- Preparation method of bilastine intermediate
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The invention relates to a preparation method of a bilastine intermediate represented by a formula 1. The preparation method specifically comprises: carrying out a reaction in a first solvent in the presence of DBU by using 2-bromoethyl anisole (formula I
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Paragraph 0086-0087
(2020/02/10)
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- Synthesis method of bilastine intermediate
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The invention relates to a synthesis method of a bilastine intermediate. The synthesis method comprises the following steps: S1, carrying out a Friedel-Crafts reaction on phenethyl acetate and isobutyryl halide under catalysis of Lewis acid to generate an intermediate compound B; S2, hydrolyzing the intermediate compound B to remove ester groups under an alkaline or acidic condition to obtain an intermediate compound C; S3, carrying out a hydroxyl protection reaction on the intermediate compound C to obtain an intermediate compound D by adding benzyl or p-methoxybenzyl protection groups to theintermediate compound C; S4, carrying out a bromination reaction on the intermediate compound D to generate an intermediate compound E; S5, carrying out a rearrangement reaction on the intermediate compound E under catalysis of a metal reagent to generate an intermediate compound F; and S6, carrying out hydrogenation or oxidative deprotection on the intermediate compound F to generate a target compound bilastine intermediate methyl alpha,alpha-dimethyl-4-(2-hydroxyethyl)phenylacetate. The method provided by the invention has low raw material cost and simple requirements on equipment and experimental conditions, can realize industrial production, and has a high application value.
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Paragraph 0007; 0024
(2020/02/14)
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- A 2 - methyl - 2' - phenyl propanoic acid derivatives of preparation method and its intermediate (by machine translation)
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The invention relates to a 2 - methyl - 2' - phenyl propionic acid derivatives preparation method and intermediate thereof, the method is simple and efficient, less side reaction, high yield, low cost, and is suitable for industrial production. (by machin
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Paragraph 0070; 0071
(2018/04/01)
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- Alternative synthesis of bilastine
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A new and efficient synthesis of the non-sedating histamine H1 receptor antagonist Bilastine is reported. The new route employs a convergent strategy, with a longest linear sequence of five steps, giving slightly improved yields over the previous routes.
- Collier, Steven J.,Wu, Xiang,Poh, Zhiying,Rajkumar, Gurubatham Abraham,Yet, Larry
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p. 1394 - 1402
(2011/05/11)
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- PROCESS FOR THE PREPARATION OF 2-METHYL-2'-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS
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The present invention relates to a process for preparing 2-methyl-2′-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present inv
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Page/Page column 5
(2011/02/15)
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- PROCESS FOR PREPARATION OF 2-METHYL-2′-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS
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The present invention relates to a process for preparing 2-methyl-2'-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present inv
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Page/Page column 13
(2009/10/09)
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