1000536-33-3Relevant academic research and scientific papers
Preparation method of bilastine intermediate
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Paragraph 0086-0087, (2020/02/10)
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
Synthesis method of bilastine intermediate
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Paragraph 0007; 0024, (2020/02/14)
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.
A 2 - methyl - 2' - phenyl propanoic acid derivatives of preparation method and its intermediate (by machine translation)
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Paragraph 0070; 0071, (2018/04/01)
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
Alternative synthesis of bilastine
Collier, Steven J.,Wu, Xiang,Poh, Zhiying,Rajkumar, Gurubatham Abraham,Yet, Larry
, p. 1394 - 1402 (2011/05/11)
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.
PROCESS FOR THE PREPARATION OF 2-METHYL-2'-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS
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Page/Page column 5, (2011/02/15)
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
PROCESS FOR PREPARATION OF 2-METHYL-2′-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS
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Page/Page column 13, (2009/10/09)
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
