1196713-67-3Relevant articles and documents
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
Method for preparing Niraparib of PARP (poly-ADP-ribose polymerase) inhibitor
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, (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.
Process development of C-N cross-coupling and enantioselective biocatalytic reactions for the asymmetric synthesis of niraparib
Chung, Cheol K.,Bulger, Paul G.,Kosjek, Birgit,Belyk, Kevin M.,Rivera, Nelo,Scott, Mark E.,Humphrey, Guy R.,Limanto, John,Bachert, Donald C.,Emerson, Khateeta M.
, p. 215 - 227 (2014/05/20)
Process development of the synthesis of the orally active poly(ADP-ribose)polymerase inhibitor niraparib is described. Two new asymmetric routes are reported, which converge on a high-yielding, regioselective, copper-catalyzed Narylation of an indazole derivative as the late-stage fragment coupling step. Novel transaminase-mediated dynamic kinetic resolutions of racemic aldehyde surrogates provided enantioselective syntheses of the 3-aryl-piperidine coupling partner. Conversion of the C-N cross-coupling product to the final API was achieved by deprotection and salt metathesis to isolate the desired crystalline salt form.