- Method for synthesizing 1-(3-chloropropyl)-benzimidazole-2-ketone
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The invention provides a method for synthesizing 1-(3-chloropropyl)-benzimidazole-2-ketone. The reaction route is shown in the description. The method has the beneficial effects that 1, the inventiondesigns the novel synthesis route to prepare a domperidone intermediate with the structure shown in the formula (DOM-4), and the novel synthesis route is realized; the reaction selectivity of the route is good, the controllability is strong, and the route is quite favorable for the implementation of large-scale industrial production; 2, by using the route and the method provided by the invention,the production cost of the domperidone intermediate is greatly lowered, and the purity of the domperidone intermediate is increased, so that the production cost of the domperidone intermediate is greatly reduced.
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Paragraph 0028; 0029; 0030; 0031; 0039; 0040
(2018/07/06)
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- Synthesis method of domperidone drug intermediate 1-(3-chloropropyl)-benzimidazolyl-2-one
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The invention relates to a synthesis method of a domperidone drug intermediate 1-(3-chloropropyl)-benzimidazolyl-2-one, which comprises the following steps: adding 0.19mol of 1-allylbenzoimidazolyl-2-one, 120-140ml of ethylene glycol and 0.26-0.28mol of sodium sulfite, heating to 35-40 DEG C, controlling the stirring rate at 110-130 rpm, dropwisely adding 0.23-0.25mol of 1-amido-3-bromo-propane within 2-3 hours, reacting for 4-5 hours, pouring the reaction product into a sodium chloride solution, extracting with cyclohexanol 5-7 times, drying the cyclohexanol extracting solution with calcium oxide, evaporating to remove the solvent to obtain oily 1-allyl-3-(3-chloropropyl)benzimidazolyl-2-one (3); and adding 120ml of phosphoric acid solution and 60ml of propionitrile into the oily product (3), controlling the stirring rate at 110-130 rpm, heating the solution to 70-75 DEG C, reacting for 3-4 hours, evaporating to remove partial propionitrile, cooling to precipitate a solid, filtering, washing the solid with salt solution, and dehydrating to obtain the 1-(3-chloropropyl)-benzimidazolyl-2-one.
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Paragraph 0008; 0020
(2016/11/21)
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- 2-SULFANYL-BENZOIMIDAZOL-1-YL-ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS
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The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent "chemoattractant receptor-homologous molecule expressed on Th2 cells" antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.
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Page/Page column 93
(2010/10/20)
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- TRICYCLIC ANALOGUES OF THE ANTIALLERGIC AGENT OXATOMIDE: 1-(3-(4-(10,11-DIHYDRO-5H-DIBENZOCYCLOHEPTENE-5-YL)-1-PIPERAZINYL)PROPYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE AND THE RELATED 6,11-DIHYDRODIBENZOTHIEPIN, 4,9-DIHYDROTHIENO-2-BENZOTHIEPIN, AND ...
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11-Chloro-6,11-dihydrodibenzothiepin and its 2-methyl derivative VI were transformed via the 11-(4-(ethoxycarbonyl)-1-piperazinyl) compounds IVc and Vc to 11-(1-piperazinyl) compounds IVb and Vb.Their reactions with 1-(3-chloropropyl)-1,3-dihydro-2H-benzimidazol-2-one (II) afforded the title compounds IVa and IVb.Similar reactions and sequences in the series of 10,11-dihydro-5H-dibenzocycloheptene, 4,9-dihydrothieno-2-benzothiepin, and 10,11-dihydrodibenzothiepin led to further oxatomide (Ia) analogues IIIa and VIIa-XIa.In the test of passivecutaneous anaphylaxis in rats, compound VIIIa was more active than Ia, and IVa had similar activity like Ia.
- Jilek, Jiri,Holubek, Jiri,Svatek, Emil,Metys, Jan,Frycova, Hana,et al.
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p. 870 - 883
(2007/10/02)
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- A New Approach to 1-Alkyl-1,3-dihydro-2H-benzimidazol-2-ones
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A new procedure for preparing 1-alkyl-1,3-dihydro-2H-benzimidazol-2-ones from o-nitroanilines by succesive ethoxycarbonylation, catalytic hydrogenation and thermal cyclization under neutral conditions is described. - (Keywords: Thermal cyclization)
- Gomez-Parra, Vicente,Sanchez, Felix,Torres, Tomas
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p. 639 - 644
(2007/10/02)
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- 1,3-Dihydro-1-[3-(1-piperidinyl)propyl]-2H-benzimidazol-2-ones and related compounds
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Compounds of the class of 1-(benzazolyalkyl)piperidine derivatives useful as antiemetic agents.
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