DayangChem exported this product to many countries and regions at best price. If you are looking for the material's manufacturer or supplier in China, DayangChem is your best choice. Pls contact with us freely for getting detailed product spe
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inquiryAliskiren hemifumarate Henan Tianfu Chemical Co.,LTD was built in 2009 with an ISO certificate in the past 5 years, we have grown up as a famous fine chemicals supplier in china and we had established stable business relationships with samsung,lg
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inquiryAppearance:White to yellow powder Storage:Store in a cool,dry place and keep away from direct strong light Package:As customer request Application:Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM . An orall
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inquiryAliskiren CAS 173334-58-2 Quality standard :Enterprise standard Appearance:White solid powder Storage:Stored in dry and cool place, keeping out of moisture and sunshine, shelf life is two year. Package:on request Application:synthetic n
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(1S,2S,4S)-4-(2-carbamoyl-2-methylpropyl-carbamoyl)-2-hydroxy-1-{(S)-2-[4-methoxy-3-(3-methoxypropoxy)-benzyl]-3-methylbutyl}-5-methylhexyl-carbamic acid benzyl ester
(2E)-but-2-enedioic acid
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
Stage #1: (1S,2S,4S)-4-(2-carbamoyl-2-methylpropyl-carbamoyl)-2-hydroxy-1-{(S)-2-[4-methoxy-3-(3-methoxypropoxy)-benzyl]-3-methylbutyl}-5-methylhexyl-carbamic acid benzyl ester With palladium 10% on activated carbon; hydrogen In isopropyl alcohol at 20℃; under 760.051 Torr; Stage #2: (2E)-but-2-enedioic acid In ethanol | 100% |
Stage #1: (1S,2S,4S)-4-(2-carbamoyl-2-methylpropyl-carbamoyl)-2-hydroxy-1-{(S)-2-[4-methoxy-3-(3-methoxypropoxy)-benzyl]-3-methylbutyl}-5-methylhexyl-carbamic acid benzyl ester With palladium 10% on activated carbon In isopropyl alcohol at 20℃; under 760.051 Torr; Stage #2: (2E)-but-2-enedioic acid In ethanol | 85% |
tert-butyl (3S,5S,6S,8S)-8-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-6-hydroxy-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-2,9-dimethyldecan-5-ylcarbamate
(2E)-but-2-enedioic acid
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
Stage #1: tert-butyl (3S,5S,6S,8S)-8-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-6-hydroxy-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-2,9-dimethyldecan-5-ylcarbamate With hydrogenchloride In dichloromethane at 0℃; for 3h; Stage #2: (2E)-but-2-enedioic acid In ethanol | 85% |
Stage #1: tert-butyl (3S,5S,6S,8S)-8-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-6-hydroxy-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-2,9-dimethyldecan-5-ylcarbamate With hydrogenchloride In dichloromethane at 0℃; for 3h; Stage #2: (2E)-but-2-enedioic acid In ethanol | 85% |
(2E)-but-2-enedioic acid
(2S,4S,5S,7S)-5-Amino-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxy-propoxy)-benzyl]-8-methyl-nonanoic acid (2-carbamoyl-2-methyl-propyl)-amide
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
In methanol Solvent; Concentration; Time; Temperature; | 81.5% |
In methanol at 35℃; for 1h; Product distribution / selectivity; | 74.25% |
In ethanol at 20℃; Product distribution / selectivity; |
aliskiren
(2E)-but-2-enedioic acid
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
Stage #1: aliskiren With sodium hydroxide In water at 0℃; Stage #2: (2E)-but-2-enedioic acid In methanol |
(2E)-but-2-enedioic acid
(2S,4S,5S,7S)-5-Amino-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxy-propoxy)-benzyl]-8-methyl-nonanoic acid (2-carbamoyl-2-methyl-propyl)-amide
A
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
In ethanol at 40℃; Product distribution / selectivity; | A 93 %Chromat. B n/a |
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
In ethanol; acetonitrile at 20℃; Purification / work up; | 98.8 %Chromat. |
aminopivalinamide
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: triethylamine; 2-hydroxypyridin / 16 h / 85 - 90 °C 2: hydrogen; ethanolamine / palladium 10% on activated carbon / isopropyl alcohol / 3 h 3: ethanol / 0.17 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone / 4 h / 75 - 80 °C 1.2: 15 h / 85 - 90 °C 1.3: 3 h 2.1: ethanol / 0.17 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: thionyl chloride / 1,2-dichloro-ethane / 5 h / 75 - 80 °C 1.2: 90 - 95 °C 1.3: 10 - 15 °C / pH 14 2.1: triethylamine; 2-hydroxypyridin / 30 h / 80 - 90 °C 3.1: sodium hydroxide; dihydrogen peroxide / water / 20 - 40 °C 4.1: hydrogen; ethanolamine / 5%-palladium/activated carbon / ethanol / 2206.72 Torr View Scheme |
3-methylbutyric acid
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
Multi-step reaction with 13 steps 1.1: dmap / 1,1-dichloroethane / 0.5 h / 20 °C 1.2: 14.5 h / 10 - 30 °C 2.1: lithium hexamethyldisilazane / tetrahydrofuran / 2 h / -70 °C / Inert atmosphere 2.2: -70 - 5 °C 3.1: dihydrogen peroxide; lithium hydroxide monohydrate / water; tetrahydrofuran / 0 - 30 °C 4.1: sodium tetrahydroborate / tetrahydrofuran / 1 h / 0 - 5 °C / Inert atmosphere 4.2: 5.75 h / 0 - 30 °C 5.1: N-chloro-succinimide; triphenylphosphine / dichloromethane / 5.5 h / -40 - 30 °C 6.1: magnesium; ethylene dibromide / tetrahydrofuran / 4.17 h / 63 - 68 °C / Inert atmosphere 6.2: 12.5 h / 0 - 5 °C 7.1: water; lithium hydroxide / tetrahydrofuran; methanol / 26 h / 65 - 70 °C 7.2: 0.5 h / 0 - 5 °C 8.1: hydrogenchloride / 1,1-dichloroethane; water / 0 - 5 °C / pH 2.5 8.2: 14.25 h / 0 - 30 °C 9.1: N-Bromosuccinimide; phosphoric acid / water; tetrahydrofuran / 1.25 h / 0 - 5 °C 10.1: sodium azide / ethylene glycol / 20 h / 80 - 85 °C 11.1: triethylamine; 2-hydroxypyridin / 16 h / 85 - 90 °C 12.1: hydrogen; ethanolamine / palladium 10% on activated carbon / isopropyl alcohol / 3 h 13.1: ethanol / 0.17 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 10 steps 1.1: dmap / 1,1-dichloroethane / 0.5 h / 20 °C 1.2: 14.5 h / 10 - 30 °C 2.1: titanium(IV) isopropylate; N-ethyl-N,N-diisopropylamine; titanium tetrachloride / dichloromethane / 1 h / 0 - 5 °C / Inert atmosphere 2.2: -30 - -25 °C 2.3: -30 - 5 °C 3.1: hydrogen; acetic acid / palladium on activated charcoal / 60 - 70 °C / 2942.29 Torr 4.1: dihydrogen peroxide; lithium hydroxide monohydrate / water; tetrahydrofuran / 0 - 30 °C 5.1: sodium tetrahydroborate / tetrahydrofuran / 1 h / 0 - 5 °C / Inert atmosphere 5.2: 5.75 h / 0 - 30 °C 6.1: N-chloro-succinimide; triphenylphosphine / dichloromethane / 5.5 h / -40 - 30 °C 7.1: magnesium; ethylene dibromide / tetrahydrofuran / 4.17 h / 63 - 68 °C / Inert atmosphere 7.2: 1 h / 0 - 5 °C 8.1: N-Bromosuccinimide; phosphoric acid / water; tetrahydrofuran / 1.25 h / 0 - 5 °C 9.1: 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone / 4 h / 75 - 80 °C 9.2: 15 h / 85 - 90 °C 9.3: 3 h 10.1: ethanol / 0.17 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 10 steps 1.1: dmap / 1,1-dichloroethane / 0.5 h / 20 °C 1.2: 14.5 h / 10 - 30 °C 2.1: titanium(IV) isopropylate; N-ethyl-N,N-diisopropylamine; titanium tetrachloride / dichloromethane / 1 h / 0 - 5 °C / Inert atmosphere 2.2: -30 - -25 °C 2.3: -30 - 5 °C 3.1: hydrogen; acetic acid / palladium on activated charcoal / 60 - 70 °C / 2942.29 Torr 4.1: sodium tetrahydroborate / tetrahydrofuran / 0 - 15 °C 4.2: 11 h / 60 - 65 °C 5.1: N-chloro-succinimide; triphenylphosphine / dichloromethane / 5.5 h / -40 - 30 °C 6.1: magnesium; ethylene dibromide / tetrahydrofuran / 4.17 h / 63 - 68 °C / Inert atmosphere 6.2: 1 h / 0 - 5 °C 6.3: 0.75 h / 0 - 5 °C 7.1: sodium azide / ethylene glycol / 20 h / 80 - 85 °C 8.1: triethylamine; 2-hydroxypyridin / 16 h / 85 - 90 °C 9.1: hydrogen; ethanolamine / palladium 10% on activated carbon / isopropyl alcohol / 3 h 10.1: ethanol / 0.17 h / 25 - 30 °C View Scheme |
2-cyano-2-methylpropanamide
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: hydrogen; ammonia / raney nickel / methanol / 14 h / 40 - 45 °C / 2942.29 Torr 2: triethylamine; 2-hydroxypyridin / 16 h / 85 - 90 °C 3: hydrogen; ethanolamine / palladium 10% on activated carbon / isopropyl alcohol / 3 h 4: ethanol / 0.17 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: hydrogen; ammonia / raney nickel / methanol / 14 h / 40 - 45 °C / 2942.29 Torr 2.1: 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone / 4 h / 75 - 80 °C 2.2: 15 h / 85 - 90 °C 2.3: 3 h 3.1: ethanol / 0.17 h / 25 - 30 °C View Scheme |
(2E)-but-2-enedioic acid
(2S,4S,5S,7S)-N-(3-amino-2,2-dimethyl-3-oxopropyl)-5-azido-4-hydroxy-2-isopropyl-7-(4-methoxy-3-(methoxypropoxy)benzyl)-8-methylnonanamide
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
Stage #1: (2S,4S,5S,7S)-N-(3-amino-2,2-dimethyl-3-oxopropyl)-5-azido-4-hydroxy-2-isopropyl-7-(4-methoxy-3-(methoxypropoxy)benzyl)-8-methylnonanamide With hydrogen; ethanolamine; 5%-palladium/activated carbon In ethanol under 2206.72 Torr; Stage #2: (2E)-but-2-enedioic acid In ethanol Product distribution / selectivity; |
3-amino-2,2-dimethyl-propionitrile
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: triethylamine; 2-hydroxypyridin / 30 h / 80 - 90 °C 2: sodium hydroxide; dihydrogen peroxide / water / 20 - 40 °C 3: hydrogen; ethanolamine / 5%-palladium/activated carbon / ethanol / 2206.72 Torr View Scheme | |
Multi-step reaction with 4 steps 1: 2-hydroxypyridin; triethylamine / 24 h / 60 - 70 °C 2: sodium hydroxide; dihydrogen peroxide / water; ethanol / 30 - 40 °C 3: hydrogen; palladium 10% on activated carbon; ammonia / ethanol / 20 °C / 5250.53 Torr 4: ethanol; acetonitrile / 22 h / 0 - 40 °C View Scheme |
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate
(2S,4S,5S,7S)-5-Amino-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxy-propoxy)-benzyl]-8-methyl-nonanoic acid (2-carbamoyl-2-methyl-propyl)-amide
Conditions | Yield |
---|---|
With ammonia In water |
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