tert-butyl 2-(methylsulfonyl)ethylcarbamate
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride In ethyl acetate at 0 - 20℃; | 97% |
With hydrogenchloride In ethanol at 20℃; Temperature; | 88% |
With hydrogenchloride In diethyl ether; ethyl acetate at 20℃; | 78% |
(2-aminoethyl)methylsulfide
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride; dihydrogen peroxide In water at 25 - 30℃; pH=3 - 4; Solvent; | 94.8% |
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride; water at 100℃; for 10h; Reagent/catalyst; Temperature; | 92.1% |
With hydrogenchloride In water at 100℃; for 10h; | 92.1% |
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With potassium permanganate; water |
2-Methanesulfonyl-ethylamine
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride In ethanol Product distribution / selectivity; |
2-(methylsulfonyl)ethylamine hydrochloride
5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
lapatanib
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20℃; for 0.333333h; Stage #2: 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With acetic acid In tetrahydrofuran at 40℃; for 2h; Stage #3: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 25 - 40℃; for 3h; Concentration; | 100% |
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With N-ethyl-N,N-diisopropylamine In isopropyl alcohol at 50 - 60℃; for 4h; Stage #2: With sodium cyanoborohydride In isopropyl alcohol at 20℃; for 2h; | 92.6% |
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With sodium sulfate; triethylamine In methanol at 0℃; for 0.333333h; Stage #2: 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With formic acid; sodium cyanoborohydride In tetrahydrofuran; methanol; N,N-dimethyl-formamide for 2h; pH=5 - 6; | 82% |
5-(4-(3-chloro-4-hydroxyphenylamino)quinazolin-6-yl)furan-2-carbaldehyde tosylate
2-(methylsulfonyl)ethylamine hydrochloride
2-chloro-4-(6-(5-((2-(methylsulfonyl)ethylimino)methyl)furan-2-yl)quinazolin-4-ylamino)phenol
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In methanol at 20 - 25℃; for 20h; | 97.1% |
Conditions | Yield |
---|---|
With triethylamine In dichloromethane at 25 - 30℃; Inert atmosphere; | 97% |
2-(methylsulfonyl)ethylamine hydrochloride
5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((2-(methylsulfonyl)ethylimino)methyl)furan-2-yl)quinazolin-4-amine
Conditions | Yield |
---|---|
With triethylamine In methanol for 12h; Reflux; | 96% |
With triethylamine In methanol for 12h; Reflux; | 96% |
With triethylamine In methanol for 12h; Reflux; |
2-(methylsulfonyl)ethylamine hydrochloride
toluene-4-sulfonic acid
5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
lapatinib ditosylate
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With tetrabutylammomium bromide; triethylamine In tetrahydrofuran at 30℃; for 3h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 20℃; for 4h; Stage #3: toluene-4-sulfonic acid In tetrahydrofuran at 50℃; for 1h; | 94.9% |
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20℃; for 3h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 20℃; for 12h; Stage #3: toluene-4-sulfonic acid In tetrahydrofuran at 20℃; for 12h; | 82.8% |
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran; N,N-dimethyl-formamide at 35℃; for 1h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran; N,N-dimethyl-formamide at 20 - 25℃; for 2h; Stage #3: toluene-4-sulfonic acid | 72% |
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With N-ethyl-N,N-diisopropylamine In tetrahydrofuran; acetic acid at 30 - 35℃; for 1h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran; acetic acid at 22℃; for 2 - 4h; Stage #3: toluene-4-sulfonic acid With sodium hydroxide In tetrahydrofuran; acetic acid |
5-bromo-2-furancarboxaldehyde
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
Stage #1: 5-bromo-2-furancarboxaldehyde; 2-(methylsulfonyl)ethylamine hydrochloride With magnesium sulfate In dichloromethane at -5℃; for 2h; Inert atmosphere; Stage #2: With triethylamine In dichloromethane at -5℃; for 2h; Inert atmosphere; | 94.25% |
3-(3-(4-chloro-5-fluoropyrimidin-2-yl)-1-(2-fluorobenzyl)-1H-pyrazol-5-yl)isoxazole
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With triethylamine In 1,4-dioxane; water at 100℃; for 17h; | 91% |
Conditions | Yield |
---|---|
In tetrahydrofuran at 35 - 40℃; for 4h; | 90.3% |
2-(methylsulfonyl)ethylamine hydrochloride
D-arabinono-1,4-lactone 5-(dihydrogenophosphate)
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With sodium methylate at 35℃; Inert atmosphere; Stage #2: D-arabinono-1,4-lactone 5-(dihydrogenophosphate) With methanol at 20℃; for 1.5h; Inert atmosphere; | 89% |
ethyl 4-chloro-3-nitrobenzoate
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 60℃; for 16h; | 89% |
2-(methylsulfonyl)ethylamine hydrochloride
(±)-gossypol acetic acid
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With sodium hydroxide In ethanol for 1h; Reflux; Stage #2: (±)-gossypol acetic acid In ethanol for 5h; Reflux; | 86.8% |
4-((E)-{[1-(3-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]hydrazono}methyl)benzoic acid
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With diethyl cyanophosphonate; triethylamine In DMF (N,N-dimethyl-formamide) at 20℃; for 16h; | 84% |
2-(methylsulfonyl)ethylamine hydrochloride
toluene-4-sulfonic acid
5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20℃; for 3h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 20℃; for 12h; Stage #3: toluene-4-sulfonic acid With water In tetrahydrofuran at 20℃; for 12h; | 82.8% |
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
Stage #1: 2-amino-5-[(5-formyl)furan-2-yl]benzonitrile p-toluenesulfonic acid; 2-(methylsulfonyl)ethylamine hydrochloride With acetic acid; triethylamine In tetrahydrofuran at 20 - 35℃; for 1h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 22 - 25℃; for 2.5h; | 82.7% |
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With sodium sulfate; triethylamine In methanol at 0℃; for 0.333333h; Stage #2: 4-(4-(E)-(propen-1-yl)phenylamino)-6-(5-formylfuran-2-yl)quinazoline With formic acid; sodium cyanoborohydride In tetrahydrofuran; methanol; N,N-dimethyl-formamide for 2h; pH=5 - 6; | 82.6% |
4-((E)-{[1-(6-methoxypyridin-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]hydrazono}methyl)benzoic acid
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With diethyl cyanophosphonate; triethylamine In DMF (N,N-dimethyl-formamide) at 20℃; for 16h; | 81% |
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
Stage #1: 4-((E)-{[1-(2-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]hydrazono}methyl)benzoic acid; 2-(methylsulfonyl)ethylamine hydrochloride With diethyl cyanophosphonate; triethylamine In DMF (N,N-dimethyl-formamide) at 20℃; for 16h; Stage #2: With hydrogenchloride In water | 81% |
2-(methylsulfonyl)ethylamine hydrochloride
4-((E)-{[1-(3-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]hydrazono}methyl)benzoic acid
Conditions | Yield |
---|---|
With diethyl cyanophosphonate; triethylamine In DMF (N,N-dimethyl-formamide) at 20℃; for 16h; | 81% |
4-((E)-{[1-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]hydrazono}methyl)benzoic acid
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With diethyl cyanophosphonate; triethylamine In DMF (N,N-dimethyl-formamide) at 20℃; for 16h; | 80% |
2-(methylsulfonyl)ethylamine hydrochloride
toluene-4-sulfonic acid
Conditions | Yield |
---|---|
Stage #1: 5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde 4-methylbenzenesulfonate; 2-(methylsulfonyl)ethylamine hydrochloride With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 30 - 35℃; for 1h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 22℃; for 2h; Stage #3: toluene-4-sulfonic acid With sodium hydroxide; water more than 3 stages; | 80% |
5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-carbaldehyde
2-(methylsulfonyl)ethylamine hydrochloride
2-(methylsulphonyl)-N-({5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-yl}methyl)ethanamine
Conditions | Yield |
---|---|
Stage #1: 5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-carbaldheyde; 2-(methylsulfonyl)ethylamine hydrochloride With N-ethyl-N,N-diisopropylamine In dichloromethane at 20 - 35℃; for 0.5h; Inert atmosphere; Stage #2: With sodium tris(acetoxy)borohydride In dichloromethane at 20 - 25℃; for 2h; Stage #3: With sodium hydrogencarbonate In dichloromethane | 80% |
Stage #1: 5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-carbaldheyde; 2-(methylsulfonyl)ethylamine hydrochloride With N-ethyl-N,N-diisopropylamine In dichloromethane at 30 - 35℃; for 0.5h; Inert atmosphere; Stage #2: With sodium tris(acetoxy)borohydride In dichloromethane at 20 - 25℃; for 2h; | 80% |
Stage #1: 5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-carbaldheyde; 2-(methylsulfonyl)ethylamine hydrochloride With N-ethyl-N,N-diisopropylamine In dichloromethane at 20 - 35℃; for 0.5h; Inert atmosphere; Stage #2: With sodium tris(acetoxy)borohydride In dichloromethane at 20 - 25℃; for 2h; Inert atmosphere; | 80% |
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With sodium sulfate; triethylamine In methanol at 0℃; for 0.333333h; Stage #2: 4-(3-ethynyl-phenylamino)-6-(5-formylfuran-2-yl)quinazoline With formic acid; sodium cyanoborohydride In tetrahydrofuran; methanol; N,N-dimethyl-formamide for 2h; pH=5 - 6; | 79.7% |
4-(3-chloro-4-fluorophenylamino)-6-(5-formylfuran-2-yl)quinazoline
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With sodium sulfate; triethylamine In methanol at 0℃; for 0.333333h; Stage #2: N-(3-chloro-4-fluorophenyl)-6-(5-formyl-2-furyl)-4-quinazolinamine With formic acid; sodium cyanoborohydride In tetrahydrofuran; methanol; N,N-dimethyl-formamide for 2h; pH=5 - 6; | 78.1% |
2-(methylsulfonyl)ethylamine hydrochloride
trifluoroacetic acid
(2-methanesulfonyl-ethyl)-(6-methyl-5-nitro-pyridin-2-yl)-amine trifluoroacetate
Conditions | Yield |
---|---|
Stage #1: 6-fluoro-2-methyl-3-nitro-pyridine; 2-(methylsulfonyl)ethylamine hydrochloride With potassium carbonate In tetrahydrofuran at 20 - 60℃; for 100h; Stage #2: trifluoroacetic acid | 78% |
(S)-4-(4-((2-hydroxy-1-phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)-3-methoxybenzaldehyde
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 0.5h; Stage #2: (S)-4-(4-((2-hydroxy-1-phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)-3-methoxybenzaldehyde In dichloromethane at 20℃; for 6h; Stage #3: With sodium tetrahydroborate In methanol for 3h; | 77% |
4-((E)-{[1-(4-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]hydrazono}methyl)benzoic acid
2-(methylsulfonyl)ethylamine hydrochloride
Conditions | Yield |
---|---|
With diethyl cyanophosphonate; triethylamine In DMF (N,N-dimethyl-formamide) at 20℃; for 16h; | 76% |
The Ethanamine,2-(methylsulfonyl)-, hydrochloride (1:1), with CAS registry number 104458-24-4, belongs to the following product category: Intermediate of lapatinib ditosylate. It has the systematic name of 2-(methylsulfonyl)ethanamine hydrochloride (1:1). And the chemical formula of this chemical is C3H9NO2S.HCl.
Physical properties of Ethanamine,2-(methylsulfonyl)-, hydrochloride (1:1): (1)# of Rule of 5 Violations: 0; (2)ACD/BCF (pH 5.5): 1; (3)ACD/BCF (pH 7.4): 1; (4)ACD/KOC (pH 5.5): 1; (5)ACD/KOC (pH 7.4): 2; (6)#H bond acceptors: 3; (7)#H bond donors: 2; (8)#Freely Rotating Bonds: 3; (9)Polar Surface Area: 68.54 Å2; (10)Enthalpy of Vaporization: 57.92 kJ/mol; (11)Vapour Pressure: 0.000163 mmHg at 25°C.
You can still convert the following datas into molecular structure:
(1)SMILES: Cl.CS(=O)(=O)CCN
(2)InChI: InChI=1/C3H9NO2S.ClH/c1-7(5,6)3-2-4;/h2-4H2,1H3;1H
(3)InChIKey: AMYYUKGKCJKCBI-UHFFFAOYAR
(4)Std. InChI: InChI=1S/C3H9NO2S.ClH/c1-7(5,6)3-2-4;/h2-4H2,1H3;1H
(5)Std. InChIKey: AMYYUKGKCJKCBI-UHFFFAOYSA-N
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