4-benzylamino-piperidine-1-carboxylic acid tert-butyl ester
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With hydrogen; palladium 10% on activated carbon In ethanol under 5320.36 Torr; | 98% |
With hydrogen; palladium 10% on activated carbon In ethanol | 98% |
With hydrogen; palladium on activated charcoal In methanol |
tert-butyl 4-(hydroxyimino)piperidine-1-carboxylate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With hydrogen; Raney nickel In ethanol under 2585.81 Torr; | 98% |
With Raney nickel In methanol at 20℃; for 4h; | 83% |
With hydrogen; 5% rhodium on activated aluminium oxide In methanol at 50℃; |
N-tert-butyloxycarbonylpiperidin-4-one
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Stage #1: N-tert-butyloxycarbonylpiperidin-4-one With hydroxylamine hydrochloride; sodium carbonate In water at 23℃; for 14h; Stage #2: With hydrogen; Raney Ni In ethanol under 2585.81 Torr; for 3.5h; Solid phase; | 96% |
In ammonia-saturated methanol; aluminum nickel | 95.4% |
Stage #1: N-tert-butyloxycarbonylpiperidin-4-one With titanium(IV) isopropylate; ammonia In ethanol at 25℃; for 6h; Stage #2: With sodium tetrahydroborate In ethanol at 25℃; for 3h; Further stages.; | 88% |
A
1,1,1-trifluoroacetophenone
B
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With chloro-trimethyl-silane; lithium chloride | A n/a B 90% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With chloro-trimethyl-silane; lithium chloride In N,N-dimethyl-formamide at 60℃; for 12h; | 90% |
4-aminopiperidine
di-tert-butyl dicarbonate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Stage #1: 4-aminopiperidine; di-tert-butyl dicarbonate In 4-methyl-2-pentanone at 0 - 20℃; for 0.5h; Inert atmosphere; Reflux; Stage #2: With water In isopropyl alcohol at 50℃; | 85% |
In dichloromethane at 0℃; for 5h; | 71.9% |
Stage #1: 4-aminopiperidine With benzaldehyde In toluene for 3h; Heating / reflux; Stage #2: di-tert-butyl dicarbonate In toluene at 20℃; | |
With triethylamine In 1,4-dioxane; water | |
With triethylamine In 1,4-dioxane; water |
tert-butyl 4-(2,2,2-trifluoroacetamido)piperidine-1-carboxylate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With ammonium hydroxide In methanol for 2h; Heating; | 81% |
With ammonium hydroxide In methanol for 6h; Heating; | 5.75 g |
With sodium bicarbonate; potassium carbonate In methanol |
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With palladium on activated charcoal; hydrogen In methanol at 25℃; for 16h; | 81% |
1,1-dimethylethyl 4-[bis(phenylmethyl)amino]-1-piperidinecarboxylate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With hydrogen; palladium(II) hydroxide In tetrahydrofuran; ethanol at 23℃; under 760.051 Torr; for 6h; Inert atmosphere; | 77% |
tert-butyl 4-azidopiperidine-1-carboxylate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With ammonium hydroxide; triphenylphosphine In 1,4-dioxane; methanol at 27 - 28℃; for 0.5h; | 44% |
With hydrogen; palladium on activated charcoal In methanol under 2068.59 Torr; | |
palladium-carbon In methanol | |
palladium-carbon In methanol; hexane; ethyl acetate |
4-(benzylidene-amino)-piperidine-1-carboxylic acid tert-butyl ester
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With acetic acid for 48h; | 160 mg |
With potassium hydrogensulfate for 1.5h; | 4.76 g |
With sodium hydrogen sulfate; water for 2h; | |
With potassium hydrogensulfate; water In tert-butyl methyl ether at 20℃; for 4h; Inert atmosphere; | 6.0 g |
N-phenylmethylidenepiperidinyl-4-amine
A
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: toluene / 12 h / 25 °C 2: 4.76 g / aq. KHSO4 / 1.5 h View Scheme |
4-aminopiperidine
A
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: toluene / 4 h / Heating 2: toluene / 12 h / 25 °C 3: 4.76 g / aq. KHSO4 / 1.5 h View Scheme |
N-phenylmethylidenepiperidinyl-4-amine
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: Et3N / CH2Cl2 / 48 h / 20 °C 2: 160 mg / aq. AcOH / 48 h View Scheme | |
Multi-step reaction with 2 steps 1: toluene / 14.08 h / 0 - 20 °C / Inert atmosphere 2: potassium hydrogensulfate; water / tert-butyl methyl ether / 4 h / 20 °C / Inert atmosphere View Scheme |
4-aminopiperidine
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: Na2SO4 / CH2Cl2 / 24 h / 20 °C 2: Et3N / CH2Cl2 / 48 h / 20 °C 3: 160 mg / aq. AcOH / 48 h View Scheme | |
Multi-step reaction with 3 steps 1: toluene / 5.5 h / Inert atmosphere; Reflux 2: toluene / 14.08 h / 0 - 20 °C / Inert atmosphere 3: potassium hydrogensulfate; water / tert-butyl methyl ether / 4 h / 20 °C / Inert atmosphere View Scheme |
N-tert-butyloxycarbonylpiperidin-4-one
A
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: NaHB(OAc)3 / 1,2-dichloro-ethane 2: H2 / Pd/C / methanol View Scheme |
4-amino-1-benzylpiperidine
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 94 percent / Et3N / CH2Cl2 / 12 h / 20 °C 2: H2 / Pd(OH)2/C / methanol / 12 h / 2585.81 Torr 3: CH2Cl2 / 6 h 4: 5.75 g / aq. NH3 / methanol / 6 h / Heating View Scheme | |
Multi-step reaction with 4 steps 1: 94 percent / Et3N / CH2Cl2 / 0.25 h / 0 °C 2: H2 / Pearlman's catalyst / methanol / 48 h / 3102.9 Torr 3: 82 percent / Et3N / CH2Cl2 / 2 h / Ambient temperature 4: 81 percent / 37percent aq. NH4OH / methanol / 2 h / Heating View Scheme |
4-trifluoromethylcarbonylamino piperidine
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: CH2Cl2 / 6 h 2: 5.75 g / aq. NH3 / methanol / 6 h / Heating View Scheme | |
Multi-step reaction with 2 steps 1: 82 percent / Et3N / CH2Cl2 / 2 h / Ambient temperature 2: 81 percent / 37percent aq. NH4OH / methanol / 2 h / Heating View Scheme |
N-(1-benzyl-4-piperidinyl)-2,2,2-trifluoroacetamide
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: H2 / Pd(OH)2/C / methanol / 12 h / 2585.81 Torr 2: CH2Cl2 / 6 h 3: 5.75 g / aq. NH3 / methanol / 6 h / Heating View Scheme | |
Multi-step reaction with 3 steps 1: H2 / Pearlman's catalyst / methanol / 48 h / 3102.9 Torr 2: 82 percent / Et3N / CH2Cl2 / 2 h / Ambient temperature 3: 81 percent / 37percent aq. NH4OH / methanol / 2 h / Heating View Scheme |
4-bromo-1H-piperidine
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: DIPEA / CH2Cl2 2: NaN3 / dimethylformamide / 20 °C 3: H2 / 10 percent Pd/C / methanol / 2068.59 Torr View Scheme |
di-tert-butyl dicarbonate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: DIPEA / CH2Cl2 2: NaN3 / dimethylformamide / 20 °C 3: H2 / 10 percent Pd/C / methanol / 2068.59 Torr View Scheme | |
Multi-step reaction with 2 steps 1: triethylamine / dichloromethane / 16 h / 20 °C 2: palladium on activated charcoal; ammonia; hydrogen / methanol / 20 °C View Scheme |
tert-butyl 4-bromo-1-piperidinecarboxylate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: NaN3 / dimethylformamide / 20 °C 2: H2 / 10 percent Pd/C / methanol / 2068.59 Torr View Scheme |
water
N-tert-butyloxycarbonylpiperidin-4-one
sodium carbonate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
In tetrahydrofuran; EtOH (abs); ethanol | |
In tetrahydrofuran; EtOH (abs); ethanol |
water
N-tert-butyloxycarbonylpiperidin-4-one
sodium carbonate
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
In tetrahydrofuran; EtOH (abs); ethanol | |
In tetrahydrofuran | |
In tetrahydrofuran; EtOH (abs); ethanol |
N-tert-butyloxycarbonylpiperidin-4-one
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With sodium carbonate In tetrahydrofuran; water |
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Stage #1: C17H24N2O2 With potassium hydrogensulfate In water for 1.5h; Stage #2: With potassium hydroxide In water pH=10; |
4-aminopiperidine
di-tert-butyl dicarbonate
benzaldehyde
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Stage #1: 4-aminopiperidine; benzaldehyde In toluene for 3h; Heating / reflux; Stage #2: di-tert-butyl dicarbonate In toluene at 20℃; |
piperidin-4-one
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: triethylamine / dichloromethane / 16 h / 20 °C 2: palladium on activated charcoal; ammonia; hydrogen / methanol / 20 °C View Scheme |
2-benzthiazole thioacetic acid
1-(tert-butoxycarbonyl)-4-aminopiperidine
N-(1-tert-butoxycarbonylpiperidin-4-yl)-(2-benzothiazolylthio)acetamide
Conditions | Yield |
---|---|
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In chloroform at 20℃; for 20h; | 100% |
2-chloro-4,6-dimethoxy-1 ,3,5-triazine
1-(tert-butoxycarbonyl)-4-aminopiperidine
4-(4,6-dimethoxy-[1,3,5]triazin-2-ylamino)-piperidine-1-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
In acetonitrile at 160℃; for 0.333333h; microwave irradiation; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
(2-formylthiophen-3-yl)carbamic acid ethyl ester
Conditions | Yield |
---|---|
100% |
2,4-dinitrobenzenesulfonyl chloride
1-(tert-butoxycarbonyl)-4-aminopiperidine
tert-butyl 4-{[(2,4-dinitrophenyl)sulfonyl]amino}piperidine-1-carboxylate
Conditions | Yield |
---|---|
Stage #1: 2,4-dinitrobenzenesulfonyl chloride; 1-(tert-butoxycarbonyl)-4-aminopiperidine With lutidine In dichloromethane at 0 - 20℃; for 18.5h; Stage #2: With potassium hydrogensulfate; water for 0.5h; pH=2.5 - 3; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
2,4-dimethyl-1H-imidazole-5-carbaldehyde
Conditions | Yield |
---|---|
With sodium tris(acetoxy)borohydride; acetic acid In 1,2-dichloro-ethane at 0 - 20℃; Cooling with ice; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
chloroacetyl chloride
tert-butyl 4-(2-chloroacetamido)piperidine-1-carboxylate
Conditions | Yield |
---|---|
With triethylamine In dichloromethane at 0 - 20℃; for 1h; | 100% |
With triethylamine In dichloromethane at 0 - 20℃; for 0.333333h; Inert atmosphere; | 90% |
With N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 20℃; for 0.5h; | 89% |
2,4-dichlorothiazole-5-carboxaldehyde
1-(tert-butoxycarbonyl)-4-aminopiperidine
4-{[(2,4-dichloro-thiazol-5-yl)methyl]-amino}-piperidine-1-carboxylic acid t-butyl ester
Conditions | Yield |
---|---|
Stage #1: 2,4-dichlorothiazole-5-carboxaldehyde; 1-(tert-butoxycarbonyl)-4-aminopiperidine With acetic acid In 1,2-dichloro-ethane at 21 - 26℃; for 1.5h; Stage #2: With sodium tris(acetoxy)borohydride In 1,2-dichloro-ethane at 20 - 27℃; for 4.46667h; | 100% |
With sodium tris(acetoxy)borohydride; acetic acid In 1,2-dichloro-ethane at 20℃; for 18h; | 62% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
2,5(4)-dimethyl-1H-imidazole-4(5)-carboxaldehyde
tert-butyl 4-{[(2,4-dimethyl-1H-imidazol-5-yl)methyl]amino}piperidine-1-carboxylate
Conditions | Yield |
---|---|
With sodium tris(acetoxy)borohydride; acetic acid In methanol at 20℃; for 2h; | 100% |
Stage #1: 1-(tert-butoxycarbonyl)-4-aminopiperidine; 2,5(4)-dimethyl-1H-imidazole-4(5)-carboxaldehyde With sodium tris(acetoxy)borohydride; acetic acid In 1,2-dichloro-ethane at 20℃; for 15h; Stage #2: With water; potassium carbonate | 100% |
4-chloro-2-fluoro-nitrobenzene
1-(tert-butoxycarbonyl)-4-aminopiperidine
tert-butyl 4-((5-chloro-2-nitrophenyl)amino)piperidine-1-carboxylate
Conditions | Yield |
---|---|
With sodium carbonate In N,N-dimethyl-formamide at 80℃; for 1h; | 100% |
With sodium carbonate In N,N-dimethyl-formamide at 80℃; for 1h; | 100% |
With potassium carbonate; potassium iodide In N,N-dimethyl-formamide at 80℃; for 18h; | 93.2% |
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20 - 80℃; for 1h; | |
With potassium carbonate In dimethyl sulfoxide at 20℃; Inert atmosphere; |
4-fluoro-2-methyl-5-nitro-benzonitrile
1-(tert-butoxycarbonyl)-4-aminopiperidine
1,1-dimethylethyl 4-[(4-cyano-5-methyl-2-nitrophenyl)amino]-1-piperidinecarboxylate
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 80℃; | 100% |
4-fluoro-3-nitrobenzonitrile
1-(tert-butoxycarbonyl)-4-aminopiperidine
tert-butyl 4-((4-cyano-2-nitrophenyl)amino)piperidine-1-carboxylate
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; for 72h; | 100% |
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 27℃; Cooling with ice; |
methyl 2,4-difluoro-5-nitrobenzoate
1-(tert-butoxycarbonyl)-4-aminopiperidine
tert-butyl 4-{[5-fluoro-4-(methoxycarbonyl)-2-nitrophenyl]amino}piperidine-1-carboxylate
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; for 72h; | 100% |
4-methyl-benzaldehyde
1-(tert-butoxycarbonyl)-4-aminopiperidine
tert-butyl 4-((4-methylphenyl)methyl)aminopiperidine carboxylate
Conditions | Yield |
---|---|
Stage #1: 4-methyl-benzaldehyde; 1-(tert-butoxycarbonyl)-4-aminopiperidine In ethanol for 4h; Reflux; Stage #2: With sodium tetrahydroborate; ethanol at 20℃; for 24h; | 100% |
Stage #1: 4-methyl-benzaldehyde; 1-(tert-butoxycarbonyl)-4-aminopiperidine In ethanol for 4h; Heating / reflux; Stage #2: With sodium tetrahydroborate In ethanol at 20℃; for 24h; Stage #3: With water In ethanol | 100% |
With sodium tris(acetoxy)borohydride; acetic acid In 1,2-dichloro-ethane at 20℃; |
1-(tert-butoxycarbonyl)-4-aminopiperidine
2-methylimidazole-4(5)-carbaldehyde
tert-butyl4-{[(2-methyl-1H-imidazol-5-yl)methyl]amino}piperidine-1-carboxylate
Conditions | Yield |
---|---|
With sodium tris(acetoxy)borohydride; acetic acid In methanol at 20℃; for 2h; | 100% |
3-(Trifluoromethyl)benzenesulfonyl chloride
1-(tert-butoxycarbonyl)-4-aminopiperidine
4-(3-trifluoromethylbenzenesulfonylamino)piperidine-1-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With triethylamine In dichloromethane for 2h; | 100% |
4,6-bis-benzyloxy-5'-isopropyl-2'-methoxybiphenyl-3-carboxylic acid
1-(tert-butoxycarbonyl)-4-aminopiperidine
4-[(4,6-bis-benzyloxy-5'-isopropyl-2'-methoxybiphenyl-3-carbonyl)amino]piperidine-1-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; for 16h; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
3,5-ditrifluoromethylisocyanate
tert-butyl 4-(3-(3,5-bis(trifluoromethyl)phenyl)ureido)piperidine-1-carboxylate
Conditions | Yield |
---|---|
In dichloromethane at 20℃; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
4-Nitrobenzenesulfonyl chloride
4-(4-nitrobenzenesulfonylamino)piperidine-1-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20℃; for 1h; Inert atmosphere; | 100% |
With N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20℃; for 1h; Inert atmosphere; |
N-(6-chloro-4-((cis-2,6-dimethylmorpholino)methyl)pyridin-2-yl)thiazolo[5,4-b]pyridin-2-amine
1-(tert-butoxycarbonyl)-4-aminopiperidine
1,1-dimethylethyl 4-{[4-{[cis-2,6-dimethyl-4-morpholinyl]methyl}-6-([1,3]thiazolo[5,4-b]pyridin-2-ylamino)-2-pyridinyl]amino}-1-piperidinecarboxylate
Conditions | Yield |
---|---|
With lithium hexamethyldisilazane; (NHC)Pd(allyl)Cl In tetrahydrofuran at 80℃; for 1h; Microwave irradiation; Inert atmosphere; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
2,4-dibromobutanoyl chloride
tert-butyl 4-(2,4-dibromobutanamido)piperidin-1-carboxylate
Conditions | Yield |
---|---|
Stage #1: 1-(tert-butoxycarbonyl)-4-aminopiperidine; 2,4-dibromobutanoyl chloride With triethylamine In dichloromethane at 0℃; Stage #2: With sodium hydrogencarbonate In dichloromethane Product distribution / selectivity; | 100% |
With triethylamine In tetrahydrofuran at 20℃; for 0.5h; | |
With triethylamine In tetrahydrofuran at 20℃; for 0.5h; |
1-(benzenesulfonyl)-4-chloro-5-nitro-1H-pyrrolo[2,3-b]pyridine
1-(tert-butoxycarbonyl)-4-aminopiperidine
4-(1-benzenesulphonyl-5-nitro-1H-pyrrolo[2,3-b]pyridine-4ylamino)piperidine-1-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In isopropyl alcohol for 2h; Reflux; | 100% |
With N-ethyl-N,N-diisopropylamine In isopropyl alcohol Inert atmosphere; Heating; |
1-(tert-butoxycarbonyl)-4-aminopiperidine
4-bromobutanenitrile
Conditions | Yield |
---|---|
With potassium carbonate In acetonitrile for 48h; Reflux; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
In 1-methyl-pyrrolidin-2-one at 180℃; for 2h; Time; Microwave irradiation; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 15h; Inert atmosphere; | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
5,7-dichloropyrazolo[1,5-a]pyrimidine
Conditions | Yield |
---|---|
With triethylamine In acetonitrile at 100℃; for 12h; | 100% |
With triethylamine In acetonitrile at 100℃; for 12h; |
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 15h; | 100% |
2-(4-chloro-3-fluorophenoxy)acetic acid
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Stage #1: 2-(4-chloro-3-fluorophenoxy)acetic acid; 1-(tert-butoxycarbonyl)-4-aminopiperidine With HATU In N,N-dimethyl-formamide at 20℃; for 0.166667h; Stage #2: With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; | 100% |
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 25℃; for 12h; |
6-chloro-2-quinolinecarboxylic acid
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
Stage #1: 6-chloro-2-quinolinecarboxylic acid; 1-(tert-butoxycarbonyl)-4-aminopiperidine With HATU In N,N-dimethyl-formamide at 20℃; for 0.166667h; Stage #2: With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide | 100% |
1-(tert-butoxycarbonyl)-4-aminopiperidine
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In dimethyl sulfoxide at 70℃; for 2h; | 100% |
The 4-Amino-1-boc-piperidine is the chemical compound with the formula C10H20N2O2. Its molecular weight is 200.28. It is white to light yellow crystal powder. With cas registry number of 87120-72-7, it belongs to the categories of (1)Amino acid; (2)Amines; (3)blocks; (4)Amines and Anilines; (5)Piperidines, Piperidones,Piperazines; (6)pharmacetical; (7)Pyrans, Piperidines & Piperazines; (8)API intermediates; (9)Piperidines; (10)Piperazine; (11)Pyrans, Piperidines & Piperazines.
Physical properties of 4-Amino-1-boc-piperidine are: (1) ACD/LogP: 1.09 ; (2) # of Rule of 5 Violations: 0 ; (3) ACD/LogD (pH 5.5): ; (4) ACD/LogD (pH 7.4): ; (5) ACD/BCF (pH 5.5): 1 ; (6) ACD/BCF (pH 7.4): 1 ; (7) ACD/KOC (pH 5.5): 1 ; (8) ACD/KOC (pH 7.4): 1.004 ; (9) #H bond acceptors: 4 ; (10) #H bond donors: 2 ; (11) #Freely Rotating Bonds: 3 ; (12) Index of Refraction: 1.484 ; (13) Molar Refractivity: 54.993 cm3 ; (14) Molar Volume: 192.269 cm3 ; (15) Surface Tension: 37.816 dyne/cm ; (16) Density: 1.042 g/cm3 ; (17) Flash Point: 121.509 °C ; (18) Enthalpy of Vaporization: 51.586 kJ/mol ; (19) Boiling Point: 277.303 °C at 760 mmHg ; (20) Vapour Pressure: 0.005 mmHg at 25°C.
Preparation of 4-Amino-1-boc-piperidine : This chemical can be prepared by 4-(2,2,2-trifluoro-acetylamino)-piperidine-1-carboxylic acid tert-butyl ester .
The reaction will use reagent aq. NH3, solvent Methanol and other conditions like heating. The reaction time is about 6 hours. Yield is about 5.75 g.
Uses of 4-Amino-1-boc-piperidine : It is used to prepare other chemicals. Here is a example below.
The reaction occurs at the temperature of 120 ℃ using reagents of K2CO3, KI, solvent of dimethylformamide for 24 hours. The yield is 58%.
When you are using this chemical, please be cautious about it as the following:
This chemical is sensitive to CO2. It is harmful by inhalation, in contact with skin and if swallowed and irritating to eyes, respiratory system and skin. Wear suitable protective clothing, gloves and eye/face protection before use it. During use it, do not breathe dust. In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. Keep it under argon.
You can still convert the following datas into molecular structure:
(1) SMILES:CC(C)(C)OC(=O)N1CCC(CC1)N;
(2) InChI:InChI=1/C10H20N2O2/c1-10(2,3)14-9(13)12-6-4-8(11)5-7-12/h8H,4-7,11H2,1-3H3;
(3) InChIKey:LZRDHSFPLUWYAX-UHFFFAOYAC
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