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inquiryProductName: (R)-1H-3-BENZAZEPINE,8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-,HYDROCHLORIDESynonyms:(R)-1H-3-BENZAZEPINE,8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-,HYDROCHLORIDE;LORCASERINHCL;Lorc… Founded in 2014, as a professional international pha
Jinlan Pharm-Drugs Technology Co.,Limited (with its export company Hangzhou Royall Import & Export Co.,Ltd.)is located in Hangzhou, Zhejiang Province. Neighboring Ningbo port, Shanghai port, Hangzhou Xiaoshan Int’l Airport and Shanghai Pu
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inquiryUnique advantages Guaranteed purity High quality & competitive price Quality control Fast feedback Prompt shipment Appearance:White powder Storage:cool dry place Package:1kg/foil bag;25kg/drum Application:medicine raw material Transportatio
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inquiryName: (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine hydrochloride CAS:846589-98-8 MF: C11H14ClN·ClH Appearance:White Powder Storage:Store in cool and dry place, away from sun light. Package:25kg Application:API Transportation:B
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inquiry(R)-1H-3-BENZAZEPINE,8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-,HYDROCHLORIDE CAS: 846589-98-8 Specification tests specifications results assay 98% 98% appearance
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inquiryAppearance:White or almost white crystalline powder Storage:3 years if properly stored Package:25 kgs/ fiber drum or according to customer's demand Application:Lorcaserin hydrochloride as an addition to a reduced-calorie diet and exercise, for chron
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inquiryLorcaserin hydrochloride
Conditions | Yield |
---|---|
Stage #1: 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine L-(+)-tartrate With sodium hydroxide In dichloromethane; water at 10 - 30℃; for 1h; Stage #2: With hydrogenchloride In ethyl methyl ether at 0 - 10℃; pH=1.5 - 2.5; | 98.6% |
Multi-step reaction with 2 steps 1.1: sodium hydroxide / water; dichloromethane; tert-butyl alcohol 1.2: 90 - 100 °C / Inert atmosphere 1.3: 10 h / 20 °C 2.1: sodium hydroxide / water / 0.17 h / 20 °C 2.2: 0.08 h / 20 °C View Scheme |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride In methanol; water at 0 - 5℃; Solvent; Concentration; | 98% |
With hydrogenchloride In water; ethyl acetate pH=<= 5; pH-value; Large scale; | 98% |
With hydrogenchloride In dichloromethane; water at 20℃; for 0.166667h; | 97% |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Stage #1: (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hemitartrate With potassium carbonate In water; ethyl acetate at 15℃; Large scale; Stage #2: With hydrogenchloride In water; ethyl acetate pH=<= 5; Temperature; Large scale; | 98% |
Stage #1: (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hemitartrate With potassium carbonate In water; ethyl acetate at 20 - 25℃; for 0.5 - 0.666667h; Stage #2: With hydrogenchloride In water; ethyl acetate at 0 - 5℃; | 89.9% |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Stage #1: (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine L-(+)-tartrate With potassium carbonate In water; ethyl acetate at 20℃; for 1h; Stage #2: With hydrogenchloride In water; ethyl acetate at 0 - 8℃; for 2h; Concentration; | 90.5% |
Stage #1: (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine L-(+)-tartrate With potassium carbonate In dichloromethane; water at 20℃; for 1h; Stage #2: With hydrogenchloride In dichloromethane; water for 4h; Solvent; Reagent/catalyst; Cooling with ice; | 35.3% |
Stage #1: (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine L-(+)-tartrate With sodium hydroxide In water at 20℃; for 0.166667h; Stage #2: With hydrogenchloride In diethyl ether; dichloromethane at 20℃; for 0.0833333h; | 3.88 g |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Stage #1: bis((R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine) L-(+)-tartarate With potassium carbonate In water; ethyl acetate at 20 - 25℃; for 0.5 - 0.666667h; Stage #2: With hydrogenchloride In water; ethyl acetate at 0 - 5℃; for 3.5 - 4h; (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine; | 89.9% |
Stage #1: bis((R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine) L-(+)-tartarate With sodium hydroxide In dichloromethane; water at 25℃; for 0.5h; pH=10; Stage #2: With hydrogenchloride In ethyl acetate at 0℃; for 2.5h; pH=2; | 2.25 g |
Stage #1: bis((R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine) L-(+)-tartarate With potassium carbonate In water at 10 - 25℃; for 0.333333h; Stage #2: With hydrogenchloride In water; ethyl acetate at 0 - 5℃; Temperature; | 21.4 g |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Stage #1: 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine L-hemitartrate With potassium carbonate In water; ethyl acetate at 20 - 25℃; for 50.6667h; Stage #2: With hydrogenchloride In ethyl acetate at 0 - 5℃; for 3.5 - 4h; | 89.9% |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 5 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 3: acetone; water / 3 h / 50 °C / Large scale 4: potassium carbonate / water 5: hydrogenchloride / ethyl acetate; ethanol / 20 °C / pH 2 View Scheme | |
Multi-step reaction with 4 steps 1.1: hydrogenchloride / ethyl acetate / 20 °C 2.1: aluminum (III) chloride / 1,2-dichloro-benzene / 110 °C 3.1: acetone; water / 3 h / 50 °C 3.2: 5 h / 0 - 5 °C / Reflux 4.1: sodium hydroxide / dichloromethane; water / 0.5 h / 25 °C / pH 10 4.2: 2.5 h / 0 °C / pH 2 View Scheme | |
Multi-step reaction with 4 steps 1.1: dichloromethane / 25 °C 2.1: aluminum (III) chloride / 1,2-dichloro-benzene / 110 °C 3.1: acetone; water / 3 h / 50 °C 3.2: 5 h / 0 - 5 °C / Reflux 4.1: sodium hydroxide / dichloromethane; water / 0.5 h / 25 °C / pH 10 4.2: 2.5 h / 0 °C / pH 2 View Scheme | |
Multi-step reaction with 4 steps 1: aluminum (III) chloride / chlorobenzene / 110 °C 2: acetone / 3 h / 50 °C 3: potassium carbonate / water / pH 8-9 4: hydrogenchloride / ethanol; ethyl acetate / 1 h / 20 °C / pH 1-2 View Scheme |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: aluminum (III) chloride / 1,2-dichloro-benzene / 110 °C 2.1: acetone; water / 3 h / 50 °C 2.2: 5 h / 0 - 5 °C / Reflux 3.1: sodium hydroxide / dichloromethane; water / 0.5 h / 25 °C / pH 10 3.2: 2.5 h / 0 °C / pH 2 View Scheme |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: sodium hydroxide / methanol / 3 h / 60 °C 2.1: aluminum (III) chloride / 1,2-dichloro-benzene / 90 °C 3.1: acetone; water / 3 h / 50 °C 3.2: 5 h / 0 - 5 °C / Reflux 4.1: sodium hydroxide / dichloromethane; water / 0.5 h / 25 °C / pH 10 4.2: 2.5 h / 0 °C / pH 2 View Scheme |
N-(4-chlorophenylethyl)propyl-2-ene-1-amine
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: aluminum (III) chloride / 1,2-dichloro-benzene / 90 °C 2.1: acetone; water / 3 h / 50 °C 2.2: 5 h / 0 - 5 °C / Reflux 3.1: sodium hydroxide / dichloromethane; water / 0.5 h / 25 °C / pH 10 3.2: 2.5 h / 0 °C / pH 2 View Scheme |
1-[[2-(4-chlorophenyl)ethyl]amino]-2-hydroxypropane
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: N,N-dimethyl-formamide; thionyl chloride / toluene / 2 h / 45 - 60 °C 2.1: aluminum (III) chloride / 1,2-dichloro-benzene / 3 h / 125 - 130 °C 3.1: L-Tartaric acid / acetone; water / 0.5 h / 45 - 50 °C 4.1: potassium carbonate / water / 0.33 h / 10 - 25 °C 4.2: 0 - 5 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: thionyl chloride / toluene / 10 h / 70 °C 2.1: aluminum (III) chloride / 1,2-dichloro-benzene / 10 h / 140 °C 3.1: L-Tartaric acid / ethanol; water / 80 °C 3.2: pH 12 3.3: 1 h / 5 - 10 °C View Scheme |
1-((2-(4-chlorophenyl)ethyl)amino)-2-chloropropane hydrochloride
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: aluminum (III) chloride / 1,2-dichloro-benzene / 3 h / 125 - 130 °C 2.1: L-Tartaric acid / acetone; water / 0.5 h / 45 - 50 °C 3.1: potassium carbonate / water / 0.33 h / 10 - 25 °C 3.2: 0 - 5 °C View Scheme |
(R)-N-tert-butoxycarbonyl-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride In methanol; water | 1.8 g |
2-(2-bromo-4-chlorophenyl)ethan-1-amine
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: ethanol / 0.5 h 1.2: 1 h / Cooling with ice 2.1: methanol / 3 h 3.1: triethylamine / acetonitrile / 10 h / 80 °C / Inert atmosphere 4.1: palladium on activated charcoal; hydrogen; dimethylsulfide; thiourea / quinoline / 4 h / 3750.38 Torr 5.1: hydrogenchloride / methanol; water View Scheme |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: methanol / 3 h 2: triethylamine / acetonitrile / 10 h / 80 °C / Inert atmosphere 3: palladium on activated charcoal; hydrogen; dimethylsulfide; thiourea / quinoline / 4 h / 3750.38 Torr 4: hydrogenchloride / methanol; water View Scheme |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: triethylamine / acetonitrile / 10 h / 80 °C / Inert atmosphere 2: palladium on activated charcoal; hydrogen; dimethylsulfide; thiourea / quinoline / 4 h / 3750.38 Torr 3: hydrogenchloride / methanol; water View Scheme |
(±)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride
A
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
With Chiralpak IA column In methanol; ethanol; hexane; diethylamine at 20℃; Temperature; Resolution of racemate; |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: borane-THF / tetrahydrofuran / 15 h / 25 °C 1.2: 1 h / 5 - 25 °C 2.1: aluminum (III) chloride / neat (no solvent) / 150 °C 3.1: hydrogenchloride / diethyl ether; water; dichloromethane View Scheme |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: aluminum (III) chloride / dichloromethane / 0.17 h / 20 °C / Inert atmosphere 2: hydrogenchloride; platinum(IV) oxide; hydrogen / water; methanol / 48 h / 25 °C / 3750.38 Torr 3: phenol; hydrogen bromide; propionic acid / 6 h / Reflux 4: hydrogenchloride / diethyl ether; water; dichloromethane View Scheme |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: hydrogenchloride; platinum(IV) oxide; hydrogen / water; methanol / 48 h / 25 °C / 3750.38 Torr 2: phenol; hydrogen bromide; propionic acid / 6 h / Reflux 3: hydrogenchloride / diethyl ether; water; dichloromethane View Scheme |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: sodium hydroxide / water 2.1: sodium carbonate / dichloromethane / 0.25 h / 5 - 10 °C 2.2: 25 °C 3.1: borane-THF / tetrahydrofuran / 15 h / 25 °C 3.2: 1 h / 5 - 25 °C 4.1: aluminum (III) chloride / neat (no solvent) / 150 °C 5.1: hydrogenchloride / diethyl ether; water; dichloromethane View Scheme | |
Multi-step reaction with 7 steps 1: sodium hydroxide / water 2: potassium carbonate / N,N-dimethyl-formamide / 120 °C / Inert atmosphere 3: pyridine / dichloromethane / 2.5 h / 0 - 20 °C 4: aluminum (III) chloride / dichloromethane / 0.17 h / 20 °C / Inert atmosphere 5: hydrogenchloride; platinum(IV) oxide; hydrogen / water; methanol / 48 h / 25 °C / 3750.38 Torr 6: phenol; hydrogen bromide; propionic acid / 6 h / Reflux 7: hydrogenchloride / diethyl ether; water; dichloromethane View Scheme |
Lorcaserin hydrochloride
acrylonitrile
Conditions | Yield |
---|---|
With sodium In methanol at 55℃; for 12h; Inert atmosphere; | 96% |
Conditions | Yield |
---|---|
In acetone Solvent; | 94.7% |
Lorcaserin hydrochloride
2-Chloroethyl chloroformate
Conditions | Yield |
---|---|
Stage #1: Lorcaserin hydrochloride With triethylamine In dichloromethane at 0℃; for 0.166667h; Stage #2: 2-Chloroethyl chloroformate In dichloromethane at 0℃; for 2h; | 94.5% |
Lorcaserin hydrochloride
D-(+)-camphoric acid
Conditions | Yield |
---|---|
at 20 - 25℃; Concentration; Temperature; Reflux; | 81% |
Lorcaserin hydrochloride
1,1'-carbonyldiimidazole
2-(Diethylamino)ethanol
Conditions | Yield |
---|---|
Stage #1: 1,1'-carbonyldiimidazole; 2-(Diethylamino)ethanol In dichloromethane at 0 - 20℃; for 5.16667h; Inert atmosphere; Stage #2: Lorcaserin hydrochloride In dichloromethane at 20℃; | 80.4% |
Conditions | Yield |
---|---|
With potassium carbonate; potassium iodide In acetonitrile at 90℃; for 18h; Sealed tube; | 70% |
Conditions | Yield |
---|---|
Stage #1: Lorcaserin hydrochloride With sodium hydroxide In water pH=10; Stage #2: oxalic acid With hydrogenchloride In ethyl acetate at 20 - 25℃; Concentration; Reagent/catalyst; pH-value; Temperature; Solvent; | 68% |
Lorcaserin hydrochloride
trifluoroacetic anhydride
(1R)-N-trifluoroacetyl-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine
Conditions | Yield |
---|---|
With pyridine In dichloromethane at 0 - 20℃; for 3h; |
Lorcaserin hydrochloride
acetyl chloride
(R)-1-(8-chloro-1-methyl-4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)ethanone
Conditions | Yield |
---|---|
With triethylamine In dichloromethane at 20℃; for 0.5h; |
Lorcaserin hydrochloride
methoxypropionyl chloride
3-methoxy-1-((R)-1-methyl-8-(4-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)phenyl)-4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)propan-1-one
Conditions | Yield |
---|---|
With pyridine In dichloromethane at 20℃; for 4h; |
Lorcaserin hydrochloride
Conditions | Yield |
---|---|
With human sulfotransferase; 3′-phosphoadenosine 5′-phosphosulfate In aq. buffer at 37℃; for 0.05h; pH=7.5; Reagent/catalyst; Enzymatic reaction; |
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