is: 2 - [4 - ((3S) - 3 - piperidinyl) phenyl] - 2H - indazole - 7 - carboxamide). (by machine translation)
Method for preparing Niraparib of PARP (poly-ADP-ribose polymerase) inhibitor
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Paragraph 0052; 0053, (2017/07/19)
The invention discloses a method for preparing 2-(4-((3S)-3-piperidyl) phenyl)-2H-indazole-7-formamide of a compound. Benzyl protected-piperidone is generated into piperidone of 3-triflic anhydride under the action of triflic anhydride, the piperidone and nitrobenzoic acid are subjected to Suzuki reaction to obtain a coupled product, 3-(4-aminophenyl) piperidine is obtained under the action of a palladium reagent, (S)-3-(4-halogenated phenyl) piperidine is prepared with a chirality resolution reagent, the (S)-3-(4-halogenated phenyl) piperidine is condensed with 3-formyl-2-methyl nitrobenzoate to form pyrazolone ring under the action of sodium azide, and the Niraparid (with the molecular entity of 2-(4-((3S)-3-piperidyl) phenyl)-2H-indazole-7-formamide) is prepared via aminolysis.
Development of a fit-for-purpose large-scale synthesis of an oral PARP inhibitor
Wallace, Debra J.,Baxter, Carl A.,Brands, Karel J. M.,Bremeyer, Nadine,Brewer, Sarah E.,Desmond, Richard,Emerson, Khateeta M.,Foley, Jennifer,Fernandez, Paul,Hu, Weifeng,Keen, Stephen P.,Mullens, Peter,Muzzio, Daniel,Sajonz, Peter,Tan, Lushi,Wilson, Robert D.,Zhou, George,Zhou, Guoyue
experimental part, p. 831 - 840 (2012/07/03)
Compound (1) a poly(ADP-ribose)polymerase (PARP) inhibitor has been made by a fit-for-purpose large-scale synthesis using either a classical resolution or chiral chromatographic separation. The development and relative merits of each route are discussed,
