19733-56-3Relevant articles and documents
PROCESSES FOR THE PREPARATION OF NIRAPARIB AND INTERMEDIATES THEREOF
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, (2019/03/05)
The present invention relates to novel procedures and novel intermediates useful in the synthesis of Niraparib or any salt thereof.
Method for preparing 4-(piperidine-3-yl)aniline
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Paragraph 0045; 0046, (2017/04/03)
The invention discloses a method for preparing 4-(piperidine-3-yl)aniline. The method is characterized by comprising the steps that a salifying reaction is carried out, wherein 3-(4-nitrophenyl)pyridine and 3-halogenated propylene react to obtain N-allyl-3-(4-nitrophenyl)pyridine quaternary ammonium salt; a reduction reaction is carried out, wherein N-allyl-3-(4-nitrophenyl)pyridine quaternary ammonium salt is mixed with zinc chloride, and then sodium borohydride is added for reduction to obtain 4-(piperidine-3-yl)aniline. According to the method, use of precious metal is avoided, production cost of the intermediate 4-(piperidine-3-yl)aniline is greatly lowered, conditions are mild, nitryl and a pyridine ring are subjected to reduction at a time, a good yield is obtained, and the method is especially suitable for large-scale industrial production.
A prepares Nepal to pull handkerchief Nepal method (by machine translation)
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, (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)