2098974-13-9Relevant academic research and scientific papers
Novel and practical synthesis of vonoprazan fumarate
Yu, Qian-Ying,Zeng, Huang,Yao, Kai,Li, Jian-Qi,Liu, Yu
, p. 1169 - 1174 (2017)
A novel and practical strategy for the synthesis of vonoprazan fumarate 1, a novel potassium-competitive acid blocker, has been developed. Vonoprazan fumarate was obtained through a four-step process starting from 5-(2-fluorophenyl)-1H-pyrrole-3-carboxylate and including ester hydrolyzing, methylamine substitution, sulfonyl chloride substitution, and amide reduction. Key to the strategy is the amide reduction taking a novel and practical protocol. The main advantages of this route include two parts: controllable impurity and acceptable overall yield.
Preparation method of funolasan fumarate
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, (2022/01/10)
The present invention provides a method for preparing funorasine fumarate, comprising the following steps: (1) the compound of formula I is azidine to give a compound of formula II.; (2) the compound of formula II. is cyclized with the compound of formula III. to give a compound of formula IV.; (3) the compound of formula IV. is condensed with a compound of formula VI. to give a compound of formula VII. compound; (4) a compound of formula VII. is deprotected with acid to obtain a vonorasin free base; (5) a vonorasin free base is salted with fumarate to give vonorasin fumarate. According to the method of the present invention to synthesize vonoracin fumarate, compared with the prior art, the total yield of vonora fumarate increased to more than 60%, and the yield has been greatly improved. Furthermore, compound formula IV. can be used as a new intermediate for the preparation of funolasine fumarate.
Preparation method of tenosynol fumarate
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, (2021/11/19)
The invention discloses a preparation method of fumarate administered by a synthetic digestive system. In particular, the invention relates to a method for large-scale preparation of tenoteno fumarate; the adopted starting materials are easy to obtain; th
Preparation method of high-purity vonoprazan fumarate
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Paragraph 0054, (2021/05/26)
The invention discloses a preparation method of high-purity vonoprazan fumarate. The preparation method comprises the steps of 1, preparing 5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl) pyrrole-3-formaldehyde; 2, dissolving the 5-(2-fluorophenyl)-1-(pyridine
Vonoprazan fumarate intermediate and preparation method thereof
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, (2021/10/27)
The invention provides a vonoprazan fumarate intermediate compound as well as a preparation method and application thereof. Compared with the prior art, the technical scheme provided by the invention avoids the hydrogenation reaction operation with higher
Preparation method of high purity funolasine fumarate
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Paragraph 0071-0078, (2022/01/08)
The present invention discloses a method for preparing a pure vonorasine fumarate, comprising the following steps: 5- (2-fluorophenyl)-1 [(pyridin-3-yl) sulfonyl] -1H- pyrrole-3-formaldehyde as the starting material, the starting material is dissolved in
Vonoprazan fumarate preparation method
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, (2020/02/10)
The invention provides a vonoprazan fumarate preparation method, which comprises: reducing 5-(2-fluorophenyl)-1-(pyridine-3-ylsulfonyl)-1H-pyrrole-3-formaldehyde with a reducing agent, adding oxalic acid, carrying out a reaction to prepare a crude vonopra
Preparation method of low-impurity Vonoprazan fumarate
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, (2020/01/03)
The invention provides a preparation method of low-impurity Vonoprazan fumarate. A method for removing impurities A-E during preparation of Vonoprazan comprises the steps: preparing Vonoprazan hydrobromide from Vonorazan, and removing the impurities A-E which are difficult to remove by using a recrystallization purifying method, wherein the method for removing the impurities A-E during preparationof Vonoprazan has good selectivity to the impurities A-E. The preparation method of low-impurity Vonoprazan fumarate comprises the steps: performing a reaction on 5-(2-fluorophenyl)-1-(pyridyl-3-ylsulfonyl)-1H-pyrrole-3-formaldehyde and methylamine or a salt of methylamine, then performing reduction so as to obtain Vonoprazan, then preparing Vonoprazan hydrobromide, then performing salt dissociation so as to obtain Vonoprazan free alkali, preparing Vonoprazan fumarate with a purity of 99.7% or above, and then performing recrystallization refining so as to obtain Vonoprazan fumarate with a purity of 99.9% or above. The invention provides an impurity D, a preparation method of the impurity D and application of the impurity D as an impurity reference substance in Vonoprazan fumarate.
An Efficient, Scalable and Eco-friendly Synthesis of 4,5-substituted Pyrrole-3-Carbonitriles by Intramolecular Annulation on Pd/C and HZSM-5
Chen, Jianchao,Li, Chengtao,Zhou, Yanan,Sun, Changshan,Sun, Tiemin
, p. 1943 - 1948 (2019/03/26)
An efficient and eco-friendly protocol for the synthesis of diverse 4,5-substituted 1H-pyrrole-3-carbonitriles has been developed using commercially available HZSM-5 and Pd/C as recyclable heterogeneous catalysts with more excellent yields (up to 98 %) than traditional liquids acids, and successfully applied in the practical synthesis of vonoprazan. The conspicuous features of this protocol are higher product yield, easy work-up, eco-friendly and reusability of catalysts.
Preparation method of vonoprazan fumarate
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Paragraph 0038-0051, (2019/11/25)
The invention provides a preparation method of vonoprazan fumarate (I). The method comprises the following steps: selecting easily-available 5-(2-fluorophenyl)-1-(3-pyridylsulfonyl)-3-cyano-1H-pyrrole(II) as a raw material, carrying out a reaction in one
