123654-26-2Relevant articles and documents
Continuous synthesis method of succinate (by machine translation)
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, (2020/09/16)
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)
PROCESSES FOR THE PREPARATION OF HIGHLY PURE PRUCALOPRIDE SUCCINATE AND ITS INTERMEDIATES
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Page/Page column 26; 27, (2017/09/05)
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.
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
Kakigami, Takuji,Usui, Toshinao,Tsukamoto, Katsura,Kataoka, Tadashi
, p. 42 - 52 (2007/10/03)
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.