CASNumber: 75438-57-2 Name: 5-Pyrimidinamine,4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-…Appearance:powder Storage:room temperatur Package:foil bags Application:for pharma Transportation:b
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inquiryProduct Name: Moxonidine Synonyms: MOXONIDINE;MOXONIDINE HCL;4-chloro-n-(4,5-dihydro-1h-imidazol-2-yl)-6-methoxy-2-methyl-5-pyrimidinamin;bdf5895;be5895;BDF-5895 HCL;4-CHLORO-6-METHOXY-2-METHYL-5-(2-IMIDAZO
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inquirySuperior quality, moderate price & quick delivery. Appearance:crystal Storage:Stored in cool, dry and ventilation place; Away from fire and heat Package:1kg/bag, 1kg/drum or 25kg/drum or as per your request. Application:Moxonidine is an ant
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mono-Moxonidine oxalate
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
C
moxonidine
Conditions | Yield |
---|---|
With sodium hydroxide In water at 20℃; for 1h; pH=10 - 11; Product distribution / selectivity; | A n/a B n/a C 94% |
methanol
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
A
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
moxonidine
Conditions | Yield |
---|---|
With potassium carbonate at 65℃; for 3h; Product distribution / selectivity; | A n/a B 90.7% |
methanol
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
C
moxonidine
Conditions | Yield |
---|---|
With sodium hydrogencarbonate In water at 65℃; for 6h; Product distribution / selectivity; | A n/a B n/a C 88.3% |
With potassium hydrogencarbonate In water at 65℃; for 10h; Product distribution / selectivity; | A n/a B n/a C 88.3% |
With potassium hydroxide; potassium carbonate at 20℃; for 16h; Product distribution / selectivity; | A n/a B n/a C 85.9% |
methanol
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
moxonidine
Conditions | Yield |
---|---|
With sodium hydroxide In water at 25℃; for 24h; Product distribution / selectivity; | A n/a B 88.3% |
With potassium hydroxide at 25℃; for 12h; Product distribution / selectivity; | A n/a B 88.3% |
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
sodium methylate
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
C
moxonidine
Conditions | Yield |
---|---|
In methanol at 0 - 65℃; for 1.5 - 48h; Product distribution / selectivity; | A n/a B n/a C 84.7% |
In tetrahydrofuran at 25℃; for 30h; Product distribution / selectivity; | A n/a B n/a C 76.4% |
In toluene at 25℃; for 30h; Product distribution / selectivity; | A n/a B n/a C 66.8% |
methanol
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
moxonidine
Conditions | Yield |
---|---|
With pyrographite; 1,8-diazabicyclo[5.4.0]undec-7-ene at 65℃; for 3.5h; | 84.4% |
With potassium hydroxide at 20℃; for 30h; Product distribution / selectivity; | 83.5% |
With tetrabutylammomium bromide; water; sodium hydroxide In dichloromethane at 20 - 35℃; for 2.5h; pH-value; Reagent/catalyst; Solvent; Temperature; | 3.43 g |
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
moxonidine
Conditions | Yield |
---|---|
With potassium hydroxide In methanol; water at 20℃; for 31h; | 83.5% |
With sodium methylate In methanol; water | |
In tetrahydrofuran; methanol |
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
sodium methylate
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
moxonidine
Conditions | Yield |
---|---|
In methanol at 0℃; for 48h; Product distribution / selectivity; | A n/a B 77.6% |
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
sodium methylate
A
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
moxonidine
Conditions | Yield |
---|---|
In dimethyl sulfoxide at 25℃; for 30h; Product distribution / selectivity; | A n/a B 76.4% |
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
C
moxonidine
Conditions | Yield |
---|---|
Stage #1: 4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine With potassium carbonate In methanol at 47 - 52℃; for 5h; Stage #2: With water; acetic acid In methanol for 0.5h; Stage #3: With ammonia In methanol; water for 1h; Product distribution / selectivity; |
methanol
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
1-[1-((4,6-dichloro-2-methyl-pyrimidin-5-yl)imino)-ethyl]-imidazolidin-2-one
sodium methylate
A
1-[1-[(4-chloro-2-methyl-6-methoxy-pyrimidin-5-yl)imino]ethyl]-imidazolidin-2-one
B
moxonidine
Conditions | Yield |
---|---|
at 20℃; | A 0.12 %Chromat. B 96.66 %Chromat. |
methanol
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
sodium methylate
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
C
moxonidine
Conditions | Yield |
---|---|
for 2h; Heating / reflux; | A 1.45 - 1.48 %Chromat. B 5.27 - 5.32 %Chromat. C 93.22 - 93.25 %Chromat. |
methanol
4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine
sodium methylate
moxonidine
Conditions | Yield |
---|---|
at 30 - 35℃; for 0.75h; | 520 mg |
5-amino-4-methoxy-6-chloro-2-methyl-pyrimidine
moxonidine
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: sodium carbonate; trichlorophosphate / dimethyl sulfoxide / 49 h / 5 - 60 °C / Inert atmosphere 2: hydrogenchloride / isopropyl alcohol / 8 h / 20 °C 3: base / water / pH 9 View Scheme |
moxonidine
Conditions | Yield |
---|---|
With base In water pH=9; |
1-acetylimidazolidin-2-one
5-amino-4-methoxy-6-chloro-2-methyl-pyrimidine
moxonidine
Conditions | Yield |
---|---|
Stage #1: 1-acetylimidazolidin-2-one; 5-amino-4-methoxy-6-chloro-2-methyl-pyrimidine With sodium carbonate; trichlorophosphate In dimethyl sulfoxide at 5 - 60℃; for 50.5h; Cooling with acetone-dry ice; Inert atmosphere; Stage #2: With hydrogenchloride In water; isopropyl alcohol at 20℃; for 8h; |
oxalic acid
moxonidine
A
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
mono-Moxonidine oxalate
Conditions | Yield |
---|---|
In methanol; diethyl ether Product distribution / selectivity; Heating / reflux; | A n/a B 95% |
In methanol; propan-1-ol at 0 - 20℃; for 3.5h; Product distribution / selectivity; Heating / reflux; | A n/a B 83.6% |
In propan-1-ol; dimethyl sulfoxide Product distribution / selectivity; Heating / reflux; | A n/a B 58% |
formic acid
moxonidine
A
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
mono-Moxonidine formate
Conditions | Yield |
---|---|
In propan-1-ol at 0 - 20℃; for 4h; Product distribution / selectivity; Heating / reflux; | A n/a B 92.7% |
In isopropyl alcohol at 0 - 20℃; for 4h; Product distribution / selectivity; Heating / reflux; | A n/a B 85% |
In N,N-dimethyl-formamide at 0 - 20℃; for 4h; Product distribution / selectivity; Heating / reflux; | A n/a B 84% |
In dimethyl sulfoxide at 0 - 20℃; for 4h; Product distribution / selectivity; Heating / reflux; | A n/a B 66% |
oxalic acid
moxonidine
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
mono-Moxonidine oxalate
Conditions | Yield |
---|---|
In propan-1-ol at 0 - 20℃; for 2h; Product distribution / selectivity; Heating / reflux; | A n/a B 87.3% |
oxalic acid
moxonidine
A
4,6-dichloro-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
B
4,6-dimethoxy-2-methyl-5-(2-imidazolin-2-yl)-aminopyrimidine
C
mono-Moxonidine oxalate
Conditions | Yield |
---|---|
In methanol; propan-1-ol at 0 - 20℃; for 3.5h; Heating / reflux; | A n/a B n/a C 87% |
moxonidine
4-methoxy-2-methyl-6-methylthio-5-(2-imidazolin-2-yl)-aminopyrimidine
Conditions | Yield |
---|---|
In toluene |
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