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616202-92-7

616202-92-7

Identification

  • Product Name:Lorcaserin

  • CAS Number: 616202-92-7

  • EINECS:809-254-4

  • Molecular Weight:195.692

  • Molecular Formula: C11H14ClN

  • HS Code:2933990090

  • Mol File:616202-92-7.mol

Synonyms:(R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine;1H-3-Benzazepine,8-chloro-2,3,4,5-tetrahydro-1-methyl-, (1R)-;

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Safety information and MSDS view more

  • Signal Word:Warning

  • Hazard Statement:H302 Harmful if swallowedH410 Very toxic to aquatic life with long lasting effects

  • First-aid measures: General adviceConsult a physician. Show this safety data sheet to the doctor in attendance.If inhaled If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician. In case of skin contact Wash off with soap and plenty of water. Consult a physician. In case of eye contact Rinse thoroughly with plenty of water for at least 15 minutes and consult a physician. If swallowed Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician.

  • Fire-fighting measures: Suitable extinguishing media Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. Wear self-contained breathing apparatus for firefighting if necessary.

  • Accidental release measures: Use personal protective equipment. Avoid dust formation. Avoid breathing vapours, mist or gas. Ensure adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust. For personal protection see section 8. Prevent further leakage or spillage if safe to do so. Do not let product enter drains. Discharge into the environment must be avoided. Pick up and arrange disposal. Sweep up and shovel. Keep in suitable, closed containers for disposal.

  • Handling and storage: Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Avoid exposure - obtain special instructions before use.Provide appropriate exhaust ventilation at places where dust is formed. For precautions see section 2.2. Store in cool place. Keep container tightly closed in a dry and well-ventilated place.

  • Exposure controls/personal protection:Occupational Exposure limit valuesBiological limit values Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and at the end of workday. Eye/face protection Safety glasses with side-shields conforming to EN166. Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). Skin protection Wear impervious clothing. The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique(without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and the standard EN 374 derived from it. Respiratory protection Wear dust mask when handling large quantities. Thermal hazards

Supplier and reference price

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  • Manufacture/Brand:Usbiological
  • Product Description:Lorcaserin
  • Packaging:50mg
  • Price:$ 335
  • Delivery:In stock
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  • Manufacture/Brand:DC Chemicals
  • Product Description:Lorcaserin 99%
  • Packaging:1 g
  • Price:$ 600
  • Delivery:In stock
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  • Manufacture/Brand:DC Chemicals
  • Product Description:Lorcaserin 99%
  • Packaging:100 mg
  • Price:$ 150
  • Delivery:In stock
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  • Manufacture/Brand:DC Chemicals
  • Product Description:Lorcaserin 99%
  • Packaging:250 mg
  • Price:$ 300
  • Delivery:In stock
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  • Manufacture/Brand:Biosynth Carbosynth
  • Product Description:Lorcaserin
  • Packaging:50 mg
  • Price:$ 225
  • Delivery:In stock
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  • Manufacture/Brand:Biosynth Carbosynth
  • Product Description:Lorcaserin
  • Packaging:10 mg
  • Price:$ 85
  • Delivery:In stock
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  • Manufacture/Brand:American Custom Chemicals Corporation
  • Product Description:LORCASERIN 95.00%
  • Packaging:10MG
  • Price:$ 750.75
  • Delivery:In stock
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  • Manufacture/Brand:American Custom Chemicals Corporation
  • Product Description:LORCASERIN 95.00%
  • Packaging:100MG
  • Price:$ 1963.5
  • Delivery:In stock
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  • Manufacture/Brand:Abosyn
  • Product Description:(1R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine 98%-99%
  • Packaging:5g
  • Price:$ 1760
  • Delivery:In stock
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  • Manufacture/Brand:Abosyn
  • Product Description:(1R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine 98%-99%
  • Packaging:1g
  • Price:$ 760
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Relevant articles and documentsAll total 37 Articles be found

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.

Niclosin hydrochloride pellet, and preparation method and preparation thereof

-

Paragraph 0049; 0084; 0088, (2020/05/14)

A lorcaserin hydrochloride mini-pill is provided. The mini-pill comprises a blank pill core, a medicine loading layer, a slow-release layer and a quick-release layer in order from inside to outside. The medicine loading layer comprises lorcaserin hydrochloride, lactose monohydrate, highly substituted hydroxypropylcellulose and talcum powder. The slow-release layer comprises ethyl cellulose, highly substituted hydroxypropylcellulose, talcum powder and triethyl citrate. The quick-release layer comprises lorcaserin hydrochloride, lactose monohydrate, highly substituted hydroxypropylcellulose and talcum powder. The mass ratio of the sum of the weight of the blank pill core and the weight of the medicine loading layer to the mass of the slow-release layer is 1:(0.25-0.35). The mini-pill comprises the slow-release layer and the quick-release layer, and therefore a medicine can rapidly work and functions of the medicine in a body are prolonged. A preparing method of the lorcaserin hydrochloride mini-pill and a preparation of the lorcaserin hydrochloride mini-pill are also provided.

Method for preparing lorcaserin

-

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.

A new enantioselective synthesis of antiobesity drug lorcaserin

Ghotekar, Ganesh S.,More, Devidas A.,Nalla, Viswanadh,Muthukrishnan

, p. 16876 - 16880 (2019/11/14)

A simple and efficient enantioselective synthesis of anti-obesity drug lorcaerin starting from easily accessible 3-chlorostyrene oxide has been described for the first time employing hydrolytic kinetic resolution as a source of chirality. The protocol might also be useful in the synthesis of structural variants of lorcaserin.

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

-

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.

Process route upstream and downstream products

Process route

(1S)-N-trifluoroacetyl-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine
616202-78-9

(1S)-N-trifluoroacetyl-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine
616202-81-4,616202-92-7

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine

Conditions
Conditions Yield
With methanol; sodium hydroxide; water; at 20 ℃; for 2.66667h;
99%
With sodium hydroxide; In methanol; water; at 20 ℃; for 2.66667h;
99%
With sodium hydroxide; In methanol; at 60 ℃; for 3.5h;
tert-butyl (S)-8-chloro-1-methyl-1,2-dihydro-3H-benzo[d]azepine-3-carboxylate

tert-butyl (S)-8-chloro-1-methyl-1,2-dihydro-3H-benzo[d]azepine-3-carboxylate

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine
616202-81-4,616202-92-7

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine

Conditions
Conditions Yield
With triethylsilane; trifluoroacetic acid; In dichloromethane; at 20 ℃; for 2h; Schlenk technique; Inert atmosphere;
N-(4-chlorophenylethyl)-2-chloropropanamide
34164-14-2

N-(4-chlorophenylethyl)-2-chloropropanamide

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine
616202-81-4,616202-92-7

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine

Conditions
Conditions Yield
Multi-step reaction with 3 steps
1: AlCl3 / 150 - 200 °C
2: BH3 / diethyl ether
3: chiral HPLC
With aluminium trichloride; borane; In diethyl ether; 1: Friedel-Crafts cyclization;
4-chlorophenylethylamine
156-41-2

4-chlorophenylethylamine

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine
616202-81-4,616202-92-7

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine

Conditions
Conditions Yield
Multi-step reaction with 4 steps
1: pyridine / CH2Cl2
2: AlCl3 / 150 - 200 °C
3: BH3 / diethyl ether
4: chiral HPLC
With pyridine; aluminium trichloride; borane; In diethyl ether; dichloromethane; 2: Friedel-Crafts cyclization;
8-chloro-1-methyl-4,5-dihydro-1H-benzo[d]azepin-2(3H)-one
824430-77-5

8-chloro-1-methyl-4,5-dihydro-1H-benzo[d]azepin-2(3H)-one

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine
616202-81-4,616202-92-7

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine

Conditions
Conditions Yield
Multi-step reaction with 2 steps
1: BH3 / diethyl ether
2: chiral HPLC
With borane; In diethyl ether;
(+/-)-Lorcaserin
616201-80-0,616202-92-7

(+/-)-Lorcaserin

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine
616202-81-4,616202-92-7

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine

lorcaserin
616202-92-7

lorcaserin

Conditions
Conditions Yield
chiral HPLC;
(+/-)-Lorcaserin
616201-80-0,616202-92-7

(+/-)-Lorcaserin

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine
616202-81-4,616202-92-7

(S)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine

lorcaserin
616202-92-7

lorcaserin

Conditions
Conditions Yield
chiral HPLC;
1-[[2-(4-chlorophenyl)ethyl]amino]-2-chloropropane hydrochloride
953789-37-2

1-[[2-(4-chlorophenyl)ethyl]amino]-2-chloropropane hydrochloride

(+/-)-Lorcaserin
616201-80-0,616202-92-7

(+/-)-Lorcaserin

Conditions
Conditions Yield
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 120 - 125 ℃; Inert atmosphere;
99%
With aluminum (III) chloride; at 120 - 125 ℃; for 3h; Inert atmosphere; Large scale;
97%
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 135 - 140 ℃;
96.1%
With aluminum oxide; In 1,2-dichloro-benzene; at 130 - 140 ℃; Inert atmosphere;
96.1%
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 140 ℃; for 10h;
95%
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 125 - 130 ℃; for 3h;
90%
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 130 ℃; for 16h; Solvent;
78.2%
1-[[2-(4-chlorophenyl)ethyl]amino]-2-chloropropane hydrochloride; With aluminum (III) chloride; In 1,2-dichloro-benzene; at 125 - 130 ℃; for 14 - 18h;
With water; In 1,2-dichloro-benzene; at 60 ℃;
With sodium hydroxide; In cyclohexane; water; at 20 ℃; for 1h; pH=>= 13;
1-[[2-(4-chlorophenyl)ethyl]amino]-2-chloropropane hydrochloride; With aluminum (III) chloride; In 1,2-dichloro-benzene; at 125 - 130 ℃; for 14 - 18h;
With sodium hydroxide; In cyclohexane; water; pH=> 13;
1-[[2-(4-chlorophenyl)ethyl]amino]-2-chloropropane hydrochloride; aluminum (III) chloride; In 1,2-dichloro-benzene; at 125 - 130 ℃; for 14 - 18h; Industry scale;
With sodium hydroxide; In cyclohexane; water; at 20 ℃; for 0.5h; Industry scale;
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 126 ℃; for 16h; Temperature; Inert atmosphere; Large scale;
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 120 ℃;
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 150 ℃; for 1h; Temperature; Reagent/catalyst;
N-allyl-N-(4-chlorophenethyl)carbamic acid tert-butyl ester

N-allyl-N-(4-chlorophenethyl)carbamic acid tert-butyl ester

(+/-)-Lorcaserin
616201-80-0,616202-92-7

(+/-)-Lorcaserin

Conditions
Conditions Yield
With aluminum (III) chloride; In chlorobenzene; at 110 ℃; Solvent; Temperature;
81.6%
Multi-step reaction with 2 steps
1: hydrogenchloride / ethyl acetate / 20 °C / pH 2 / Large scale
2: aluminum (III) chloride / 1,2-dichloro-benzene / 4 h / 110 °C / Inert atmosphere; Large scale
With hydrogenchloride; aluminum (III) chloride; In ethyl acetate; 1,2-dichloro-benzene; 2: |Friedel-Crafts Alkylation;
Multi-step reaction with 2 steps
1: hydrogenchloride / ethyl acetate / 20 °C
2: aluminum (III) chloride / 1,2-dichloro-benzene / 110 °C
With hydrogenchloride; aluminum (III) chloride; In ethyl acetate; 1,2-dichloro-benzene; 2: |Friedel-Crafts Alkylation;
Multi-step reaction with 2 steps
1: dichloromethane / 25 °C
2: aluminum (III) chloride / 1,2-dichloro-benzene / 110 °C
With aluminum (III) chloride; In dichloromethane; 1,2-dichloro-benzene; 2: |Friedel-Crafts Alkylation;
Multi-step reaction with 2 steps
1: hydrogenchloride / water; ethyl acetate / 20 °C
2: aluminum (III) chloride / 1,2-dichloro-benzene / 110 °C
With hydrogenchloride; aluminum (III) chloride; In water; ethyl acetate; 1,2-dichloro-benzene;
N-(4-chlorophenylethyl)propyl-2-ene-1-amine hydrochloride

N-(4-chlorophenylethyl)propyl-2-ene-1-amine hydrochloride

(+/-)-Lorcaserin
616201-80-0,616202-92-7

(+/-)-Lorcaserin

Conditions
Conditions Yield
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 110 ℃; for 4h; Solvent; Temperature; Reagent/catalyst; Inert atmosphere; Large scale;
92.3%
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 110 ℃;
84.5%
With aluminum (III) chloride; In 1,2-dichloro-benzene; at 110 ℃;
84.5%
With zinc(II) chloride; at 125 ℃; for 6.41667h; Reagent/catalyst;
230 mg

Global suppliers and manufacturers

Global( 171) Suppliers
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  • Hangzhou Dingyan Chem Co., Ltd
  • Business Type:Manufacturers
  • Contact Tel:86-571-86465881,86-571-87157530,86-571-88025800
  • Emails:sales@dingyanchem.com
  • Main Products:95
  • Country:China (Mainland)
  • Chemwill Asia Co., Ltd.
  • Business Type:Manufacturers
  • Contact Tel:021-51086038
  • Emails:sales@chemwill.com
  • Main Products:55
  • Country:China (Mainland)
  • Amadis Chemical Co., Ltd.
  • Business Type:Lab/Research institutions
  • Contact Tel:86-571-89925085
  • Emails:sales@amadischem.com
  • Main Products:29
  • Country:China (Mainland)
  • Shaanxi BLOOM TECH Co.,Ltd
  • Business Type:Lab/Research institutions
  • Contact Tel:+86-29-86470566
  • Emails:sales@bloomtechz.com
  • Main Products:79
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  • Shanghai Upbio Tech Co.,Ltd
  • Business Type:Lab/Research institutions
  • Contact Tel:+86-21-52196435
  • Emails:upbiocn@hotmail.com
  • Main Products:88
  • Country:China (Mainland)
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