847063-12-1

Basic information

• Product Name: Lorcaserin-L-tartrate (2:1)
• Synonyms: Lorcaserin-L-tartrate (2:1);1H-3-Benzazepine, 8-chloro-2,3,4,5-tetrahydro-1-methyl-, (1R)-,;Lorcaserin Hemi-L-tartrate;Lorcaserin Tartarte;Lorcaserin L-(+)-Tartaric acid;CL263;R-Lorcaserin tartrate(2:1)
• CAS NO: 847063-12-1
• Molecular Formula: C26H34Cl2N2O6
• Molecular Weight: 541.46396
• EINECS: 1312995-182-4
• Product Categories: 5-HT 2c receptor agonist
• Mol File: 847063-12-1.mol
• Article Data: 18

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Lorcaserin-L-tartrate (2:1)(CAS DataBase Reference)
• NIST Chemistry Reference: Lorcaserin-L-tartrate (2:1)(847063-12-1)
• EPA Substance Registry System: Lorcaserin-L-tartrate (2:1)(847063-12-1)

Safety Data

• Hazardous Substances Data: 847063-12-1(Hazardous Substances Data)

Usage

General Description

Lorcaserin-L-tartrate (2:1) is a chemical compound that is commonly used as a weight loss medication. It works by increasing feelings of fullness and reducing food consumption, leading to overall decreased calorie intake. The compound is a combination of lorcaserin, a selective serotonin 2C receptor agonist, and L-tartrate, a salt of the tartaric acid. Lorcaserin-L-tartrate (2:1) is typically prescribed for individuals with obesity or overweight who also have weight-related health issues such as high blood pressure, high cholesterol, or type 2 diabetes.

Upstream product

• 87-69-4 L-Tartaric acid 
• 616201-80-0 (+/-)-Lorcaserin 
• 953789-37-2 1-[[2-(4-chlorophenyl)ethyl]amino]-2-chloropropane hydrochloride 
• 847063-13-2 1-[[2-(4-chlorophenyl)ethyl]amino]-2-hydroxypropane 
• 156-41-2 4-chlorophenylethylamine 
• 140-53-4 p-chlorobenzyl cyanide 
• 616202-92-7 lorcaserin 
• 1247548-14-6 N-(4-chlorophenylethyl)propyl-2-ene-1-amine 
• 167886-56-8 1-[2-(tert-butoxycarbonylamino)ethyl]4-chlorobenzene 
• 1030624-36-2 2-(4-chlorophenyl)-N-(2-hydroxypropyl)acetamide 
• 1878-66-6 4-chlorophenylacetic Acid 
• 824430-78-6 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine L-(+)-tartrate 
• 1006037-59-7 (S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine hydrochloride 
• 616202-81-4 (S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine 

Downstream Products

• 616202-92-7 lorcaserin 
• 846589-98-8 Lorcaserin hydrochloride 
• 824430-78-6 (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine L-(+)-tartrate 
• 1006037-59-7 (S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine hydrochloride 

Relevant articles and documents

Method for preparing lorcaserin

The invention discloses a method for preparing lorcaserin. Specifically, the method comprises the steps: taking p-chlorophenylacetonitrile as an initial raw material, preparing p-chlorophenylethylamine through reduction; carrying out a reaction with p-toluenesulfonyl chloride to form an amino occupying intermediate; enabling the intermediate to carry out a reaction with monochloroacetone under analkaline condition to form N-(2-(4-chlorphenyl)ethyl)-4-methyl-N-(2-propionyl)benzenesulfonamide, and then carrying out reduction, chlorination, p-toluenesulfonyl removal and intramolecular Friedel-Crafts alkylation to synthesize 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzoazepine, carrying out L-(+)-tartaric acid resolution and alkalization on azepine to remove tartaric acid, and acting with hydrogen chloride diethyl ether to salify to prepare lorcaserin. The method has the characteristics of simple synthesis method, good reaction selectivity, high product purity, environmental protectionand low preparation cost.

Preparation method of lorcaserin intermediate

The invention discloses a preparation method of a lorcaserin intermediate (I). According to the preparation method, p-chlorobenzyl cyanide is taken as the primary raw material, and the lorcaserin intermediate (I) is obtained after reduction reactions and condensation reactions. The primary raw materials (p-chlorobenzyl cyanide and 1-chloro-2-propanol) are cheap and easily available; raw materials, which can easily get polluted and are explosive, such as sulfoxide chloride, hydrobromic acid, borane, and the like are not used; the preparation method will not produce a large amount of wastewater and is beneficial for the environment protection; moreover, the requirements on the protection of workers are lowered, and safe production is guaranteed. The route design is novel, the raw materials are easily available, the operation is simple and feasible, and the preparation method is environment-friendly and can be applied to massive industrial production.

PROCESSES FOR THE PREPARATION OF LORCASERIN

The present invention relates to stable crystalline Form A of lorcaserin hydrochloride of Formula (IA) and processes for its preparation. The invention also relates to processes for the preparation of lorcaserin and pharmaceutically acceptable salts, solvates and hydrates thereof.