- Method for preparing ebastine
-
The invention provides a method for preparing ebastine. The method comprises the following steps: condensing an initial raw material benzophenone and 4-hydroxypiperidine to obtain 4-benzhydryloxypiperidine; condensing with 4-chloro-1-(4-tert-butylphenyl)-1-butanone to obtain ebastine. According to the method, benzophenone with low price is used as the initial raw material, has low cost and is simple and convenient to operate, only one reaction kettle is used, alkaline washing and rinsing are performed in the middle process, and the final product can be obtained by freezing and crystallizing with alcohol. The method has the advantages of good economic benefit, high safety, high yield, good purity and the like, and is suitable for industrial production.
- -
-
Paragraph 0052-0064
(2019/04/27)
-
- PROCESS OF PREPARING EBASTINE
-
The present invention relates to a novel process for the preparation of pure Ebastine and use of the same in formulation without micronising. The invention further relates to the process of preparation of 1 -[4-(1, 1 -dimethyl ethyl) phenyl] -4-(4-hydroxy piperidin-1-yl) butan-1-one (compound II), an intermediate or preparation of Ebastine and use of the same in the preparation of pure Ebastine with the maximum particle size more than 1000 μm and D90 from 250 μm -1000 μm.
- -
-
-
- PROCESS FOR THE PREPARATION OF 1-[4-(1,1-DIMETHYLETHYL)PHENYL]-4-[4-(DIPHENYLMETHOXY)-1-PIPERIDINYL]-1-BUTANONE AND ACID ADDITION SALTS THEREOF
-
The present invention describes processes for the preparation of 1-[4-(11,- dimethylethyl)phenyl] -4- [4-(diphenylmethoxy)- 1 -piperidinyl] - 1 -butanone and acid addition salts thereof.
- -
-
Page/Page column 40-41
(2011/10/13)
-
- Process for the preparation of 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone and acid addition salts thereof
-
The present invention describes processes for the preparation of 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone and acid addition salts thereof.
- -
-
Page/Page column 28
(2011/10/13)
-
- PROCESS OF PREPARING EBASTINE
-
The present invention relates to a novel process for preparing ebastine from 1-[4-(1,1-dimethylethyl) phenyl]-4-(4-hydroxy piperidin-1-yl) butan-1-one and diphenyl methanol, which is easily reproducible on an industrial scale. A process for preparation of 1-[4-(1,1-dimethylethyl) phenyl]-4-(4-hydroxy piperidin-1-yl) butan-1-one.
- -
-
Page/Page column 11
(2010/01/30)
-
- Piperidine derivatives
-
Compounds of the general formula I: STR1 wherein R1 represents a thienyl group, or a phenyl group optionally substituted by a halogen (preferably fluorine or chlorine) atom, a lower alkoxy or lower alkyl group, R2 represents a hydrogen or halogen (preferably fluorine) atom, a lower alkoxy or lower alkyl group, R3 represents a hydrogen or halogen (preferably fluorine) atom, a lower alkylthio, lower alkoxy or lower alkyl group, or a cycloalkyl group containing 5 or 6 carbon atoms, or a group of the general formula: STR2 wherein R4 and R5 singly each represents a hydrogen atom or lower alkyl group, R6 represents a cycloalkyl, hydroxymethyl, carboxy or lower alkoxycarbonyl group, and W represents a carbonyl STR3 or a hydroxymethylene [viz. --CH(OH)--] group, and pharmacologically acceptable salts thereof possess potent selective Histamine H1 -receptor blocking and calcium antagonist properties and are of interest in the treatment of a variety of respiratory, allergenic and cardiovascular disease states. The new compounds can be prepared by various methods based on the condensation of α-substituted benzyl halides with N-(benzoylpropyl or phenyl-hydroxypropyl)-4-hydroxy piperidines or condensation of di-substituted-methoxy-piperidines with a benzoylpropyl halide or a phenyl-hydroxypropyl-halide followed, where necessary, by removal of protecting groups.
- -
-
-
