448904-47-0

Basic information

• Product Name: DESVENLAFAXINE SUCCINATE
• Synonyms: Desvenlafaxine (O-DesMethyl Venlafaxine) Succinate;O-Desmethylvenlafaxine succinate;O-DESMETHYL VENLAFAXINE SUCCINATE IMPURITIES;O-DESMETHYL VENLAFAXIN SUCCINATE
• CAS NO: 448904-47-0
• Molecular Formula: C₄H₆O₄*C₁₆H₂₅NO₂
• Molecular Weight: 381.47
• Mol File: 448904-47-0.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: DESVENLAFAXINE SUCCINATE(CAS DataBase Reference)
• NIST Chemistry Reference: DESVENLAFAXINE SUCCINATE(448904-47-0)
• EPA Substance Registry System: DESVENLAFAXINE SUCCINATE(448904-47-0)

Safety Data

• Hazardous Substances Data: 448904-47-0(Hazardous Substances Data)

Usage

Uses

WY 45233 Succinate has been used in the treatment of major depressive disorder (MDD).

Upstream product

• 110-15-6 succinic acid 
• 93413-62-8 O-desmethylvenlafaxine 
• 104-47-2 p-methoxybenzylnitrile 
• 108-94-1 cyclohexanone 
• 99300-78-4 venlafaxine hydrochloride 
• 93413-69-5 1-[2-dimethylamino-1-(4-methoxyphenyl)ethyl]cyclohexanol 

Downstream Products

• 386750-22-7 [2-(1-hydroxycyclohexyl)-2-(4-hydroxyphenyl)ethyl]dimethylammonium 3-carboxypropanoate monohydrate 

Relevant articles and documents

POLYMORPHIC FORMS OF O-DESMETHYL-VENLAFAXINE SUCCINATE FIELD OF THE INVENTION

The present invention discloses polymorphic forms of O-desmethyl-venlafaxine succinate and processes for the preparation thereof.

POLYMORPHIC FORMS OF O-DESMETHYL-VENLAFAXINE SUCCINATE

The present invention discloses polymorphic forms of O-desmethyl-venlafaxine succinate and processes for the preparation thereof.

PROCESS FOR THE PREPARATION OF O-DESMETHYL-VENLAFAXINE AND SALTS THEREOF

The present invention relates to a novel process for the preparation of O-desmethyl venlafaxine (ODV) and the pharmaceutically acceptable salts thereof, wherein it comprises (i) provision of spiro-venlafaxine compound as intermediate; (ii) conversion of spiro-venlafaxine intermediate into ODV free base in a one-pot process; and (iii) optionally conversion ODV free base into pharmaceutically acceptable salts. The present invention further relates to novel processes for the preparation of crystalline salts of OD V-succinate and ODV-oxalate.

A METHOD OF PREPARATION OF DESVENLAFAXINE AND ITS SALTS

A method of preparation of 4-(2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl)phenol of formula (I), known under the generic name desvenlafaxine, and its pharmaceutically acceptable salts, which comprises (a) stirring up O-benzyl desvenlafaxine or its derivative of formula (II), or its salt, where R is selected from H, 4-methyl, 4-methoxy, 3,4-dimethoxy, 2-nitro, 4-nitro, 4-chloro, 4-bromo, 2,6-dichloro and 2,6-difluoro, in an organic solvent or a mixture of organic solvents, followed by dissolution of the starting substance at pH 3 to 8; (b) transformation of O-benzyl desvenlafaxine or its derivative of formula (II) to desvenlafaxine (I) by catalytic hydrogenation; (c) removing the catalyst from the desvenlafaxine solution with the pH value of 3 to 8 by filtration, followed by increasing pH to a value higher than 8 and lower than 11 by addition of an inorganic or organic base; (d) isolation of desvenlafaxine base (I) by filtration; and (e) transformation of desvenlafaxine base (I) to a pharmaceutically acceptable salt.

Method for preparation of o-desmethylvenlafaxine using polythiolates

This invention relates to methods of making O-desmethylvenlafaxine from venlafaxine. In the methods venlafaxine is contacted with a polythiolate. The polythiolate may be prepared from the corresponding polythiol in the presence of base. The present methods provide the O-desmethylvenlafaxine in good yields and high purity and are suitable for use on an industrial scale.

PROCESS FOR SYNTHESIZING DESVENLAFAXINE FREE BASE AND SALTS OR SOLVATES THEREOF

The invention relates generally to an improved process for manufacturing desvenlafaxine free base and salts or solvates thereof.

POLYMORPHS OF O-DESMETHYL VENLAFAXINE SUCCINATE

The present invention relates to crystalline forms of O-desmethyl venlafaxine (ODV) succinate monohydrate, namely Forms I and II, in pure form and to novel processes for their preparation. The present invention provides a process for the preparation of Form II free of Form I and a process for the preparation of Form I free of Form II. The present invention provides direct methods for the preparation of ODV succinate Form II from ODV free base and for the preparation of ODV succinate Form I from ODV free base.

NOVEL PROCESS FOR PREPARATION OF O-DESMETHYLVENLAFAXINE

The present invention relates to the novel processes for the preparation of 4-(2- (dimethylamino)-1-(1-hydroxycyclohexyl)ethyl)phenol, commonly known as O- desmethylvenlafaxine of formula (I) and its pharmaceutically acceptable salts thereof The present invention also relates to the novel process for the preparation of O- desmethylvenlafaxine of formula (I) and its pharmaceutically acceptable salts thereof formula (V) or formula (VI) formula (I) or formula (VII) wherein, R is hydrogen, methoxyethoxymethyl (MEM), methoxymethyl (MOM), aryloyl, arylsulfonyl, tetrahydropyranyl or substituted silyl.

Processes for the preparation of odesmethylvenlafaxine, free from its dimer impurities

The present invention provides isolated O-desmethylvenlafaxine impurities ODV-Dimer and ODV-N-Dimer, their use as a reference marker and reference standard, and a process for the preparation of O-desmethylvenlafaxine free from said impurities

PROCESS FOR PRODUCING 1-[2-(DIMETHYLAMINO)-1-(4-PHENOL)ETHYL]CYCLOHEXANOL

The present invention relates to an improved, process for large scale production of 1-[2-(dimethylamino)-1-(4-phenol)ethyl]cyclohexanol (O- desmethylvenlafaxine) or its pharmaceutically acceptable salts with increased yield and minimal impurities.