6628-77-9

Basic information

• Product Name: 5-Amino-2-methoxypyridine
• Synonyms: 3-PYRIDINAMINE, 6-METHOXY-;5-AMINO-2-METHOXYPYRIDINE;6-Methoxy-3-pyridylamine;6-METHOXY-PYRIDIN-3-YLAMINE;2-METHOXY-5-AMINOPYRIDINE;OTAVA-BB BB7020410079;3-Amino-6-methoxypyridine;5-amino-2-methoxy-pyridin
• CAS NO: 6628-77-9
• Molecular Formula: C₆H₈N₂O
• Molecular Weight: 124.14
• EINECS: 229-612-8
• Product Categories: piridines;Pyridine;Pyridines, Pyrimidines, Purines and Pteredines;Pyridine series;Pyridines derivates;Pyridines;Boronic Acid;C6;Heterocyclic Building Blocks;Amino-pyridine series
• Mol File: 6628-77-9.mol
• Article Data: 23

Chemical Properties

• Melting Point: 29-31 °C(lit.)
• Boiling Point: 85-90 °C1 mm Hg(lit.)
• Flash Point: >230 °F
• Appearance: Yellow-brown or red to very dark red/Liquid
• Density: 1.575
• Vapor Pressure: 0.00951mmHg at 25°C
• Refractive Index: n20/D 1.575(lit.)
• Storage Temp.: 2-8°C
• Solubility: Chloroform, Methanol (Slightly)
• PKA: 4.33±0.10(Predicted)
• Water Solubility: Slightly soluble
• CAS DataBase Reference: 5-Amino-2-methoxypyridine(CAS DataBase Reference)
• NIST Chemistry Reference: 5-Amino-2-methoxypyridine(6628-77-9)
• EPA Substance Registry System: 5-Amino-2-methoxypyridine(6628-77-9)

Safety Data

• Hazard Codes: Xn,Xi
• Statements: 22-36/37/38
• Safety Statements: 26-37/39-36
• WGK Germany: 3
• RTECS: US1836000
• HazardClass: IRRITANT
• Hazardous Substances Data: 6628-77-9(Hazardous Substances Data)

Usage

Chemical Properties

yellow-brown or red to very dark red liquid

Uses

5-Amino-2-methoxypyridine is used as a reagent in the synthesis of a novel series of thienopyrimidines as highly potent and selective PI3K inhibitors. 5-Amino-2-methoxypyridine is also used to synthesize EMPA (E521550); a novel high-affinity selective antagonist for the OX2 receptor.

InChI:InChI=1/C6H8N2O/c1-9-6-3-2-5(7)4-8-6/h2-4H,7H2,1H3

Synthetic route

2-methoxy-5-nitropyridine (5446-92-4) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
With potassium fluoride; polymethylhydrosiloxane; palladium diacetate In tetrahydrofuran at 20℃; for 0.5h;	100%
With cyclohexa-1,4-diene; 5%-palladium/activated carbon In methanol at 120℃; for 0.0833333h; Microwave irradiation;	99%
With iron; calcium chloride In ethanol for 2h; Heating;	97%

2-methoxy-5-bromopyridine (13472-85-0) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
With copper(l) iodide; 2-carboxyquinoline N-oxide; potassium carbonate; ammonium hydroxide In dimethyl sulfoxide at 80℃; for 23h; Inert atmosphere;	95%
With ammonium hydroxide; potassium phosphate; 1-(5,6,7,8-tetrahydroquinolin-8-yl)-2-methylpropan-1-one; copper(I) bromide In dimethyl sulfoxide at 110℃; for 24h; Inert atmosphere; Sealed tube;	86%
Multi-step reaction with 2 steps 1.1: copper(l) iodide; potassium carbonate; L-proline / dimethyl sulfoxide / Inert atmosphere 1.2: 80 °C / Inert atmosphere 2.1: palladium on activated charcoal; ammonium formate / methanol / Reflux View Scheme

2-methoxy-5-nitropyridine N-oxide (96530-77-7) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
With iron In acetic acid	89%

2-chloro-5-nitropyridine (4548-45-2) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
With sodium hydroxide anschliessendes Hydrieren an Palladium/CaCO3;
Multi-step reaction with 2 steps 2: iron-powder; acetic acid; aqueous methanol View Scheme
Multi-step reaction with 2 steps 2: platinum; ethanol / Hydrogenation View Scheme

2-bromo-6-methoxy-3-nitropyridine → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
With hydrogen; Lindlar's catalyst In ethanol

6-methyoxy-3-pyridinecarboxamide (7150-23-4) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
With sodium hydroxide; bromine In tetrahydrofuran at 5 - 70℃; Hoffmann rearrangement;

2-chloro-5-nitropyridine (4548-45-2) + potassium-salt of/the/ 4-acetylamino-benzenesulfinic acid → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
Multi-step reaction with 2 steps 1: 82 percent / NaH / tetrahydrofuran / 1 h / Ambient temperature 2: hydrogen / 5 percent Pd/C / methanol / 760 Torr / Ambient temperature View Scheme
Multi-step reaction with 2 steps 1: 99 percent / 1.) sodium metal / 24 h / 70 °C / Heating 2: cyclohexene / 5percent Pd-C / ethanol / Heating View Scheme

6-bromo-2-methoxypyridine (40473-07-2) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
Multi-step reaction with 2 steps 1: 89 percent / potassium nitrate, concd. H2SO4 / 2 h / 75 °C 2: H2 / 5percent Pd/CaCO3 / ethanol View Scheme

2-iodo-5-nitropyridine (28080-54-8) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
Multi-step reaction with 2 steps 1: sodium methylate; methanol 2: SnCl2; HCl; diethyl ether View Scheme

N-benzyl-6-methoxypyridin-3-amine (342793-48-0) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
With palladium on activated charcoal; ammonium formate In methanol Reflux;

5-nitro-pyridin-2-ylamine (4214-76-0) → 6-methoxy-pyridin-3-ylamine (6628-77-9)

Conditions	Yield
Multi-step reaction with 4 steps 1: hydrogenchloride; sodium nitrite / water / 0.67 h / 0 - 6 °C 2: trichlorophosphate / N,N-dimethyl-formamide / 2 h / 20 °C / Reflux 3: methanol / 1 h / Reflux 4: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 60 °C / 7500.75 Torr View Scheme
Multi-step reaction with 4 steps 1: sodium hydroxide / Reflux 2: trichlorophosphate / N,N-dimethyl-formamide / Reflux 3: Reflux 4: iron; acetic acid / ethanol / Reflux View Scheme

6-methoxy-pyridin-3-ylamine (6628-77-9) + diethyl 2-ethoxymethylenemalonate (87-13-8) → diethyl {[(6-methoxypyridin-3-yl)amino]methylidene}propanedioate (53241-90-0)

Conditions	Yield
In ethanol for 4h; Heating / reflux;	100%
In ethanol for 4h; Heating / reflux;	100%
In ethanol for 4h; Heating / reflux;	100%

6-methoxy-pyridin-3-ylamine (6628-77-9) → 2-bromo-6-methoxy-pyridin-3-ylamine (135795-46-9)

Conditions	Yield
With bromine; sodium acetate In acetic acid at 20℃; for 0.5h;	100%
With hydrogen bromide; dihydrogen peroxide In water at 5 - 20℃;	97%
With bromine; sodium acetate In acetic acid for 0.333333h;	60%

6-methoxy-pyridin-3-ylamine (6628-77-9) + pivaloyl chloride (3282-30-2) → 2,2-dimethyl-N-<5-(2-methoxypyridinyl)>propanamide (227180-19-0)

Conditions	Yield
With triethylamine In dichloromethane for 0.5h; Cooling with ice;	100%
With triethylamine In dichloromethane 0 deg C, 10 min; RT, 2h;	99%
With triethylamine In dichloromethane at 0 - 20℃; for 2.16667h;

6-methoxy-pyridin-3-ylamine (6628-77-9) → 6-methoxypyridin-3-diazonium tetrafluoroborate

Conditions	Yield
With tetrafluoroboric acid; sodium nitrite In ethanol; water at 0℃; for 3h;	100%
With tetrafluoroboric acid; sodium nitrite In ethanol; water at 0℃; for 3h; Product distribution / selectivity;	91%
With tetrafluoroboric acid; sodium nitrite In ethanol; water at 0℃; for 2h;	91%
Stage #1: 6-methoxy-pyridin-3-ylamine With boron trifluoride diethyl etherate In tetrahydrofuran for 0.0833333h; Cooling with ice; Stage #2: With tert.-butylnitrite In tetrahydrofuran at 0℃;	80%
With tetrafluoroboric acid; sodium nitrite at 5℃;	72%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 3,3-tetramethylene glutaric anhydride (5662-95-3) → 8-(6-methoxypyridin-3-yl)-8-azaspiro[4.5]decane-7,9-dione hydrochloride

Conditions	Yield
Stage #1: 6-methoxy-pyridin-3-ylamine; 3,3-tetramethylene glutaric anhydride In dichloromethane at 20℃; for 3h; Stage #2: With thionyl chloride In dichloromethane at 20℃; for 3.5h;	100%
Stage #1: 6-methoxy-pyridin-3-ylamine; 3,3-tetramethylene glutaric anhydride In dichloromethane at 20℃; for 3h; Stage #2: With thionyl chloride In dichloromethane at 20℃; for 3.5h;	100%

6-methoxy-pyridin-3-ylamine (6628-77-9) + cyclohexanylcarbonyl chloride (2719-27-9) → cyclohexanecarboxylic acid (6-methoxy-pyridin-3-yl)-amide hydrochloride (548763-48-0)

Conditions	Yield
In tetrahydrofuran; diethyl ether	100%

6-methoxy-pyridin-3-ylamine (6628-77-9) + cyclohexylacetic acid chloride (23860-35-7) → 2-Cyclohexyl-N-(6-methoxy-pyridin-3-yl)-acetamide hydrochloride (548763-51-5)

Conditions	Yield
In tetrahydrofuran; diethyl ether	100%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 5-methoxymethylene-2,2-dimethyl-1,3-dioxane-4,6-dione (15568-85-1) → 5-[[(6-methoxypyridin-3-yl)amino]methylidene]-2,2-dimethyl-1,3-dioxane-4,6-dione (25063-69-8)

Conditions	Yield
In isopropyl alcohol Heating;	100%
In isopropyl alcohol at 70℃; for 0.5h;
In isopropyl alcohol for 1h; Heating / reflux;

6-methoxy-pyridin-3-ylamine (6628-77-9) + 3,4-diethoxy-3-cyclobuten-1,2-dione (5231-87-8) → C12H12N2O4 (1018682-14-8)

Conditions	Yield
In methanol; water for 0.5h; Heating;	100%

1,2,3-triazole (288-36-8) + 6-methoxy-pyridin-3-ylamine (6628-77-9) + C12H13ClN2O2 (864178-16-5) → 5-[3-(4-ethoxy-3-methyl-phenyl)-5-[1,2,3]triazol-2-ylmethyl-[1,2,4]triazol-4-yl]-2-methoxy-pyridine + 5-[3-(4-ethoxy-3-methyl-phenyl)-5-[1,2,3]triazol-1-ylmethyl-[1,2,4]triazol-4-yl]-2-methoxy-pyridine

Conditions	Yield
Stage #1: 1,2,3-triazole; C12H13ClN2O2 With potassium carbonate In DMF (N,N-dimethyl-formamide); acetonitrile for 18h; Stage #2: 6-methoxy-pyridin-3-ylamine; toluene-4-sulfonic acid In xylene at 140℃; for 6h;	A 100% B 100%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 1,1'-Thiocarbonyldiimidazole (6160-65-2) → 5-isothiocyanato-2-methoxypyridine (52023-93-5)

Conditions	Yield
In tetrahydrofuran	100%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 3-methoxyphenylacetic acid chloride (6834-42-0) → 2-(3-methoxyphenyl)-N-{2-methoxy(5-pyridyl)}acetamide (295318-90-0)

Conditions	Yield
	99%

6-methoxy-pyridin-3-ylamine (6628-77-9) + trimethylpyruvic acid (815-17-8) → C12H18N2O3 (1028253-88-4)

Conditions	Yield
Stage #1: 6-methoxy-pyridin-3-ylamine; trimethylpyruvic acid With sodium tris(acetoxy)borohydride In 1,2-dichloro-ethane for 24h; Stage #2: With water; ammonium chloride In 1,2-dichloro-ethane	99%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 4-(chlorosulfonyl)benzenesulfonyl fluoride → C12H11FN2O5S2

Conditions	Yield
With pyridine In chloroform at 20℃; for 48h; chemoselective reaction;	99%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 2,4-dichloroquinazoline (607-68-1) → 2-chloro-N-(6-methoxypyridin-3-yl)quinazolin-4-amine

Conditions	Yield
With sodium acetate In tetrahydrofuran; water at 60℃; for 0.75h;	98%
With sodium acetate In tetrahydrofuran; water at 60℃; for 0.75h;	98%

6-methoxy-pyridin-3-ylamine (6628-77-9) + di-tert-butyl dicarbonate (24424-99-5) → tert-butyl N-(6-methoxypyridin-3-yl)carbamate (183741-80-2)

Conditions	Yield
In 1,4-dioxane Reflux;	97%
In 1,4-dioxane	96%
In 1,4-dioxane for 0.5h; Heating;	94%

6-methoxy-pyridin-3-ylamine (6628-77-9) + ammonium thiocyanate (1147550-11-5) → 5-methoxythiazolo[5,4-b]pyridin-2-amine (13797-77-8)

Conditions	Yield
Stage #1: 6-methoxy-pyridin-3-ylamine; ammonium thiocyanate In acetonitrile at 20℃; for 0.166667h; Stage #2: With benzyltrimethylazanium tribroman-2-uide In acetonitrile at 20℃;	97%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 3-(2-Chloro-4-phenylamino-pyrimidin-5-yl)-2-(4-methoxy-phenyl)-propionic acid methyl ester (710324-65-5) → 3-[2-(6-Methoxy-pyridin-3-ylamino)-4-phenylamino-pyrimidin-5-yl]-2-(4-methoxy-phenyl)-propionic acid methyl ester (710324-66-6)

Conditions	Yield
In ethyl acetate at 110℃; for 4h;	96.8%

6-methoxy-pyridin-3-ylamine (6628-77-9) + phenyl chloroformate (1885-14-9) → (6-methoxy-pyridin-3-yl)-carbamic acid phenyl ester (102671-59-0)

Conditions	Yield
With pyridine In tetrahydrofuran at 0 - 20℃; for 12h;	96%
With pyridine In tetrahydrofuran at 0 - 20℃;	96%
With pyridine In tetrahydrofuran at 0 - 20℃;	96%

6-methoxy-pyridin-3-ylamine (6628-77-9) + methyl 2-chloropyridine-3-carboxylate (40134-18-7) → methyl 2-(6-methoxy-3-pyridinyl)aminonicotinate (1239165-03-7)

Conditions	Yield
With caesium carbonate; tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene In toluene at 90℃; for 72h;	96%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 2,2,2-Trichloroethyl chloroformate (17341-93-4) → 2,2,2-trichloroethyl (6-methoxypyridin-3-yl)carbamate (887624-73-9)

Conditions	Yield
With pyridine In tetrahydrofuran at 0℃; for 0.5h;	95.4%

6-methoxy-pyridin-3-ylamine (6628-77-9) + cycl-isopropylidene malonate (2033-24-1) + orthoformic acid triethyl ester (122-51-0) → 5-[[(6-methoxypyridin-3-yl)amino]methylidene]-2,2-dimethyl-1,3-dioxane-4,6-dione (25063-69-8)

Conditions	Yield
In ethanol for 1h; Reflux; Large scale;	95%
In ethanol for 1h; Reflux; Large scale;	95%
In ethanol for 1h; Reflux; Large scale;	95%

6-methoxy-pyridin-3-ylamine (6628-77-9) → 5-hydrazinyl-2-methoxy pyridine (160664-95-9)

Conditions	Yield
Stage #1: 6-methoxy-pyridin-3-ylamine With hydrogenchloride; sodium nitrite In water at 0℃; for 0.5h; Stage #2: With hydrogenchloride; tin(II) chloride dihdyrate In water at 0℃; for 2.5h; Stage #3: With potassium hydroxide In water	95%
Stage #1: 6-methoxy-pyridin-3-ylamine With hydrogenchloride; sodium nitrite In water at 0℃; for 0.5h; Stage #2: With hydrogenchloride; tin(II) chloride dihdyrate In water at 0℃; for 2.5h;	95%
Stage #1: 6-methoxy-pyridin-3-ylamine With hydrogenchloride; water; sodium nitrite at 0 - 5℃; Stage #2: With hydrogenchloride; tin(ll) chloride at -25 - -20℃; for 2.5h; Stage #3: With water; potassium hydroxide In dichloromethane at 0 - 5℃; for 1.5h;	70%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 2-(4-(2-bromobenzoyl)phenoxy)acetic acid → 2-[4-(2-bromobenzoyl)phenoxy]-N-(6-methoxypyridin-3-yl)acetamide

Conditions	Yield
With triethylamine; 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℃;	94%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 2-[(5-fluoropyridine-2-carbonyl)amino]malonic acid diethyl ester (787564-31-2) → 5-(5-fluoro-2-pyridyl)-1-(6-methoxy-3-pyridyl)-1H-1,2,4-triazole-3-carboxylic acid sodium salt (787564-29-8)

Conditions	Yield
Stage #1: 6-methoxy-pyridin-3-ylamine With hydrogenchloride; acetic acid; sodium nitrite In water at 0℃; for 0.25h; Stage #2: 2-[(5-fluoropyridine-2-carbonyl)amino]malonic acid diethyl ester With potassium carbonate In water; acetone at -15 - 0℃; for 2.5h; Stage #3: With sodium methylate In methanol at 20℃; for 60h;	93%

6-methoxy-pyridin-3-ylamine (6628-77-9) + tert-butyl 6-oxo-3-azabicyclo[3.1.1]heptane-3-carboxylate → tert-butyl 6-((6-methoxypyridin-3-yl)amino)-3-azabicyclo[3.1.1]heptane-3-carboxylate

Conditions	Yield
With nido-decaborane In methanol; trans-1,2-dichloroethylene at 20℃; Inert atmosphere;	93%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 1,1'-Thiocarbonyldi-2(1H)-pyridone (102368-13-8) → 5-isothiocyanato-2-methoxypyridine (52023-93-5)

Conditions	Yield
In dichloromethane at 0 - 20℃; for 3.5h;	92%

6-methoxy-pyridin-3-ylamine (6628-77-9) + 4-fluorophthalic anhydride (319-03-9) → 5-fluoro-2-(6-methoxypyridin-3-yl)isoindoline-1,3-dione

Conditions	Yield
With sodium acetate; acetic acid at 118℃; for 2h;	91.4%

Upstream product

• 5418-51-9 5-nitro-2-hydroxypyridine 
• 504-29-0 2-aminopyridine 
• 4214-76-0 5-nitro-pyridin-2-ylamine 
• 342793-48-0 N-benzyl-6-methoxypyridin-3-amine 
• 13472-85-0 2-methoxy-5-bromopyridine 
• 28080-54-8 2-iodo-5-nitropyridine 
• 40473-07-2 6-bromo-2-methoxypyridine 
• 4548-45-2 2-chloro-5-nitropyridine 
• 7150-23-4 6-methyoxy-3-pyridinecarboxamide 
• 344296-05-5 2-bromo-6-methoxy-3-nitropyridine 
• 96530-77-7 2-methoxy-5-nitropyridine N-oxide 
• 5446-92-4 2-methoxy-5-nitropyridine 

Downstream Products

• 183741-80-2 tert-butyl N-(6-methoxypyridin-3-yl)carbamate 
• 118420-41-0 (E)-N-[4-(4-Benzhydryl-piperazin-1-yl)-butyl]-3-(6-methoxy-pyridin-3-yl)-acrylamide 
• 352228-92-3 4-Chloro-2-nitro-N-(6-methoxy-3-pyridyl)-benzoylamide 
• 179543-88-5 5-hydrazinyl-2-methoxypyridine hydrochloride 
• 160664-95-9 5-hydrazinyl-2-methoxy pyridine 
• 112860-04-5 ICIA0858 
• 25063-69-8 5-[[(6-methoxypyridin-3-yl)amino]methylidene]-2,2-dimethyl-1,3-dioxane-4,6-dione 
• 137081-15-3 N-(2-methoxy-5-pyridyl)-1-fluorocyclopropanecarboxamide 
• 342793-48-0 N-benzyl-6-methoxypyridin-3-amine 
• 227180-19-0 2,2-dimethyl-N-<5-(2-methoxypyridinyl)>propanamide 
• 138305-11-0 4-Hydroxy-N-(2-methoxypyridin-5-yl)-2-oxo-1-phenyl-1H-1,8-naphthyridine-3-carboxamide 
• 123534-01-0 N-(phenylmethylene)-5-amino-2-methoxypyridine 
• 13797-77-8 5-methoxythiazolo[5,4-b]pyridin-2-amine 
• 100724-26-3 N-(6-methoxy-[3]pyridyl)-anthranilic acid 

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