- Synthesis method of domperidone drug intermediate 1-(3-chloropropyl)-benzimidazolyl-2-one
-
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.
- -
-
Paragraph 0007; 0018; 0019
(2016/11/21)
-
- N-Bridged Heterocycles. Part 5. α,ω-Bis-(2-oxobenzimidazolinyl)-alkanes and -ethers as Selective Ligands for Group-1 and -2 Metals
-
A series of the title compounds (10), (12), and (13) and several analogues were synthesised from the readily available 1-isopropenylbenzimidazolin-2-one.Various substituents were attached to the unsubstituted nitrogen atoms of the benzimidazolinone moieties and the series of products obtained were tested for their complexing ability with group-1 and -2 metal-salts.The isolation of crystalline complexes, the solubilisation of the salts in chloroform by ligand, the i.r. carbonyl absorption shift, and the ion-transport ability of the ligand were examined as an index of complexation.Selective complexation, particularly for calcium, was noted in several cases.
- Meth-Cohn, Otto,Smith, David I.
-
p. 261 - 270
(2007/10/02)
-
- 1,3-Dihydro-1-[3-(1-piperidinyl)propyl]-2H-benzimidazol-2-ones and related compounds
-
Compounds of the class of 1-(benzazolyalkyl)piperidine derivatives useful as antiemetic agents.
- -
-
-
- 1-Benzazolylalkyl-4-substituted-piperidines
-
Compounds of the class of 1-(benzazolyalkyl)piperidine derivatives, useful as neuroleptic agents.
- -
-
-