1006376-62-0Relevant articles and documents
Preparation method of phenyl-containing compound
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Paragraph 0090-0098, (2022/01/04)
The present invention discloses a method for preparing an phenyl-containing compound. The present invention provides a method for preparing a compound shown in formula I, comprising the following steps: in the presence of formamide or acetamide, in the pr
Preparation method of chiral aromatic cyclopropylamine and salt thereof and intermediate used in preparation method
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, (2020/06/20)
The embodiment of the invention provides a preparation method of a compound as shown in a formula I or salt thereof, which comprises the following steps: (1) reacting a compound as shown in a formulaVI with a compound as shown in a formula VII in a first
Preparation method of ticagrelor key intermediate aromatic cyclopropanamide
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Paragraph 0028-0034, (2019/11/20)
The invention discloses a preparation method of a ticagrelor key intermediate, aromatic cyclopropanamide. The method comprises the following steps: with (1R,2R)-2-(3,4-difluorophenyl)-1-cyclopropyl formate (I) as an initial raw material, carrying out tran
Preparation method of ticagrelor
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, (2018/04/21)
The invention discloses a preparation method of ticagrelor. The preparation method comprises the following steps: (1) preparation of ticagrelor intermediate product 1-TK acid; (2) preparation of ticagrelor intermediate product 2-TK-amide; (3) preparation of ticagrelor intermediate product 3-TK-amino compound hydrochloride; (4) preparation of ticagrelor intermediate product 4-TK-amino compound R-tartrate; ( 5) preparation of ticagrelor intermediate product 5-TK-amino compound L-mandelate; and (6) preparation of ticagrelor-TK. The preparation method has the advantages of cost advantage, mature and stable process, stable product quality, and safe and reliable production process.
Synthetic method for ticagrelor intermediate (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine
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, (2018/07/30)
The invention discloses a synthetic method for a ticagrelor intermediate (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine. The method comprises the following steps: (5H)-furan-2-one is taken as a starting raw material, the (5H)-furan-2-one and a 3,4-difluor
(1 R, 2 S) - 2 - (3, 4 - difluorophenyl) amine ·D - mandelic acid salt preparation method
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Paragraph 0119-0122, (2018/02/04)
The invention discloses a preparation method of (1R,2S)-2-(3,4-difluorophenyl) rolicyprine.D-mandelate. The preparation method comprises the following steps: carrying out cyclopropanation on a compound shown in a formula V to obtain a compound shown in a formula IV; carrying out amide generation and Hofmann degradation to obtain a compound shown in a formula II; and performing salification with D-mandelic acid to obtain a compound shown in a formula I. The compound shown in the formula V is prepared in a way that a compound shown in a structure formula VI is subjected to CBS asymmetric reduction reaction, wherein a catalyst for the CBS asymmetric reduction reaction is a compound shown in a structural formula VII, and a reduction agent for the CBS asymmetric reduction reaction can be borane-tetrahydrofuran or borane-N,N-diethyl phenylamine.
Synthetic method of ticagrelor intermediate and intermediate thereof
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Paragraph 0043-0045; 0058, (2017/07/21)
The invention discloses a synthetic method of a ticagrelor intermediate and the intermediate thereof. The synthetic method comprises the following steps of: firstly, performing a diazo-reaction on a compound (2) to prepare a compound (3); performing a rho
for standard auspicious Luo river intermediate preparation method
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Paragraph 0082; 0083, (2017/08/25)
The inventiondiscloses a preparation method of ticagrelor. The method comprises the following steps: (1) reducing a compound shown in a formula III in the presence of a proton source provided by sodium borohydride or potassium borohydride and diethyl aniline hydrochloride to obtain a compound shown in a formula IV; (2) reacting the compound IV in the presence of alkali to generate a compound VI; (3) hydrolyzing the compound VI without purification to generate a compound VII; (4) reacting the compound VII to generate acyl chloride, reacting the acyl chloride to generate formamide, thus obtaining a compound shown in a formula IX; and (5) carrying out Hofmann rearrangement on the compound IX to obtain a compound shown in a formula II. Regents used in the method are nontoxic, harmless, environmentally friendly and low in price; the used key reagents can be recycled. Therefore, the method is applicable to industrial production.
Intermediate for standard auspicious Luo river (1R, 2S) - 2 - (2,3-difluorophenyl) method for the preparation of cyclopropylamines (by machine translation)
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Paragraph 0038; 0044, (2017/03/23)
The invention discloses a method for preparing ticagrelor midbody (1R,2S)-2-(2,3-difluorophenyl) cyclopropylamine, belonging to the technical fields of organic synthesis route design and preparation of raw material medicines and midbodies. The method comprises the following steps: performing alcoholysis on succinic anhydride, thereby obtaining mono-methyl succinate, performing acylating chlorination reaction on mono-methyl succinate, thereby obtaining a compound methyl 4-chloro-4-oxobutyrate, performing Fridel-Crafts reaction on methyl 4-chloro-4-oxobutyrate and o-difluorobenzene, thereby obtaining a compound methyl 4-ketone-4-(3,4-difluorophenyl) butyrate (IV), and further performing asymmetric reduction reaction, cyclization reaction and Hoffman degradation on the compound IV, thereby obtaining the compound (1R,2S)-2-(2,3-difluorophenyl) cyclopropylamine. Initial raw materials used in the method are low in cost and easy to obtain, the reaction condition is gentle, the operation is safe, simple and convenient, the environment pollution is small, and the key ticagrelor midbody prepared by using the method is simple and convenient in after treatment, and is beneficial to on-scale production.
Synthesizing method of (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine
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, (2017/02/28)
The invention provides a synthesizing method of (1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine. The synthesizing method comprises the steps that a compound (I) reacts with diethyl cyanomethylphosphonate in the presence of alkaline substances to obtain a c