186694-45-1

Basic information

• Product Name: (R)-Licarbazepine Acetate
• Synonyms: (R)-Licarbazepine Acetate;(10R)-10-(Acetyloxy)-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxaMide;(R)-(+)-10-Acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxaMide;BIA 2-059
• CAS NO: 186694-45-1
• Molecular Formula: C17H16N2O3
• Molecular Weight: 296.32054
• Product Categories: Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Amines, Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals
• Mol File: 186694-45-1.mol
• Article Data: 29

Chemical Properties

• Appearance: /
• CAS DataBase Reference: (R)-Licarbazepine Acetate(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-Licarbazepine Acetate(186694-45-1)
• EPA Substance Registry System: (R)-Licarbazepine Acetate(186694-45-1)

Safety Data

• Hazardous Substances Data: 186694-45-1(Hazardous Substances Data)

Usage

Uses

A promising antiepileptic drug structurally related to Carbamazepine and Oxcarbazepine.

Upstream product

• 28721-07-5 oxcarbazepine 
• 952740-00-0 10-acetoxy-5H-dibenzo[b,f]azepine-5-carboxamide 
• 108-24-7 acetic anhydride 
• 104746-04-5 S-licarbazepine 
• 108-05-4 vinyl acetate 
• 29331-92-8 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide 
• 108-22-5 Isopropenyl acetate 
• 127-08-2 potassium acetate 
• 1346462-62-1 (R)-((S)-5-carbamoyl-10,11-dihydro-5H-dibenzo[b,f]azepin-10-yl) 1-benzylpyrrolidine-2-carboxylate 
• 475674-43-2 C₂₃H₂₂N₂O₉ 
• 4698-11-7 10-methoxy-5H-dibenzo[b,f]azepine 
• 21737-58-6 10,11-dihydro-5H-dibenzo[b,f]azepin-10-one 
• 1189-71-5 isocyanate de chlorosulfonyle 
• 1431547-12-4 (S)-10,11-dihydro-5H-dibenzo[b,f]azepin-10-yl acetate 

Downstream Products

• 104746-03-4 R-licarbazepine 
• 186694-45-1 eslicarbazepine acetate 
• 36507-30-9 carbamazepine 10,11-epoxide 

Relevant articles and documents

Synthesis method of high-purity stable crystal form of escilitalopine acetate

The present invention discloses a high-purity method for the synthesis of escitazepine acetate and a novel stable crystal form thereof. The preparation method disclosed in the present invention is achieved by the following steps: 10-methoxyiminopyrene as the starting material, the starting material is dissolved in acetone and deprotected to form 10-carbonyliminocarbenzene; the use of dichloromethane, borane dimethyl sulfide, (R)-2-methyl -CBS- oxazoleboran asymmetrical reduction to generate (10S)-10-hydroxyiminopyrene; (10S)-10-hydroxyiminostilbeneylated into esters, amidated with chlorosulfonyl isocyanate, To obtain escilitalopine acetate and a stable new crystal form. The preparation method provided by the present invention is simple synthesis process, few reaction steps, less pollution, raw materials are readily available and inexpensive, the final product is easy to purify and separate and the crystal form is stable, and the industrial application prospects are broad.

NOVEL CRYSTALLINE FORM OF ESLICARBAZEPINE

The present invention provides novel crystalline form L1 of eslicarbazepine characterized by diffraction peaks at 7.09, 10.03, 11.73, 14.12, 16.94, 18.03, 20.00, 23.20, 23.58, 23.76, 26.05, 26.52, 28.37, 29.90, 31.42±0.2 degree two theta in an X-ray diffraction pattern. The present invention further provides conversion of crystalline form L1 of eslicarbazepine to eslicarbazepine acetate.

Brain-targeting eslicarbazepine ester prodrug and application thereof

The invention relates to an eslicarbazepine ester prodrug and an application thereof, wherein the prodrug is a compound represented by the formula (I) or optical isomers or physiologically acceptable salts of the compound represented by the formula (I), wherein R represents a lipophilic substituent. The compound represented by the formula (I) is the eslicarbazepine ester prodrug containing the lipophilic substituent, is converted into eslicarbazepine through metabolism in vivo to play pharmacological effects, and can be applied in preparation of drugs for treatment, prevention or adjuvant treatment of central nervous system diseases, such as epilepsy and the like.