120014-07-5Relevant articles and documents
An improved and efficient process for the production of donepezil hydrochloride: Substitution of sodium hydroxide for n-butyl lithium via phase transfer catalysis
Niphade, Navanath,Mali, Anil,Jagtap, Kunal,Ojha, Ramesh Chandra,Vankawala, Pravinchandra J.,Mathad, Vijayavitthal T.
, p. 731 - 735 (2008)
A simple, efficient and highly economic process for the production of donepezil hydrochloride (1), an anti-Alzheimer drug is reported. The process relies upon improved and large-scale synthesis of a key intermediate: 1-benzylpiperidine-4-carboxaldehyde (2), and the introduction of operationally simple chemistry at the penultimate stage wherein 2 is reacted with 5,6-dimethoxy indanone (3) in the presence of sodium hydroxide and a phase transfer catalyst (PTC) in a biphasic solvent to furnish the intermediate 4, which is reduced and directly treated with hydrochloric acid to furnish highly pure donepezil hydrochloride with desired polymorphic form. The improved process provides donepezil hydrochloride at considerably lower cost and allows the omission of hazardous chemicals.
Purification method of donepezil hydrochloride key intermediate compound (by machine translation)
-
Paragraph 0031-0037, (2020/08/17)
The invention discloses a purification method of a donepezil hydrochloride key intermediate compound, and the crude molecular formula of the compound (I) is shown in the specification. Solid potassium fluoride (KFFFAl) on alumina2 O3 In the presence C6 -C12 In the aromatic hydrocarbon-containing organic solvent, the reaction 70 - 110 °C is stirred at 0.5 - 3h to obtain a high-purity compound (I), in C. 6 -C12 The benzene-containing aromatic hydrocarbon organic solvent is selected from benzene, toluene and xylene, is simple and convenient to operate, high in yield and good in product purity, and is suitable for industrial production. (by machine translation)
Preparation method of donepezil hydrochloride
-
Paragraph 0039; 0042; 0043, (2016/10/17)
The invention discloses a preparation method of donepezil hydrochloride. The preparation method comprises the steps that 3-chlorine-1-(3, 4-dimethoxy phenyl) propane-1-ketone (II) is made to react with N-benzyl-4-formyl-piperidine (III) under the conditio