- Continuous synthesis method of succinate (by machine translation)
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The invention discloses a method for continuously synthesizing succinic acid, which is designed according to 3D printing technology, and sequentially combines the chlorination, hydrolysis, condensation, salt forming and refining steps of 4 -acetylamino -2, 3 -dihydrobenzofuran -7 - methyl formate into each reaction chamber to realize the continuous synthesis of drugs. To the method, tedious manual operation is not needed, chemical synthesis is carried out rapidly, the yield of a synthetic route is improved in a flowing chemical manner, and the safety problem caused by manual operation is avoided. The method provided by the invention can greatly reduce the cost generated in the aspects of drug storage, transportation and the like, thereby improving the medicine supply efficiency and stability, and bringing great economic and social benefits for the development of the pharmaceutical industry. (by machine translation)
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Paragraph 0033; 0036; 0039; 0042; 0045; 0048; 0051; 0054
(2020/09/16)
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- Synthetic method for prucalopride succinate intermediate 4-amino-5-chloro-2,3-dihydrobenzofuran-7-carboxylic acid
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The invention belongs to the technical field of medicines, and relates to a synthetic method for a prucalopride succinate intermediate 4-amino-5-chloro-2,3-dihydrobenzofuran-7-carboxylic acid. The final product 4-amino-5-chloro-2,3-dihydrobenzofuran-7-carboxylic acid is obtained by using p-aminosalicylic acid as a starting raw material, successively performing esterification, acylation, and twice halogenation to obtain 4-acetylamino-3-bromo-5-chloro-2-hydroxybenzoic acid methyl ester, then performing substitution reaction on 1,2-dibromoethane and the 4-acetylamino-3-bromo-5-chloro-2-hydroxybenzoic acid methyl ester to obtain 4-acetylamino-3-bromo-2-(2-bromoethoxy)-5-chlorobenzoic acid methyl ester, and successively performing cyclization and hydrolyzation. According to the invention, the raw materials are easy to get, the operation is simple and mild, the production period is short, the purity is high, the safety is good, the costs are low, and the synthetic method is suitable for industrialized production.
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Paragraph 0051; 0052
(2017/12/06)
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- PROCESSES FOR THE PREPARATION OF HIGHLY PURE PRUCALOPRIDE SUCCINATE AND ITS INTERMEDIATES
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Provided herein are purification processes for the preparation of highly pure prucalopride succinate salt. Provided also herein are improved, commercially viable and industrially advantageous processes for the preparation of Prucalopride and its intermediate compounds, for example, methyl 4-acetylamino-5-chloro-2,3-dihydrobenzo[b]furan-7-carboxylate and alkyl 4-[[(4-amino-5-chloro-2,3-dihydro-7-benzofuranyl)carbonyl]-amino]-1-piperidinecarboxylate.
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- Synthetic method for 4-amino-5-chloro-2,3-dihydro-7-benzofurancarboxylic acid
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The present invention relates to a drug intermediate synthetic method, in particular to a synthetic method for 4-amino-5-chloro-2,3-dihydro-7-benzofurancarboxylic acid of Prucalopride Succinate intermediate. The method comprises performing hydrolysis adopting a two-step method. According to the synthetic method disclosed by the invention, the raw material can be reacted adequately; the reaction time can be shortened; the obtained product is high in purity; and the yield is improved.
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Paragraph 0042-0044
(2017/01/17)
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- Synthesis and structure-activity relationship of 3-substituted benzamide, benzo[b]furan-7-carboxamide, 2,3-dihydrobenzo[b]furan-7- carboxamide, and indole-5-carboxamide derivatives as selective serotonin 5- HT4 receptor agonists
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The title compounds (6-9) were prepared and evaluated for serotonin 5- HT4 agonistic activity in in vitro tests. Introducing a propyl or allyl group at the 3-position of benzamide caused only a slight enhancement of agonistic activity. Construction of the benzo[b']furan skeleton and 2,3- dihydrobenzo[b]furan skeleton caused a significant enhancement of the activity. 4-Amino-N-[2-(1-azabicyclo[3.3.0]octan-5-yl)ethyl]-5-chloro-2- methylbenzo[b]furan-7-carboxamide (7b) hemifumarate was as potent as cisapride. 4-Amino-N-[2-(1-azabicyclo[3.3.0]octan-5-yl)ethyl]-5-chloro-2,3- dihydro-2-methylbenzo[b]furan-7-carboxamide (8a) hemifumarate, 4-amino-N-[2- (1-azabicyclo [3.3.0]octan-5-yl)ethyl]5-chloro-2,3-dihydro-2- ethylbenzo[b]furan-7-carboxamide (8c) hemifumarate, and 4-amino-N-]2-(1- azabicyclo[3.3.0]octan-5-yl]-5-chloro-2,3-dihydro-2,3-dimethylhenzo[b]furan- 7-carboxamide (8d) hemifumarate were more potent than cisapride. Furthermore, 8a hemifumarate was free from dopamine D1, D2, serotonin 5-HT1, 5-HT2 and muscarine M1, M2 receptor binding activity in the in vitro tests. On the other hand, construction of the indole skeleton caused a remarkable decrease in activity.
- Kakigami, Takuji,Usui, Toshinao,Tsukamoto, Katsura,Kataoka, Tadashi
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- N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
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N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.
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