515114-52-0

Upstream product

• 1369205-81-1 toluene-4-sulfonic acid 3-(3-dimethylamino-1-ethyl-1-hydroxy-2-methylpropyl)phenyl ester 
• 1369205-84-4 toluene-4-sulfonic acid 3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenyl ester 
• 1369205-80-0 toluene-4-sulfonic acid 3-propionylphenyl ester 
• 50-00-0 formaldehyd 
• 1369205-83-3 toluene-4-sulfonic acid 3-[1-(2-dimethylamino-1-methylethyl)propenyl]phenyl ester 
• 1369205-94-6 toluene-4-sulfonic acid 3-(3-dimethylamino-2-methylpropionyl)phenyl ester 
• 1343471-61-3 rac-3-(dimethylamino)-1-(3-hydroxyphenyl)-2-methylpropan-1-one 
• 13103-80-5 1-(3-hydroxyphenyl)propan-1-one 
• 1313429-14-9 2-cyano-3-(3-methoxy-phenyl)-pentanoic acid ethyl ester 
• 1313374-17-2 N,N-dimethyl-2-methyl-3-(3-methoxyphenyl)valeramide 
• 1313429-27-4 3-(3-methoxy-phenyl)-2-methyl-pentanoic acid ethyl ester 
• 1616-70-2 2-methyl-3-(3-methoxyphenyl)valeric acid 
• 1313429-25-2 2-cyano-3-(3-methoxy-phenyl)-2-methyl-pentanoic acid 
• 1313429-24-1 2-methyl-3-(3-methoxyphenyl)pentanenitrile 

Downstream Products

• 175591-09-0 3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol hydrochloride 
• 1243574-48-2 C₂₄H₄₀N₂O₄ 
• 175591-09-0 tapentadol hydrochloride 
• 175591-23-8 tapentadol 
• 1314003-87-6 (rac)-tapentadol-PABA carbamate tert-butyl ester 

Relevant academic research and scientific papers

Novel Intermediate Used for Preparing Tapentadol or Analogues Thereof

The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.

Compounds and Methods for Preparing Substituted 3-(1-amino-2-methylpentane-3-yl)phenyl Compounds

Compounds and methods for preparing substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds from an isomerically pure starting material are described. In particular, methods of preparing a 3-(1-(dimethylamino)-2-methylpentane-3-yl)phenol as a substan

PROCESS FOR PREPARING L-PHENYL-3-DIMETHYLAMINOPROPANE DERIVATIVE

Provided is a process for the preparing 1-phenyl-3-dimethylaminopropane derivatives of formula I, (The formula should be inserted here) and its pharmaceutically acceptable salts thereof via novel intermediates.

NOVEL INTERMEDIATE USED FOR PREPARING TAPENTADOL OR ANALOGUES THEREOF

The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.

PROCESS FOR PREPARING L-PHENYL-3-DIMETHYLAMINOPROPANE DERIVATIVE

Provided is a process for the preparing l-phenyl-3-dimethylaminopropane derivatives of formula I, (The formula should be inserted here) and its pharmaceutically acceptable salts thereof via novel intermediates.

PROCESS FOR THE PREPARATION OF 1-PHENYL-3-DIMETHYLAMINOPROPANE DERIVATIVES

A process for the preparation of 1-phenyl-3-dimethylaminopropane derivatives of formula (I) and its pharmaceutically acceptable salts thereof from cyano intermediate of formula (II), wherein R1 can be selected from -OR2, halo, -CH2OR2, -SR2, -SOR2, SO2R2, -SO3H, -NO2, -NR2R2', -CONR2R2', carboxylic esters, sulfonate esters or phosphate esters, R2 and R2' can be same or different, and can be selected from hydrogen, alkyl, aryl, aralkyl, heteroaryl, -COR2", -P03(R2")2 wherein R2" can be selected from alkyl, aryl, aralkyl, heteroaryl and the like.

Pharmaceutical Combination

A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.

AMINO ACID AND PEPTIDE CARBAMATE PRODRUGS OF TAPENTADOL AND USES THEREOF

Prodrugs of tapentadol with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing pain relief with the tapentadol prodrugs are provided herein. Prodrugs having side chains of valine, leucine, isoleucine and glycine amino acids and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with tapentadol administration, as well as increasing the oral bioavailability of tapentadol are provided herein.

Combination of selected opioids with muscarine antagonists for treating urinary incontinence

Active compound combinations of compounds of group A, particularly opioids, and compounds of group B, particularly anti-muscarine agents and other substances suitable for treatment of an increased urge to urinate or urinary incontinence. Related pharmaceutical formulations and methods of treatment of an increased urge to urinate or urinary incontinence are also provided.