As a leading manufacturer and supplier of chemicals in China, DayangChem not only supply popular chemicals, but also DayangChem's R&D center offer custom synthesis services. DayangChem can provide different quantities of custom synthesis ch
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inquiry(1S,4R)-4-[2-amino-6-chloro-9H-purin-9-yl]-2-cyclopentene-1-methanol
Cyclopropylamine
abacavir
Conditions | Yield |
---|---|
In ethanol at 70℃; | 98% |
In ethanol Heating; | 72% |
Stage #1: (1S,4R)-4-[2-amino-6-chloro-9H-purin-9-yl]-2-cyclopentene-1-methanol; Cyclopropylamine In butan-1-ol at 40 - 70℃; for 5h; Stage #2: With sodium hydrogencarbonate In butan-1-ol at 20 - 25℃; for 1h; Product distribution / selectivity; | |
In butan-1-ol at 45 - 90℃; for 2h; Product distribution / selectivity; | |
With sodium hydrogencarbonate In ethanol; chloroform | 0.43 g (80%) |
Cyclopropylamine
(1S,cis)-4-(2-amino-6-chloro-9-H-purin-9-yl)-2-cyclopentene-1-methanol hydrochloride
abacavir
Conditions | Yield |
---|---|
In methanol at 70℃; for 12h; Substitution; | 90% |
Stage #1: (1S,cis)-4-(2-amino-6-chloro-9-H-purin-9-yl)-2-cyclopentene-1-methanol hydrochloride With triethylamine In water Stage #2: Cyclopropylamine In water at 70 - 75℃; Concentration; Solvent; Temperature; | 90% |
In isopropyl alcohol at 90 - 95℃; for 12h; sealed reactor; | |
In ethanol at 25 - 78℃; for 6h; | |
With sodium carbonate In ethanol at 70 - 80℃; | 25 g |
(-)-N-{6-(cyclopropylamino)-9-[(1R,4S)-4-(hydroxymethyl)cyclopent-2-enyl]-9H-purin-2-yl}isobutyramide
abacavir
Conditions | Yield |
---|---|
Stage #1: (-)-N-{6-(cyclopropylamino)-9-[(1R,4S)-4-(hydroxymethyl)cyclopent-2-enyl]-9H-purin-2-yl}isobutyramide With isopropyl alcohol; sodium hydroxide for 1h; Reflux; Stage #2: With hydrogenchloride In water; isopropyl alcohol at 20 - 25℃; pH=7.0 - 7.5; Product distribution / selectivity; | 90% |
With sodium hydroxide; water; isopropyl alcohol for 1h; Heating / reflux; | 77% |
With sodium hydroxide; water; isopropyl alcohol for 1h; Product distribution / selectivity; Heating / reflux; | 43% |
pyrographite
Cyclopropylamine
(1S,cis)-4-(2-amino-6-chloro-9-H-purin-9-yl)-2-cyclopentene-1-methanol hydrochloride
abacavir
Conditions | Yield |
---|---|
With sodium hydroxide In acetone | 90% |
6-cyclopropylamine-9-((1R,4S)-4-((triisopropylsilyloxy)methyl)cyclopent-2-enyl)-9H-purin-2-amine
abacavir
Conditions | Yield |
---|---|
With tetrabutyl ammonium fluoride; water In tetrahydrofuran at 20℃; for 1h; Inert atmosphere; | 89% |
abacavir
Conditions | Yield |
---|---|
With sodium hydroxide In water; ethyl acetate at 25 - 45℃; pH=6 - 6.1; | 78% |
((1S,4R)-4-(6-(cyclopropylamino)-2-((4-methoxybenzyl)amino)-9H-purin-9-yl)cyclopent-2-en-1-yl)methanol
abacavir
Conditions | Yield |
---|---|
With trifluoroacetic acid In chloroform at 50℃; for 72h; Inert atmosphere; | 73% |
abacavir
Conditions | Yield |
---|---|
With trifluoroacetic acid In dichloromethane at 60℃; for 60h; Schlenk technique; | 70% |
((1S,4R)-4-(2-chloro-6-(cyclopropylamino)-9H-purin-9-yl)cyclopent-2-en-1-yl)methanol
abacavir
Conditions | Yield |
---|---|
With ammonium hydroxide; copper(l) iodide In ethanol at 150℃; for 40h; Schlenk technique; Sealed tube; | 63% |
Stage #1: ((1S,4R)-4-(2-chloro-6-(cyclopropylamino)-9H-purin-9-yl)cyclopent-2-en-1-yl)methanol With hydrazine In methanol; water at 50℃; Stage #2: With acetic acid; sodium nitrite In water at 0℃; for 1h; Stage #3: With tin(ll) chloride In ethanol for 2h; Product distribution / selectivity; Heating / reflux; | |
Stage #1: ((1S,4R)-4-(2-chloro-6-(cyclopropylamino)-9H-purin-9-yl)cyclopent-2-en-1-yl)methanol With hydrazine In methanol at 50℃; Stage #2: With acetic acid; sodium nitrite In water at 0℃; for 1h; Stage #3: With ammonia; triphenylphosphine In 1,4-dioxane; water for 5h; Product distribution / selectivity; Heating / reflux; | |
Multi-step reaction with 2 steps 1: dimethyl sulfoxide / 150 °C 2: trifluoroacetic acid / chloroform / 72 h / 50 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 3 steps 1: hydrazine hydrate / methanol / 50 °C 2: acetic acid; sodium nitrite / water / 1 h / Cooling with ice 3: stannous chloride dihydrate / ethanol / 2 h / Reflux View Scheme |
Cyclopropylamine
(1R,4S)-1-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-4-(hydroxymethyl)-2-cyclopentene
A
(1S, 4R)-(4-(2,5-diamino-6-chloro-4-pyrimidinyl)amino)-2-cyclopenten-1-methanol
B
abacavir
Conditions | Yield |
---|---|
In butan-1-ol at 130℃; for 21h; Substitution; hydrolysis; | A 16% B 60% |
2-Amino-6-chloropurin
Cyclopropylamine
cis-3-benzoyloxy-4-(hydroxymethyl)cyclopentene
abacavir
Conditions | Yield |
---|---|
Stage #1: 2-Amino-6-chloropurin; cis-3-benzoyloxy-4-(hydroxymethyl)cyclopentene With 1,2,2,6,6-pentamethylpiperidine; tris(dibenzylideneacetone)dipalladium (0); triphenylphosphine In tetrahydrofuran; dimethyl sulfoxide at 45℃; for 16h; Solid phase reaction; addition; elimination; Stage #2: Cyclopropylamine With N-ethyl-N,N-diisopropylamine In butan-1-ol at 80℃; for 4h; Solid phase reaction; amination; Further stages.; | 60% |
ethanesulfonic acid
orthoformic acid triethyl ester
Cyclopropylamine
abacavir
Conditions | Yield |
---|---|
In hydrogenchloride; methanol; N,N-dimethyl-formamide | 19% |
((1S,4R)-4-(2-amino-6-(cyclopropylamino)-9H-purin-9-yl)cyclopent-2-en-1-yl)methyl acetate
abacavir
Conditions | Yield |
---|---|
With sodium hydroxide; water Yield given; | |
With sodium hydroxide at 20℃; | 0.027 g |
With sodium hydroxide |
(1R,5R)-5-hydroxymethyl-2-cyclopenten-1-ol
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 2: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 3: aq. NaOH View Scheme | |
Multi-step reaction with 4 steps 1: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 2: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 3: ethanol / 5 h / Heating 4: aq. NaOH View Scheme | |
Multi-step reaction with 4 steps 1.1: Et3N 2.1: Et3N; 4-DMAP 3.1: aq. HF / acetonitrile 4.1: Pd2(dba)3; PPh3; 1,2,2,6,6-pentamethylpiperidine (pempidine) / tetrahydrofuran; dimethylsulfoxide / 16 h / 45 °C 4.2: 60 percent / EtN(i-Pr)2 / butan-1-ol / 4 h / 80 °C View Scheme |
2-amino-6-(cyclopropylamino)purine
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 2: aq. NaOH View Scheme |
2-Amino-6-chloropurin
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: dimethylsulfoxide / 16 h / 55 °C 2: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 3: aq. NaOH View Scheme |
9-[cis-(1'R,4'S)-4'-acetoxymethyl-2'-cyclopenten-1'-yl]-9H-2-amino-6-chloropurine
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: ethanol / 5 h / Heating 2: aq. NaOH View Scheme | |
Multi-step reaction with 2 steps 1: ethanol 2: NaOH, H2O View Scheme |
(1R,2R)-2-acetoxy-1-(acetoxymethyl)-3-cyclopentene
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 2: aq. NaOH View Scheme | |
Multi-step reaction with 3 steps 1: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 2: ethanol / 5 h / Heating 3: aq. NaOH View Scheme | |
Multi-step reaction with 2 steps 1: 62 percent / NaH, Pd(PPh3)4 / tetrahydrofuran; dimethylsulfoxide 2: NaOH, H2O View Scheme | |
Multi-step reaction with 3 steps 1: 65 percent / NaH, Pd(PPh3)4 / tetrahydrofuran; dimethylsulfoxide 2: ethanol 3: NaOH, H2O View Scheme |
[3(1R,2R),4S]-4-benzyl-3-(2-hydroxycyclopent-3-enecarbonyl)oxazolidin-2-one
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 78 percent / LiBH4 / tetrahydrofuran; methanol / 1 h / 0 °C 2: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 3: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 4: aq. NaOH View Scheme | |
Multi-step reaction with 5 steps 1: 78 percent / LiBH4 / tetrahydrofuran; methanol / 1 h / 0 °C 2: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 3: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 4: ethanol / 5 h / Heating 5: aq. NaOH View Scheme | |
Multi-step reaction with 4 steps 1: 78 percent / LiBH4 / tetrahydrofuran; methanol 2: 90 percent / Et3N, DMAP / CH2Cl2 3: 62 percent / NaH, Pd(PPh3)4 / tetrahydrofuran; dimethylsulfoxide 4: NaOH, H2O View Scheme | |
Multi-step reaction with 5 steps 1: 78 percent / LiBH4 / tetrahydrofuran; methanol 2: 90 percent / Et3N, DMAP / CH2Cl2 3: 65 percent / NaH, Pd(PPh3)4 / tetrahydrofuran; dimethylsulfoxide 4: ethanol 5: NaOH, H2O View Scheme |
[3(2S,4R),4S]-3-(2-allyl-3-hydroxypent-4-enoyl)-4-benzyloxazolidin-2-one
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: 97 percent / (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 0.5 h / 25 °C 2: 78 percent / LiBH4 / tetrahydrofuran; methanol / 1 h / 0 °C 3: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 4: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 5: aq. NaOH View Scheme | |
Multi-step reaction with 6 steps 1: 97 percent / (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 0.5 h / 25 °C 2: 78 percent / LiBH4 / tetrahydrofuran; methanol / 1 h / 0 °C 3: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 4: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 5: ethanol / 5 h / Heating 6: aq. NaOH View Scheme | |
Multi-step reaction with 5 steps 1: 97 percent / Grubbs catalyst / CH2Cl2 2: 78 percent / LiBH4 / tetrahydrofuran; methanol 3: 90 percent / Et3N, DMAP / CH2Cl2 4: 62 percent / NaH, Pd(PPh3)4 / tetrahydrofuran; dimethylsulfoxide 5: NaOH, H2O View Scheme | |
Multi-step reaction with 6 steps 1: 97 percent / Grubbs catalyst / CH2Cl2 2: 78 percent / LiBH4 / tetrahydrofuran; methanol 3: 90 percent / Et3N, DMAP / CH2Cl2 4: 65 percent / NaH, Pd(PPh3)4 / tetrahydrofuran; dimethylsulfoxide 5: ethanol 6: NaOH, H2O View Scheme |
[4S,2R,3R]-(4-benzyl-2-thioxooxazolidin-3-yl)(2-hydroxycyclopent-3-enyl)methanone
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 85 percent / LiBH4 / tetrahydrofuran; methanol 2: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 3: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 4: aq. NaOH View Scheme | |
Multi-step reaction with 5 steps 1: 85 percent / LiBH4 / tetrahydrofuran; methanol 2: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 3: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 4: ethanol / 5 h / Heating 5: aq. NaOH View Scheme | |
Multi-step reaction with 5 steps 1.1: 78 percent / LiBH4 / methanol 2.1: Et3N 3.1: Et3N; 4-DMAP 4.1: aq. HF / acetonitrile 5.1: Pd2(dba)3; PPh3; 1,2,2,6,6-pentamethylpiperidine (pempidine) / tetrahydrofuran; dimethylsulfoxide / 16 h / 45 °C 5.2: 60 percent / EtN(i-Pr)2 / butan-1-ol / 4 h / 80 °C View Scheme |
(E)-(2R,3R)-2-Allyl-hex-4-ene-1,3-diol
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: Et3N / CH2Cl2 2: (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 25 °C 3: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 4: aq. NaOH View Scheme | |
Multi-step reaction with 5 steps 1: Et3N / CH2Cl2 2: (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 25 °C 3: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 4: ethanol / 5 h / Heating 5: aq. NaOH View Scheme |
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 25 °C 2: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 3: aq. NaOH View Scheme | |
Multi-step reaction with 4 steps 1: (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 25 °C 2: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 3: ethanol / 5 h / Heating 4: aq. NaOH View Scheme |
(E)-(2S,3R)-2-Allyl-1-((S)-4-benzyl-2-thioxo-oxazolidin-3-yl)-3-hydroxy-hex-4-en-1-one
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: 77 percent / NaBH4 / tetrahydrofuran; H2O 2: Et3N / CH2Cl2 3: (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 25 °C 4: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 5: aq. NaOH View Scheme | |
Multi-step reaction with 6 steps 1: 77 percent / NaBH4 / tetrahydrofuran; H2O 2: Et3N / CH2Cl2 3: (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 25 °C 4: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 5: ethanol / 5 h / Heating 6: aq. NaOH View Scheme |
(E)-(2S,3R)-2-Allyl-1-((R)-4-benzyl-2-thioxo-oxazolidin-3-yl)-3-hydroxy-hex-4-en-1-one
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: 74 percent / (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 1 h / 40 °C 2: 85 percent / LiBH4 / tetrahydrofuran; methanol 3: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 4: 62 percent / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 5: aq. NaOH View Scheme | |
Multi-step reaction with 6 steps 1: 74 percent / (Cy3P)2Cl2Ru=CHPh / CH2Cl2 / 1 h / 40 °C 2: 85 percent / LiBH4 / tetrahydrofuran; methanol 3: 90 percent / Et3N; DMAP / CH2Cl2 / 0 °C 4: 0.298 g / NaH; Pd(PPh3)4 / dimethylsulfoxide; tetrahydrofuran / 45 °C 5: ethanol / 5 h / Heating 6: aq. NaOH View Scheme |
(1R,5R)-5-(tert-Butyl-dimethyl-silanyloxymethyl)-cyclopent-2-enol
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: Et3N; 4-DMAP 2.1: aq. HF / acetonitrile 3.1: Pd2(dba)3; PPh3; 1,2,2,6,6-pentamethylpiperidine (pempidine) / tetrahydrofuran; dimethylsulfoxide / 16 h / 45 °C 3.2: 60 percent / EtN(i-Pr)2 / butan-1-ol / 4 h / 80 °C View Scheme |
Benzoic acid (1R,5R)-5-(tert-butyl-dimethyl-silanyloxymethyl)-cyclopent-2-enyl ester
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: aq. HF / acetonitrile 2.1: Pd2(dba)3; PPh3; 1,2,2,6,6-pentamethylpiperidine (pempidine) / tetrahydrofuran; dimethylsulfoxide / 16 h / 45 °C 2.2: 60 percent / EtN(i-Pr)2 / butan-1-ol / 4 h / 80 °C View Scheme |
(2S,3R)-2-Allyl-1-((R)-4-benzyl-2-thioxo-oxazolidin-3-yl)-3-hydroxy-pent-4-en-1-one
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: 97 percent / catalytic ring-closing metathesis (RCM) 2.1: 78 percent / LiBH4 / methanol 3.1: Et3N 4.1: Et3N; 4-DMAP 5.1: aq. HF / acetonitrile 6.1: Pd2(dba)3; PPh3; 1,2,2,6,6-pentamethylpiperidine (pempidine) / tetrahydrofuran; dimethylsulfoxide / 16 h / 45 °C 6.2: 60 percent / EtN(i-Pr)2 / butan-1-ol / 4 h / 80 °C View Scheme |
(-)-2-azabicyclo[2.2.1]hept-5-en-3-one
abacavir
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 1.264 g / tetrahydrofuran; H2O / 18 h / 20 - 60 °C 2: 90.5 percent / LiAlH4 / tetrahydrofuran / 19.5 h / 0 °C / Heating 3: 83 percent / Et3N / ethanol / 7 h / Heating 4: 60 percent / butan-1-ol / 21 h / 130 °C View Scheme | |
Multi-step reaction with 5 steps 1: 1.264 g / tetrahydrofuran; H2O / 18 h / 20 - 60 °C 2: 90.5 percent / LiAlH4 / tetrahydrofuran / 19.5 h / 0 °C / Heating 3: 83 percent / Et3N / ethanol / 7 h / Heating 4: 92 percent / triethylorthoformate; HCl / H2O / 4 h 5: 90 percent / methanol / 12 h / 70 °C View Scheme |
abacavir
Conditions | Yield |
---|---|
With hydrogen; palladium on activated charcoal In ethanol under 2585.74 Torr; for 1.5h; Catalytic hydrogenation; | 98% |
ethyl acetate
abacavir
((1S,4R)-4-(2-amino-6-(cyclopropylamino)-9H-purin-9-yl)cyclopent-2-en-1-yl)methyl acetate
Conditions | Yield |
---|---|
With heterogeneous zinc/imidazole catalyst for 6.5h; Inert atmosphere; Schlenk technique; Reflux; chemoselective reaction; | 98% |
abacavir
Conditions | Yield |
---|---|
With sulfuric acid In water; isopropyl alcohol at 50 - 55℃; for 2h; Concentration; Temperature; Solvent; | 95% |
maleic acid
abacavir
(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol maleate
Conditions | Yield |
---|---|
In ethanol at 25 - 30℃; for 0.25h; | 94.3% |
4-dimethylamino-benzaldehyde
abacavir
Conditions | Yield |
---|---|
With acetic acid microwave irradiation; | 89% |
malonic acid
abacavir
(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol malonate
Conditions | Yield |
---|---|
In ethanol at 25 - 70℃; for 0.75h; Product distribution / selectivity; | 88% |
5-fluoro-1H-indole-2,3-dione
abacavir
Conditions | Yield |
---|---|
With acetic acid microwave irradiation; | 87% |
2,2,2-trifluoroethyl benzoate
abacavir
Conditions | Yield |
---|---|
With (μ-oxo)bis[(1,2-ethanediamino-N,N'-bis(salicylidene))iron(III)] In toluene at 120℃; for 5h; Inert atmosphere; Schlenk technique; chemoselective reaction; | 87% |
Conditions | Yield |
---|---|
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 5h; | 85% |
1-ethenesulfonyl-piperidine
abacavir
Conditions | Yield |
---|---|
Stage #1: abacavir With silver(I) acetate; 1,2-bis-(diphenylphosphino)ethane In N,N-dimethyl-formamide at -20℃; Inert atmosphere; Stage #2: 1-ethenesulfonyl-piperidine With potassium hexamethylsilazane In tetrahydrofuran; N,N-dimethyl-formamide at -20℃; for 21h; Inert atmosphere; regioselective reaction; | 85% |
abacavir
Conditions | Yield |
---|---|
With hydrogen bromide In ethanol; water at 25 - 30℃; for 0.75h; Product distribution / selectivity; | 83% |
indole-2,3-dione
abacavir
Conditions | Yield |
---|---|
With acetic acid microwave irradiation; | 82% |
abacavir
(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol hydrobromide
Conditions | Yield |
---|---|
With hydrogen bromide In ethanol; water at 25 - 30℃; for 0.75h; Product distribution / selectivity; | 82% |
5-methyl-indole-2,3-dione
abacavir
Conditions | Yield |
---|---|
With acetic acid microwave irradiation; | 78% |
abacavir
(S)-2-{[(1S,4R)-4-(2-Amino-6-cyclopropylamino-purin-9-yl)-cyclopent-2-enylmethoxy]-phenoxy-phosphorylamino}-propionic acid methyl ester
Conditions | Yield |
---|---|
Stage #1: abacavir With tert-butylmagnesium chloride In tetrahydrofuran at -78℃; Inert atmosphere; Stage #2: C13H18ClN2O5P In tetrahydrofuran at 20℃; Inert atmosphere; | 76% |
tert-butoxyacetic acid
abacavir
Conditions | Yield |
---|---|
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 25 - 30℃; | 74% |
Conditions | Yield |
---|---|
Stage #1: abacavir With pyridine; water; trichlorophosphate In acetonitrile at 0℃; Stage #2: With water; ammonium bicarbonate In acetonitrile at 0℃; pH=8; Stage #3: tetra(n-butyl)ammonium hydroxide In water; acetonitrile | 72% |
abacavir
4-Hydroxyacetophenone
Conditions | Yield |
---|---|
With acetic acid microwave irradiation; | 71% |
tetra(n-butyl)ammonium hydroxide
abacavir
Conditions | Yield |
---|---|
Stage #1: abacavir With trichlorophosphate at 0℃; for 1h; Inert atmosphere; Stage #2: With water for 1h; Cooling with ice; Stage #3: tetra(n-butyl)ammonium hydroxide In water pH=7.0; | 71% |
4-methoxy-benzaldehyde
abacavir
Conditions | Yield |
---|---|
With acetic acid microwave irradiation; | 70% |
Conditions | Yield |
---|---|
Stage #1: 1,10-decanedioic acid With dmap; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; diisopropylamine In N,N-dimethyl-formamide at -20℃; for 0.333333h; Stage #2: abacavir In N,N-dimethyl-formamide at -20 - 20℃; for 16h; | 70% |
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