- Derivative based on PARP inhibitor Niraparib and a preparation method and use thereof
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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
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- Method for preparing Niraparib of PARP (poly-ADP-ribose polymerase) inhibitor
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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.
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- A prepares Nepal to pull handkerchief Nepal method (by machine translation)
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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)
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- Development of a fit-for-purpose large-scale synthesis of an oral PARP inhibitor
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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,
- 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
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p. 831 - 840
(2012/07/03)
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