3430-22-6

Basic information

• Product Name: 3-Bromo-4-methylpyridine
• Synonyms: 4-METHYL-3-BROMOPYRIDINE;3-BROMO-4-PICOLINE;3-BROMO-4-METHYLPYRIDINE;3-BROMO-4-METHYLPYRIDINE 98%;3-BROMO-4-METHYLPYRIDINE 99+%;Bromomethylpyridine;3-BROMO-4-METHYLPYRIDINE (3-BROMO-4-PICOLINE);4-Methyl-3-bromopyridine 3-Bromo-4-picoline
• CAS NO: 3430-22-6
• Molecular Formula: C₆H₆BrN
• Molecular Weight: 172.02
• EINECS: 1592732-453-0
• Product Categories: blocks;Bromides;Pyridines;Pyridine;Pyridines, Pyrimidines, Purines and Pteredines;Halides;Pyridines derivates;Aromatics Compounds;Bromopyridines;Halopyridines;Aromatics;C6Heterocyclic Building Blocks;Halogenated Heterocycles;Heterocyclic Building Blocks;Brominated heterocyclic series;Pyridine Series;Heterocycles;Heterocycle-Pyridine series;alkyl bromide
• Mol File: 3430-22-6.mol
• Article Data: 10

Chemical Properties

• Boiling Point: 199-200 °C(lit.)
• Flash Point: 175 °F
• Appearance: Clear colorless to yellow/Liquid
• Density: 1.549 g/mL at 25 °C(lit.)
• Refractive Index: n20/D 1.56(lit.)
• Storage Temp.: Inert atmosphere,Room Temperature
• Solubility: Chloroform, Methanol
• PKA: 3.54±0.18(Predicted)
• BRN: 878354
• CAS DataBase Reference: 3-Bromo-4-methylpyridine(CAS DataBase Reference)
• NIST Chemistry Reference: 3-Bromo-4-methylpyridine(3430-22-6)
• EPA Substance Registry System: 3-Bromo-4-methylpyridine(3430-22-6)

Safety Data

• Hazard Codes: Xi,Xn
• Statements: 36/37/38-20/21/22
• Safety Statements: 26-36-2636
• RIDADR: Cool, dry,tightly closed
• WGK Germany: 3
• HazardClass: IRRITANT
• PackingGroup: III
• Hazardous Substances Data: 3430-22-6(Hazardous Substances Data)

Usage

Chemical Properties

Clear Liquid

Uses

Different sources of media describe the Uses of 3430-22-6 differently. You can refer to the following data:
1. An intermediate of pyridinyl pyrrole compounds as proton pump inhibitors with improved gastric acid secretion suppressive activity
2. 3-Bromo-4-methylpyridine may be used as a building block in the preparation of:substituted 4-(2,2-diphenylethyl)pyridine-N-oxides for use as potent phosphodiesterase type 4 (PDE4) inhibitorsbenzodiazepine site ligands bearing tricyclic pyridone moiety for human GABAA receptora novel isomer of ascididemin3-bromopyridine-4-carbonitrile

Synthetic route

3-amino-4-methylpyridine (3430-27-1) → 3-Bromo-4-methylpyridin (3430-22-6)

Conditions	Yield
Stage #1: 3-amino-4-methylpyridine With hydrogen bromide; bromine at -5℃; Stage #2: With sodium nitrite In water at 0℃; Stage #3: With sodium hydroxide In water at 0 - 20℃; for 0.5h; pH=9;	95%
Stage #1: 3-amino-4-methylpyridine With hydrogen bromide; bromine at -5℃; Stage #2: With sodium nitrite at 0℃; Stage #3: With sodium hydroxide at 20℃; for 0.5h; pH=9;

picoline (108-89-4) → 3-Bromo-4-methylpyridin (3430-22-6)

Conditions	Yield
Stage #1: picoline With aluminum (III) chloride; potassium bromide at 20℃; for 1h; Inert atmosphere; Stage #2: With bromine at 120℃; for 27h; Inert atmosphere;	57%
With aluminum (III) chloride; bromine at 95 - 105℃; for 43h; Inert atmosphere;	49%
Stage #1: picoline With aluminum (III) chloride; bromine at 95 - 100℃; for 22h; Stage #2: With sodium carbonate In water	19%
With hydrogenchloride; sodium hydroxide; bromine; aluminium trichloride In (2S)-N-methyl-1-phenylpropan-2-amine hydrate; dichloromethane; Petroleum ether
Stage #1: picoline With aluminum (III) chloride at -5℃; for 1h; Stage #2: With bromine at 100℃; for 44h;

3-Bromopyridine (626-55-1) + lithium diisopropyl amide (4111-54-0) + methyl iodide (74-88-4) → 4-bromopyridin (1120-87-2) + 4-bromo-3-methylpyridine (10168-00-0) + 3-Bromo-4-methylpyridin (3430-22-6)

Conditions	Yield
In tetrahydrofuran at -60℃; Product distribution; Mechanism; temp. change;

3-Bromopyridine (626-55-1) + methyl iodide (74-88-4) → 4-bromo-3-methylpyridine (10168-00-0) + 3-Bromo-4-methylpyridin (3430-22-6)

Conditions	Yield
THF, -60 -> -55.deg C, 1) 15 min, 2) 45 min; Yield given. Multistep reaction. Yields of byproduct given;

3-Bromopyridine (626-55-1) + methyl iodide (74-88-4) → 3-Bromo-4-methylpyridin (3430-22-6)

Conditions	Yield
THF, -60.deg C, 1) 15 min, 2) 45 min; Yield given. Multistep reaction;

3-Bromo-4-methyl-4H-pyridine-1-carboxylic acid phenyl ester (90731-85-4) → 3-Bromo-4-methylpyridin (3430-22-6)

Conditions	Yield
With o-tetrachloroquinone In acetic acid for 8h; Ambient temperature; Yield given;

3-Bromopyridine (626-55-1) → 3-Bromo-4-methylpyridin (3430-22-6)

Conditions	Yield
Multi-step reaction with 2 steps 1: 1.) CuI, (CH3)2S / 1.) THF, -20 deg C, 5 min, 2.) THF, a) -20 deg C, 15 min, b) RT, 15 min 2: o-chloranil / acetic acid / 8 h / Ambient temperature View Scheme

3-Bromo-4-methylpyridin (3430-22-6) + 2,4-dimethoxypyrimidin-5-ylboronic acid (89641-18-9) → 5-(4-methyl-pyridin-3-yl)-2,4-dimethoxy-pyrimidine (952403-13-3)

Conditions	Yield
With sodium carbonate; palladium diacetate; triphenylphosphine In propan-1-ol for 3h; Suzuki Coupling; Heating / reflux;	100%

3-Bromo-4-methylpyridin (3430-22-6) + Diethyl carbonate (105-58-8) → ethyl 2-(3-bromopyridin-4-yl)acetate (51054-99-0)

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With lithium hexamethyldisilazane In tetrahydrofuran at 20℃; for 2.5h; Stage #2: Diethyl carbonate In tetrahydrofuran for 12h;	100%
Stage #1: 3-Bromo-4-methylpyridin; Diethyl carbonate With lithium hexamethyldisilazane In tetrahydrofuran at 0℃; for 5h; Stage #2: With lithium hexamethyldisilazane In tetrahydrofuran at 20℃; for 2h;	91%
With lithium hexamethyldisilazane In tetrahydrofuran at 0℃; for 3h; Inert atmosphere;	68.2%
Stage #1: 3-Bromo-4-methylpyridin With lithium hexamethyldisilazane In tetrahydrofuran at 20℃; Stage #2: Diethyl carbonate In tetrahydrofuran at 20℃;	63%

2-formyl-4,5-(methylenedioxy)benzeneboronic acid (94838-88-7) + 3-Bromo-4-methylpyridin (3430-22-6) → 6-(4-methyl-pyridin-3-yl)-benzo[1,3]dioxole-5-carbaldehyde (1086561-33-2)

Conditions	Yield
With sodium carbonate; tetrakis(triphenylphosphine) palladium(0) In methanol; water; toluene at 90℃; for 15h; Suzuki coupling;	98%

benzo[b]thiophene-2-boronic acid (98437-23-1) + 3-Bromo-4-methylpyridin (3430-22-6) → 3-(benzo[b]thiophen-2-yl)-4-methylpyridine (1443643-88-6)

Conditions	Yield
With C43H37ClFeNiP2*C4H8O; potassium carbonate In tetrahydrofuran; acetonitrile at 50℃; for 12h; Suzuki-Miyaura Coupling; Inert atmosphere;	97%

thiophene boronic acid (6165-68-0) + 3-Bromo-4-methylpyridin (3430-22-6) → 4-methyl-3-(thiophen-2-yl)pyridine (504395-36-2)

Conditions	Yield
With potassium phosphate; C43H37ClFeNiP2*C4H8O In 1,4-dioxane at 70℃; for 8h; Suzuki-Miyaura Coupling; Inert atmosphere;	97%

4-acetylphenylboronic acid (149104-90-5) + 3-Bromo-4-methylpyridin (3430-22-6) → 1-(4-(4-methylpyridin-3-yl)phenyl)ethan-1-one

Conditions	Yield
With tetrakis(triphenylphosphine) palladium(0); sodium carbonate In water; toluene at 120℃; for 10h; Suzuki Coupling;	97%

carbonic acid dimethyl ester (616-38-6) + 3-Bromo-4-methylpyridin (3430-22-6) + methyl iodide (74-88-4) → methyl 2-(3-bromopyridin-4-yl)propanoate

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With lithium hexamethyldisilazane In tetrahydrofuran; ethylbenzene at 20℃; for 3h; Stage #2: carbonic acid dimethyl ester In tetrahydrofuran; ethylbenzene at 0 - 20℃; Stage #3: methyl iodide In tetrahydrofuran; ethylbenzene at -70 - 20℃;	97%

carbonic acid dimethyl ester (616-38-6) + 3-Bromo-4-methylpyridin (3430-22-6) → methyl 2-(3-bromopyridin-4-yl)acetate (162615-12-5)

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With lithium hexamethyldisilazane In tetrahydrofuran for 1.5h; Stage #2: carbonic acid dimethyl ester In tetrahydrofuran for 15h;	96%
Stage #1: 3-Bromo-4-methylpyridin With lithium hexamethyldisilazane In tetrahydrofuran; ethylbenzene at 20℃; for 3h; Stage #2: carbonic acid dimethyl ester In tetrahydrofuran; ethylbenzene at 0 - 20℃;	95%
With lithium hexamethyldisilazane In tetrahydrofuran at 0 - 20℃; for 2.5h;	85%
With n-butyllithium; diisopropylamine 1.) THF, hexane, r.t. to 50 deg C, 2.) THF, hexane, 50 deg C; r.t., 24 h; Yield given. Multistep reaction;

2-formylbenzene boronic acid (40138-16-7) + 3-Bromo-4-methylpyridin (3430-22-6) → 2-(4-methyl-pyridin-3-yl)-benzaldehyde (1086561-21-8)

Conditions	Yield
With tetrakis(triphenylphosphine) palladium(0); sodium carbonate In methanol; water; toluene at 90℃; for 15h; Inert atmosphere;	96%
With sodium carbonate; tetrakis(triphenylphosphine) palladium(0) In methanol; water; toluene at 90℃; for 15h; Suzuki coupling;	94%
With tetrakis(triphenylphosphine) palladium(0); sodium carbonate In tetrahydrofuran; water at 70℃; for 12h; Suzuki Coupling;	85%

methylamine (74-89-5) + 3-Bromo-4-methylpyridin (3430-22-6) → 4-Methyl-3-(methylamino)pyridine (77862-24-9)

Conditions	Yield
With copper In water at 150 - 160℃; Temperature; Reagent/catalyst;	95%
With copper In water at 100 - 110℃; for 24h; Temperature; Autoclave;	93%
With copper(II) sulfate	68%

Methyl formate (107-31-3) + 3-Bromo-4-methylpyridin (3430-22-6) → 4-methylnicotinaldehyde (51227-28-2)

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With n-butyllithium In tetrahydrofuran at -100℃; for 0.166667h; Stage #2: Methyl formate In tetrahydrofuran at -96 - -78℃; for 1h;	95%

3-[4-methoxymethyl-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yl]-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1-(2-trimethylsilanyl-ethoxymethyl)-1H-pyrazolo[3,4-b]pyridine (916326-87-9) + 3-Bromo-4-methylpyridin (3430-22-6) → 3-[4-methoxymethyl-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yl]-5-(4-methyl-pyridin-3-yl)-1-(2-trimethylsilanyl-ethoxymethyl)-1H-pyrazolo[3,4-b]pyridine (916326-94-8)

Conditions	Yield
With sodium carbonate; tetrakis(triphenylphosphine) palladium(0) In 1,4-dioxane; water at 90℃;	95%

N-boc-2-pyrroleboronic acid (135884-31-0) + 3-Bromo-4-methylpyridin (3430-22-6) → tert-butyl 2-(4-methylpyridin-3-yl)-1H-pyrrole-1-carboxylate (1443644-02-7)

Conditions	Yield
With potassium phosphate; C43H37ClFeNiP2*C4H8O In 1,4-dioxane at 70℃; for 8h; Suzuki-Miyaura Coupling; Inert atmosphere;	95%

3-Bromo-4-methylpyridin (3430-22-6) → 3-amino-4-methylpyridine (3430-27-1)

Conditions	Yield
With ammonia; copper(II) sulfate In methanol at 160℃; under 3800.26 Torr; for 8h; Temperature; Autoclave;	95%
With ammonium hydroxide; L-2-O-methyl-chiro-inositol; copper(II) acetate monohydrate In 1-methyl-pyrrolidin-2-one at 110℃; for 30h;	80%

3-Bromo-4-methylpyridin (3430-22-6) → 3-iodo-4-methyl-pyridine (38749-96-1)

Conditions	Yield
With copper(l) iodide; N,N-dimethylethylenediamine; sodium iodide In 1,4-dioxane at 110℃; for 72h; Inert atmosphere;	95%

tert-Butoxybis(dimethylamino)methane (5815-08-7) + 3-Bromo-4-methylpyridin (3430-22-6) → (E)-2-(3-bromopyridin-4-yl)-N,N-dimethylethen-1-amine

Conditions	Yield
In N,N-dimethyl-formamide at 135℃; for 5h;	95%

3-bromo-1-(trimethylsilyl)-1-propyne (38002-45-8) + 3-Bromo-4-methylpyridin (3430-22-6) → 3-bromo-4-[4-(trimethylsilyl)but-3-yn-1-yl]pyridine (1035428-67-1)

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With lithium diisopropyl amide In tetrahydrofuran; hexane at 50℃; for 0.75h; Stage #2: 3-bromo-1-(trimethylsilyl)-1-propyne In tetrahydrofuran; hexane at 0 - 20℃; Further stages.;	93%

sodium carbonate (497-19-8) + 3-Bromo-4-methylpyridin (3430-22-6) + formic acid ethyl ester (109-94-4) → 4-methylnicotinaldehyde (51227-28-2)

Conditions	Yield
With hydrogenchloride; n-butyllithium In tetrahydrofuran; hexane; water	93%

3-Bromo-4-methylpyridin (3430-22-6) → 3-bromo-4-methyl-1-oxidopyridin-1-ium (17117-15-6)

Conditions	Yield
With dihydrogen peroxide; methyltrioxorhenium(VII) In dichloromethane; water at 20℃;	93%
With 3-chloro-benzenecarboperoxoic acid In dichloromethane at 20℃; for 2h;

3-Bromo-4-methylpyridin (3430-22-6) + formic acid ethyl ester (109-94-4) → 4-methylnicotinaldehyde (51227-28-2)

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With n-butyllithium In tetrahydrofuran; hexane at -100 - 100℃; for 0.166667h; Stage #2: formic acid ethyl ester In tetrahydrofuran; hexane at 100℃; for 0.5h;	93%

allyl bromide (106-95-6) + 3-Bromo-4-methylpyridin (3430-22-6) → 3-bromo-4-(but-3-en-1-yl)pyridine (1309650-03-0)

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With lithium diisopropyl amide In tetrahydrofuran at -78℃; for 0.833333h; Stage #2: allyl bromide In tetrahydrofuran at -78 - 20℃;	92%

phenylacetylene (536-74-3) + 3-Bromo-4-methylpyridin (3430-22-6) → 3-(phenylethynyl)-4-methylpyridine (63731-34-0)

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With bis(η3-allyl-μ-chloropalladium(II)); 1-n-butyl-3-methylimidazolium tetrafluoroborate; triphenylphosphine at 60℃; Heck alkynylation; Inert atmosphere; Stage #2: phenylacetylene With pyrrolidine at 100℃; for 4h; Heck alkynylation; Inert atmosphere;	92%
With tetrabutylammomium bromide; sodium acetate In dimethyl sulfoxide at 120℃; for 50h; Sonogashira Cross-Coupling; Inert atmosphere;	69%

benzofuran-2-boronic acid (98437-24-2) + 3-Bromo-4-methylpyridin (3430-22-6) → 3-(benzofuran-2-yl)-4-methylpyridine (1269386-42-6)

Conditions	Yield
With C43H37ClFeNiP2*C4H8O; potassium carbonate In tetrahydrofuran; acetonitrile at 50℃; for 12h; Suzuki-Miyaura Coupling; Inert atmosphere;	92%

tributyl(1-ethoxyvinyl)stannane (97674-02-7) + 3-Bromo-4-methylpyridin (3430-22-6) → 3-(1-Ethoxy-vinyl)-4-methyl-pyridine (486414-68-0)

Conditions	Yield
tetrakis(triphenylphosphine) palladium(0) In toluene for 4h; Heating / reflux;	91%

benzophenone hydrazone (5350-57-2) + 3-Bromo-4-methylpyridin (3430-22-6) → diphenylmethanone (4-methylpyridin-3-yl)hydrazone (928263-96-1)

Conditions	Yield
With sodium t-butanolate; palladium diacetate; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene In toluene at 85℃;	91%

cobalt(II) chloride hexahydrate + 6-Bromo-1-hexene (2695-47-8) + butane-2,3-dione dioxime (95-45-4) + 3-Bromo-4-methylpyridin (3430-22-6) → (3-bromo-4-methylpyridine)bis(dimethylglyoximato)-5-hexenylcobalt(III)

Conditions	Yield
With sodium hydroxide; sodium tetrahydroborate In methanol stirring CoCl2, glyoxime in CH3OH at -20°C under N2; addn. of 50% aq. NaOH soln., 3-bromo-4-methylpyridine, NaBH4 in CH3OH; stirring at 20°C for 1 h; addn. of bromide at -20, stirring at 20°C in dark for 14 h;; addn. of water containing 1 drop 3-bromo-4-methylpyridine to oily residue; pptn.; drying; elem. anal.;	91%

(9-fluoro-1-methyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)boronic acid (1464115-37-4) + 3-Bromo-4-methylpyridin (3430-22-6) → 9-fluoro-1-methyl-7-(4-methyl-pyridin-3-yl)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline (1404366-47-7)

Conditions	Yield
With tetrabutylammomium bromide; palladium diacetate; sodium carbonate In ethanol; water; toluene Suzuki Coupling; Inert atmosphere; Reflux;	91%

3-Bromo-4-methylpyridin (3430-22-6) → 3-bromoisonicotinic acid (13959-02-9)

Conditions	Yield
Stage #1: 3-Bromo-4-methylpyridin With Co0.27CuO3; water Stage #2: With oxygen at 90℃;	90%
With potassium permanganate In water Heating / reflux;	32%
With hydrogenchloride; potassium permanganate In water

(5-(((tert-butoxycarbonyl)amino)methyl)furan-2-yl)boronic acid (1072946-49-6) + 3-Bromo-4-methylpyridin (3430-22-6) → tert-butyl ((5-(4-methylpyridin-3-yl)furan-2-yl)methyl)carbamate

Conditions	Yield
With trans-bis(triphenylphosphine)palladium dichloride; sodium carbonate In 1,2-dimethoxyethane; ethanol; water at 140℃; for 0.0333333h; Suzuki Coupling; Inert atmosphere; Microwave irradiation;	89.4%
With trans-bis(triphenylphosphine)palladium dichloride; sodium carbonate In 1,2-dimethoxyethane; ethanol; water at 140℃; for 0.0333333h; Microwave irradiation; Inert atmosphere;	89%

Upstream product

• 626-55-1 3-Bromopyridine 
• 4111-54-0 lithium diisopropyl amide 
• 74-88-4 methyl iodide 
• 90731-85-4 3-Bromo-4-methyl-4H-pyridine-1-carboxylic acid phenyl ester 
• 108-89-4 picoline 
• 3430-27-1 3-amino-4-methylpyridine 

Downstream Products

• 229184-01-4 3-bromo-4-[3-hydroxypropyl]pyridine 
• 13959-02-9 3-bromoisonicotinic acid 
• 627905-50-4 11-Ethyl-5,11-dihydro-5-methyl-8-{2-[2-methyl-4-(4-methyl-3-pyridinyl)phenoxy]ethyl}-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one 
• 928263-96-1 diphenylmethanone (4-methylpyridin-3-yl)hydrazone 
• 1086561-62-7 3-(2-[1,3]dioxolan-2-yl-phenyl)-4-methyl-pyridine 
• 1086561-21-8 2-(4-methyl-pyridin-3-yl)-benzaldehyde 
• 1190962-55-0 2-(3-bromopyridin-4-yl)-1-(cyclohex-1-en-1-yl)-ethanone 
• 1210868-03-3 3-(benzylsulfanyl)-4-methylpyridine 
• 1345121-21-2 methyl 4-bromo-5-methyl-8-hydropyrazolo[1,5-a]pyridine-3-carboxylate 
• 1345121-23-4 6-bromo-5-methyl-8-hydropyrazolo[1,5-a]pyridine 
• 1345121-29-0 4-bromo-5-methyl-pyrazolo[1,5-a]pyridine 
• 1345121-27-8 N-[5-(5-methyl-(8-hydropyrazolo[1,5-a]pyridin-6-yl))(2-pyridyl)](2,6-difluorophenyl)carboxamide 
• 1345121-33-6 N-[5-(5-methyl(8-hydropyrazolo[1,5-a]pyridin-4-yl))(2-pyridyl)](2,6-difluorophenyl)carboxamide 
• 1448777-15-8 3-bromo-4-methyl-2-(p-tolyl)pyridine 

Relevant articles and documents

Preparation method of (S)-4- (C)-3-(S)-bromopyridine (bromopyridine) (by machine translation)

The method disclosed by the invention has, the beneficial, effects :(1) that 4 - the reaction conditions are mild, the treatment is easy 4 - the method is easy to, operate, the, treatment, is easy . and the method is, easy to, operate 4 - and easy to ;(2) operate 4 - pH, 4 . (by machine translation)

Method for synthesizing 3-bromoisonicotinic acid intermediate

The invention relates to a method for synthesizing a 3-bromoisonicotinic acid intermediate, and belongs to the technical field of pharmaceutical intermediates. The process comprises the following steps: 4-methylpyridine is adopted as a raw material, and the 4-methylpyridine is reacted with bromine under the catalysis of an aluminum trichloride catalyst to form intermediate 3-bromo-4-methylpyridine; and a novel catalyst Co0.27CuO3 is added, oxygen is introduced for oxidization to form the target product 3-bromoisonicotinic acid. According to the method provided by the invention, in the oxidation reaction process, water is used as a solvent, the novel catalyst Co0.27CuO3 is introduced, the oxygen is used as an oxidant to replace a traditional KMnO4 oxidant, so that pollution of heavy metalsto the environment can be avoided; because the novel catalyst is not affected by the reaction environment, catalytic activity of the novel catalyst is not reduced, and after 25 cycles, activity of thecatalyst is not significantly reduced; and the method has the advantages of greatly improving the yield, reducing the costs, improving the safety, saving the energy, and the like, and conforms to modern chemical industry production requirements of a green reaction.

PROCESS FOR THE PREPARATION OF TOFACITINIB AND INTERMEDIATES THEREOF

The present invention provides compounds of Formula III and Formula VI, and processes for their preparation. The present invention further provides use of the compounds of Formula III and Formula VI for the preparation of tofacitinib or isomers or a mixture of isomers or salts thereof.