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616202-92-7

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616202-92-7 Usage

Weight loss drugs

Lorcaserin is a new drug for the treatment of obesity , belonging to oral potent selective serotonin 2C receptor agonists, lorcaserin hydrochloride is successfully developed by the US company Arena, on June 27, 2012 by the US FDA it is approved for marketing, as adjuvant therapy for obesity or merge with at least one weight-related complications in overweight adults in low-calorie diet and exercise basis . Clinical studies show that the drug can reduce weight of obesity and overweight patients ,it can improve obesity-related metabolic parameters, and it is well tolerated. Lorcaserin affinity for the 5-HT2c 100 times higher than the 5-HT2B (valvular heart disease risk) ,it has good safety,it is the first FDA-approved weight-loss drug after 1999 . In a year of Lorcaserin treatment, the average weight loss ranges from 3 to 3.7 percent.

Drug Interactions

Due to the theoretical possibility of the mechanism of lorcaserin and serotonin syndrome, when lorcaserin is used in combination with the serotonergic neurotransmitter system drugs, extreme caution should be paid, including triptans monoamine oxidase inhibitor agent selective serotonin reuptake inhibitor selective serotonin and norepinephrine reuptake inhibitors, tricyclic antidepressants bupropion dextromethorphan, lithium tramadol and St. John's wort , etc. In addition, when the present product with CYP2D6 substrates when combined with the need to be cautious, because the product can increase the exposure of these drugs. The above information is edited by the lookchem of Tian Ye.

safety

Lorcaserin has good tolerability and safety, lorcaserin is used in non-diabetic patients, the most common adverse reactions are headache, dizziness, fatigue, nausea, dry mouth and constipation. This product is used in patients with diabetes, common adverse reactions are headache, back pain, cough, low blood sugar and fatigue.studies have found that lorcaserin and placebo are Similar in the proportion of serious adverse reactions, lorcaserin does not increase the incidence of valvular heart disease. After lorcaserin treatment , the incidence of depression is lower , the research shows that the proportion of depression led by lorcaserin 10mgbid, 10mgqd and placebo are 1.9%, 1.1% and 1.8%, emotional low incidence rates are 0.6%, 0.9% and 0.9%, the proportion of suicidal thoughts are 0.9%, 0.6% and 0.7% .the product is pregnancy X-class , pregnant women are disabled; whether this product is secreted by milk is unknown, breast-feeding women need to weigh on the use of the drug; this product is not recommended for children.

Uses

Different sources of media describe the Uses of 616202-92-7 differently. You can refer to the following data:
1. diet pills. Lorcaserin was used to treat Opioid Use Disorder (OUD).
2. Lorcaserin was used to treat Opioid Use Disorder (OUD).
3. A novel selective 5-HT2C-receptor agonist for the treatment of obesity.

Chemical Properties

Yellow Oil

Definition

ChEBI: A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine substituted at position 1 by a methyl group and a t position 6 by a chloro group.

Mechanism of action

Lorcaserin acts at 5-HT2C receptors in the central nervous system (CNS), particularly the hypothalamus, to reduce appetite.

Side effects

constipationdry mouthexcessive tirednesspain in the back or musclesheadachedizzinessdifficulty falling asleep or staying asleepanxiety

Synthesis

The synthesis of?LORCASERIN is as follows:Liquid precursor 53 11-HCl (0.5mmol) was placed into a test tube equipped with a magnetic stir bar. Anhydrous 44 AlCl3?(1.75 equiv according to starting material) was added and efficiently mixed to obtain a paste. The mixture was slowly heated (10°C/min) to 150°C and stirred overnight. A saturated solution of 54 NaCl was added and the mixture was cooled. The pH was adjusted to 9.5-10 using 1M NaOH and then extracted with EtOAc. The combined organic phases were washed with brine, dried over Na2SO4?and the solvent was evaporated under reduced pressure. The obtained crude mixture was analyzed using?1H NMR spectroscopy (estimated yield by?1H NMR was 62%).

Check Digit Verification of cas no

The CAS Registry Mumber 616202-92-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,1,6,2,0 and 2 respectively; the second part has 2 digits, 9 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 616202-92:
(8*6)+(7*1)+(6*6)+(5*2)+(4*0)+(3*2)+(2*9)+(1*2)=127
127 % 10 = 7
So 616202-92-7 is a valid CAS Registry Number.
InChI:InChI=1/C11H14ClN/c1-8-7-13-5-4-9-2-3-10(12)6-11(8)9/h2-3,6,8,13H,4-5,7H2,1H3/t8-/m0/s1

616202-92-7SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 13, 2017

Revision Date: Aug 13, 2017

1.Identification

1.1 GHS Product identifier

Product name lorcaserin

1.2 Other means of identification

Product number -
Other names Apd356

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:616202-92-7 SDS

616202-92-7Relevant articles and documents

Design of oxa-spirocyclic PHOX ligands for the asymmetric synthesis of lorcaserin: Via iridium-catalyzed asymmetric hydrogenation

Ye, Xiang-Yu,Liang, Zhi-Qin,Jin, Cong,Lang, Qi-Wei,Chen, Gen-Qiang,Zhang, Xumu

supporting information, p. 195 - 198 (2021/01/14)

Phosphine-oxazoline (PHOX) ligands are a very important class of privileged ligands in asymmetric catalysis. A series of highly rigid oxa-spiro phosphine-oxazoline (O-SIPHOX) ligands based on O-SPINOL was synthesized efficiently, and their iridium complexes were synthesized by coordination of the O-SIPHOX ligands to [Ir(cod)Cl]2 in the presence of sodium tetrakis-3,5-bis(trifluoromethyl)phenylborate (NaBArF). The cationic iridium complexes showed high reactivity and excellent enantioselectivity in the asymmetric hydrogenation of 1-methylene-tetrahydro-benzo[d]azepin-2-ones (up to 99% yield and up to 99% ee). A key intermediate of the anti-obesity drug lorcaserin could be efficiently synthesized using this protocol.

Method for preparing lorcaserin

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Paragraph 0029-0034, (2020/08/22)

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.

MODIFIED-RELEASE DOSAGE FORMS OF 5-HT2C AGONISTS USEFUL FOR WEIGHT MANAGEMENT

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Paragraph 1180; 1187; 1193, (2019/05/30)

The present invention relates to methods for weight management that utilize modified-release dosage forms comprising (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts and crystalline forms thereof. The present invention further relates to (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts, crystalline forms thereof and modified-release dosage forms comprising them.

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