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inquirybetamethasone-valerate
Conditions | Yield |
---|---|
In methanol |
Conditions | Yield |
---|---|
With toluene-4-sulfonic acid In N,N-dimethyl-formamide; benzene for 1.25h; Ambient temperature; |
9α-fluoro-11β,17α,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione 17-valerate 21-acetate
betamethasone-valerate
Conditions | Yield |
---|---|
In methanol |
Conditions | Yield |
---|---|
With toluene-4-sulfonic acid In benzene for 4h; Heating; | 83% |
Conditions | Yield |
---|---|
With toluene-4-sulfonic acid In benzene for 4h; Heating; | 72% |
Conditions | Yield |
---|---|
Stage #1: succinic acid With dmap; dicyclohexyl-carbodiimide In dichloromethane at 20℃; for 0.5h; Inert atmosphere; Stage #2: betamethasone-valerate In dichloromethane at 20℃; Inert atmosphere; | 53% |
betamethasone-valerate
methanesulfonyl chloride
Pentanoic acid (8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-methanesulfonyloxy-acetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl ester
Conditions | Yield |
---|---|
In pyridine at 0 - 5℃; for 1.5h; |
betamethasone-valerate
(17R)-5'-butyl-4'-ethylthio-9α-fluoro-11β-hydroxy-16β-methyl-spiro-3,3'-dione
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine / 1.5 h / 0 - 5 °C 2: 78 percent / acetone / 7 h / Ambient temperature View Scheme |
betamethasone-valerate
9α-fluoro-11β-hydroxy-16β-methyl-21-methylthio-17α-valeryloxy-1,4-pregnadiene-3,20-dione
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine / 1.5 h / 0 - 5 °C 2: 91 percent / acetone / 1 h / Ambient temperature View Scheme |
betamethasone-valerate
21-ethylthio-9α-fluoro-11β-hydroxy-16β-methyl-17α-valeryloxy-1,4-pregnadiene-3,20-dione
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine / 1.5 h / 0 - 5 °C 2: 53 percent / NaOMe / acetone / 0.83 h / Ambient temperature View Scheme |
betamethasone-valerate
(17R)-5'-butyl-9α-fluoro-11β-hydroxy-16β-methyl-4'-propylthio-spiro-3,3'-dione
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine / 1.5 h / 0 - 5 °C 2: 74 percent / acetone / 7 h / Ambient temperature View Scheme |
betamethasone-valerate
9α-fluoro-11β-hydroxy-16β-methyl-21-propylthio-17α-valeryloxy-1,4-pregnadiene-3,20-dione
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine / 1.5 h / 0 - 5 °C 2: 80 percent / NaOMe / acetone / 0.83 h / Ambient temperature View Scheme |
betamethasone-valerate
(17R)-5'-butyl-4'-butylthio-9α-fluoro-11β-hydroxy-16β-methyl-spiro-3,3'-dione
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine / 1.5 h / 0 - 5 °C 2: 78 percent / acetone / 7 h / Ambient temperature View Scheme |
betamethasone-valerate
21-butylthio-9α-fluoro-11β-hydroxy-16β-methyl-17α-valeryloxy-1,4-pregnadiene-3,20-dione
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine / 1.5 h / 0 - 5 °C 2: 66 percent / NaOMe / acetone / 0.83 h / Ambient temperature View Scheme |
betamethasone-valerate
9α-fluoro-11β-hydroxy-16β-methyl-21-phenylthio-17α-valeryloxy-1,4-pregnadiene-3,20-dione
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine / 1.5 h / 0 - 5 °C 2: 45 percent / NaOMe / acetone / 0.83 h / Ambient temperature View Scheme |
betamethasone-valerate
A
(2S)-2-((1,1-Dimethylethoxycarbonyl)-amino)-3-methyl-butyric acid [11β,21-dihydroxy-3,20-dioxo-9-fluoro-16β-methyl-17-valeroyloxy -pregna-1,4-dien-21-yl] ester (Boc-Val-O-BMV)(2S)-2-((1,1-Dimethylethoxycarbonyl)-amino)-3-methyl-butyric acid [11β,21-dihydroxy-3,20-dioxo-9-fluoro-16β-methyl-17-valeroyloxy -pregna-1,4-dien-21-yl] ester (Boc-Val-O-BMV)
Conditions | Yield |
---|---|
With dmap In 1,4-dioxane; hexane; dichloromethane | A 10.1 g (73%) B n/a |
succinic acid
(S)-2-[{({9H-fluoren-9-yl}methoxy)carbonyl}amino]pentanedioic acid
betamethasone-valerate
N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-methionine
Fmoc-L-Gln(Trt)-OH
Conditions | Yield |
---|---|
Stage #1: Nα-(9-fluorenylmethyloxycarbonyl)-Nγ-2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl-L-arginine With benzotriazol-1-ol; diisopropyl-carbodiimide In N,N-dimethyl-formamide at 25 - 32℃; for 5h; Stage #2: With piperidine In N,N-dimethyl-formamide for 0.25h; Stage #3: succinic acid; (S)-2-[{({9H-fluoren-9-yl}methoxy)carbonyl}amino]pentanedioic acid; betamethasone-valerate; N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-methionine; Fmoc-L-Gln(Trt)-OH; Nα-(9-fluorenylmethyloxycarbonyl)-Nγ-2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl-L-arginine Further stages; |
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