- PROCESS FOR THE PREPARATION OF FEXOFENADINE AND OF INTERMEDIATES USED THEREIN
-
A new process for the preparation of fexofenadine and of related intermediates, which can be used in the preparation of fexofenadine, is provided.
- -
-
Page/Page column 41; 42
(2017/05/10)
-
- Fexofenadine hydrochloride of synthetic method
-
The invention discloses a fexofenadine hydrochloride synthesizing method. The fexofenadine hydrochloride synthesizing method comprises the steps of taking 2-(4-bromophenyl)-2-methylpropionate (2) as a raw material, enabling the 2-(4-bromophenyl)-2-methylpropionate (2) to react with nafoxidine to protect a carboxyl, and then reacting with [gamma]-butyrolactone to generate a compound 6, enabling the compound 6 to react with paratoluensulfonyl chloride, condensing a product and a [alpha], [alpha]-diphenyl-4-(Hydroxymethyl)-piperidine, and finally obtaining a target compound 1 through reduction and deprotection. The raw materials selected by the way are cheap to obtain; furthermore, the synthesizing method is mild in reaction condition, convenient to operate and smaller in environmental pollution, therefore the fexofenadine hydrochloride synthesizing method is an industrial way with a better application prospect.
- -
-
Paragraph 0050; 0051
(2017/08/25)
-
- A fexofenadine hydrochloride process for synthesizing
-
The invention discloses a synthetic process of fexofenadine hydrochloride. The synthetic process of fexofenadine hydrochloride comprises the following steps of: with alpha, alpha-dimethyl phenylacetic acid as a raw material, carrying out an esterification reaction on alpha, alpha-dimethyl phenylacetic acid and absolute ethyl alcohol under the catalysis of a silica gel loaded phosphotungstic acid (PW12/SiO2) solid acid catalyst to obtain alpha, alpha-dimethyl ethyl phenylacetate; carrying out Friedel-Grafts reaction on alpha, alpha-dimethyl ethyl phenylacetate and 4-chlorobutyryl chloride to obtain alpha, alpha-dimethyl-4-(4-chloro-1-oxo butyl) ethyl phenylacetate; reducing by virtue of sodium borohydride in 95% ethyl alcohol to obtain alpha, alpha-dimethyl-4-(4-chloro-1-hydroxyl butyl) ethyl phenylacetate; and carrying out N-alkylation reaction on alpha, alpha-dimethyl-4-(4-chloro-1-hydroxyl butyl) ethyl phenylacetate and alpha, alpha-dimethyl-4-piperidine methyl alcohol in DMF (dimethyl formamide) for 24 hours at the temperature of 80 DEG C to obtain alpha, alpha-dimethyl-4-[1-hydroxyl-4-[4-(hydroxyl diphenylmethyl)-1-piperidyl]-butyl] ethyl phenylacetate, and then carrying out alkali hydrolysis and salification by virtue of hydrochloric acid, so that fexofenadine hydrochloride is obtained. The synthetic process of fexofenadine hydrochloride is high in yield and low in cost, produces less pollution and is applicable to industrial mass production.
- -
-
Paragraph 0023
(2017/02/17)
-
- POLYMORPHIC FORM OF FEXOFENADINE HYDROCHLORIDE, INTERMEDIATES AND PROCESS FOR ITS PREPARATION
-
The present invention relates to a novel polymorphic form of Fexofenadine hydrochloride, to a process for preparing it, to pharmaceutical compositions containing it, as well as its use. The invention also relates to intermediates useful for the preparation of Fexofenadine hydrochloride, antihistamine drug used in the treatment of allergy symptoms.
- -
-
Page/Page column 13
(2012/01/06)
-
- Fexofenadine polymorphs
-
A process for the preparation of crystalline fexofenadine hydrochloride anhydrous Form I, comprising: a) dispersing crystalline fexofenadine hydrochloride monosolvate with acetonitrile in an acetonitrile and water mixture; b) seeding with crystalline fexofenadine hydrochloride anhydrous Form I; c) refluxing the reaction mixture; d) cooling the mixture; e) separating and collecting the precipitate.
- -
-
Page/Page column 4
(2012/01/06)
-
- PROCESS FOR THE PREPARATION OF AMORPHOUS FEXOFENADINE HYDROCHLORIDE
-
The present invention provides a process for the preparation of amorphous fexofenadine hydrochloride from fexofenadine via its weak acid addition salt, in high yield and purity. The present invention further provides a process for the preparation of amorphous fexofenadine hydrochloride from fexofenadine acid addition salt.
- -
-
Page/Page column 10
(2009/04/25)
-
- PROCESS FOR PREPARATION OF 4-[4-(4-(HYDROXYDIPHENYLMETHYL)- 1-PIPERIDINYL]-1-OXOBUTYL]-α,α-DIMETHYLBENZENE ACETIC ACID METHYL ESTER AND USE THEREOF
-
The present invention provides an improved process for preparing fexofenadine, its pharmaceutically acceptable salts and solvates thereof, the process comprising reacting methyl-4-(4-halo-1-oxobutyl]-α,α-dimethylphenyl acetate with α,α-diphenyl-4-piperidinemethanol in an alkyl nitrile solvent to prepare 4-[4-(4- (hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α,-dimethylbenzene acetic acid alkyl ester, which is further converted into fexofenadine.
- -
-
Page/Page column 9
(2010/01/29)
-
- INDUSTRIAL PROCESS OF FEXOFENADINE HYDROCHLORIDE WITH CONTROLLED SIDE PRODUCTS
-
The present invention relates to a process for the preparation of Anhydrous Fexofenadine Hydrochloride with controlled level of side products. Another aspect of the present invention is purification of Fexofenadine base free of meta isomer of fexofenadine base and fexofenadinone.
- -
-
Page/Page column 10; 13-14
(2008/06/13)
-
- INTERMEDIATES USEFUL FOR THE PREPARATION OF ANTIHISTAMINIC PIPERIDINE DERIVATIVE
-
The present invention relates to process for preparing antihistaminic piperidine derivative, specifically fexofenadine and its pharmaceutically acceptable salts by using novel synthetic intermediates of following formula (I), wherein R is lower alkyl; R2 is H, cyclopropyl, R1is alkyl, 4-(hydroxy-dipheτiyl-methyl)-piperidin-l-yl.
- -
-
Page/Page column 19
(2008/06/13)
-
- A PROCESS FOR THE PREPARATION OF HIGHLY PURE ANHYDROUS FEXOFENADINE HYDROCHLORIDE
-
The present invention relates to a novel and industrially advantageous process for the preparation of highly pure anhydrous Fexofenadine hydrochloride directly from fexofenadine base without isolating hydrous Fexofenadine hydrochloride.
- -
-
Page/Page column 6-7; 9
(2008/06/13)
-
- FEXOFENADINE CRYSTAL FORM AND PROCESSES FOR ITS PREPARATION THEREOF
-
Provided is a crystalline form of fexofenadine free base and processes for its preparation.
- -
-
Page/Page column 10
(2008/06/13)
-
- Fexofenadine polymorphs and process for the preparation thereof
-
The invention provides novel crystalline forms of fexofenadine hydrochloride, a process for the preparation of the novel forms and of the known form A, and their use in therapy.
- -
-
Page/Page column 4
(2008/06/13)
-
- CRYSTALLINE FORMS OF FEXOFENADINE HYDROCHLORIDE AND PROCESSES FOR THEIR PREPARATION
-
Provided are crystalline forms of fexofenadine hydrochloride and processes for their preparation.
- -
-
Page/Page column 18; 19-20; 22
(2008/06/13)
-
- Fexofenadine polymorphs and process for the preparation thereof
-
The invention provides novel crystalline forms of fexofenadine hydrochloride, a process for the preparation of the novel forms and of the known form A, and their use in therapy.
- -
-
Page/Page column 3
(2008/06/13)
-
- FEXOFENADINE POLYMORPHS AND PROCESSES OF PREPARING THE SAME
-
Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith.
- -
-
Page/Page column 28
(2008/06/13)
-
- METHOD OF PREPARATION OF TERFENADINE AND ITS DERIVATIVES
-
The invention relates to a new method of preparation of derivatives of piperidinyl butylphenylacetic acids. The compounds are histaminically active. The substances are prepared by Grignard reaction of alkylhalohydrins and suitably substituted aromatic aldehydes. The resulting diols are subjected to subsequent substitution reaction.
- -
-
-
- POLYMORPHIC FORM XVI OF FEXOFENADINE HYDROCHLORIDE
-
Provided is a crystalline (polymorphic) form of fexofenadine hydrochloride, denominated fexofenadine hydrochloride Form XVI.
- -
-
-
- Polymorphs of fexofenadine hydrochloride
-
The present invention provides novel crystal forms of fexofenadine hydrochloride Forms V, VI and VIII through XV and processes for their preparation and preparation of amorphous form and other crystalline forms of fexofenadine hydrochloride. Forms XIV and XV are solvates of ethyl acetate, while Form IX is a solvate of MTBE or cyclohexane. The forms are useful for administration to humans and animals to alleviate symptoms caused by histamine. The present invention further provides pharmaceutical compositions of the new crystalline forms.
- -
-
-
- Process for preparing anhydrous and hydrate forms of antihistaminic piperidine derivatives
-
The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.
- -
-
-
- Process for the preparation of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethly)-1-piperidinyl]-butyl]-alpha,alpha-dimethylbenzeneacetic acid
-
A process for the preparation of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-butyl]-α,α-dimethylbenzeneacetic acid (Fexofenadine) of formula 1
- -
-
-
- Polymorphs of fexofenadine hydrochloride
-
The present invention provides novel crystal forms of fexofenadine hydrochloride Forms V, VI and VIII through XV and processes for their preparation and preparation of amorphous form and other crystalline forms of fexofenadine hydrochloride. Forms XIV and XV are solvates of ethyl acetate, while Form IX is anhydrous, but can be crystallized as a solvate of MTBE or cyclohexane. The forms are useful for administration to humans and animals to alleviate symptoms caused by histamine. The present invention further provides pharmaceutical compositions of the new crystalline forms.
- -
-
-
- Processes for preparing anhydrous and hydrate forms of antihistaminic piperidine derivatives, polymorphs and pseudomorphs thereof
-
The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 12which are useful as antihistamines, antiallergic agents and bronchodilators.
- -
-
-
- Pharmaceutical composition for piperidinoalkanol compounds
-
The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.
- -
-
-
- Process for piperidine derivatives
-
The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators, these piperidine derivatives can be described by the following formulas: STR1 wherein R1 represents hydrogen or hydroxy; R2 represents hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2 ; n is an integer of from 1 to 5; R3 is --CH2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts, hydrates and individual optical isomers thereof.
- -
-
-
