36357-38-7

Usage

Uses

Used in Chemical Synthesis:
5-Acetyl-2-methylpyridine is used as a key intermediate in the preparation of pyridine-2,5-dicarboxylic acid, an important chemical compound with various applications in the chemical and pharmaceutical industries. The synthesis process involves the use of potassium permanganate as an oxidant, which facilitates the conversion of 5-acetyl-2-methylpyridine into the desired product.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, 5-acetyl-2-methylpyridine serves as a ligand for Suzuki coupling, a widely used method for the formation of carbon-carbon bonds. This coupling reaction is essential in the synthesis of various complex organic molecules, including those with potential pharmaceutical applications. The use of 5-acetyl-2-methylpyridine as a ligand enhances the efficiency and selectivity of the Suzuki coupling process, leading to the production of desired compounds with improved yields and purity.
Used in Material Science:
The unique chemical properties of 5-acetyl-2-methylpyridine also make it a valuable compound in the field of material science. Its ability to form stable complexes with various metal ions can be exploited in the development of new materials with specific properties, such as catalysts, sensors, or advanced materials for energy storage and conversion.

InChI:InChI=1/C7H6ClNO/c1-5(10)6-2-3-7(8)9-4-6/h2-4H,1H3

Synthetic route

2-methyl-5-pyridylacetylene (1945-85-3) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
With sulfuric acid In toluene at 80℃; for 3h; Inert atmosphere;	92%
With sulfuric acid In toluene at 50℃;	91%
Stage #1: 2-methyl-5-pyridylacetylene With sulfuric acid In toluene at 50℃; Stage #2: With sodium hydrogencarbonate In toluene	91%

Methyl 6-methylnicotinate (5470-70-2) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Stage #1: Methyl 6-methylnicotinate With sodium hydride In ethyl acetate; N,N-dimethyl-formamide; toluene at 80℃; for 10h; Stage #2: With sulfuric acid In water at 110℃; for 2h; Stage #3: With potassium carbonate In water pH=9;	65%
Multi-step reaction with 2 steps 1: NaH / dimethylformamide; toluene / 2.5 h / 80 °C 2: 10percent aq. H2SO4 / 2 h / Heating View Scheme

Methyl 6-methylnicotinate (5470-70-2) + ethyl acetate (141-78-6) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Stage #1: Methyl 6-methylnicotinate; ethyl acetate With sodium hydride In N,N-dimethyl-formamide; toluene at 80℃; for 10h; Stage #2: With sulfuric acid In water at 110℃; for 2h; Stage #3: With potassium carbonate In water pH=9;	65%
Stage #1: Methyl 6-methylnicotinate; ethyl acetate With lithium hexamethyldisilazane In tetrahydrofuran; N,N-dimethyl-formamide at -50 - 20℃; for 1h; Stage #2: With sulfuric acid In tetrahydrofuran; N,N-dimethyl-formamide at 0℃; for 4h; Reflux;

1-amino-1-buten-3-one (2976-86-5) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + 1-(4-methyl-pyridin-3-yl)-ethanone (51227-30-6)

Conditions	Yield
for 15h; heating on water bath;	A 47% B n/a
for 15h; heating on water bath;

5-ethyl-2-methyl-pyridine (104-90-5) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Stage #1: 5-ethyl-2-methyl-pyridine With sulfuric acid; acetic anhydride; acetic acid Stage #2: With chromium(VI) oxide at 10 - 20℃; Stage #3: With sodium carbonate In water	31%
Stage #1: 5-ethyl-2-methyl-pyridine With chromium(VI) oxide; sulfuric acid; acetic anhydride In acetic acid at 20 - 30℃; for 24h; Stage #2: With sodium carbonate In water

2-hydroxy-2-(6-methyl-[3]pyridyl)-propionitrile → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + hydrogen cyanide (74-90-8)

Conditions	Yield
beim Aufbewahren an der Luft;

acetylacetaldehyde dimethyl acetal (5436-21-5) + 1-amino-1-buten-3-one (2976-86-5) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
With ammonium acetate; acetic acid

1-amino-1-buten-3-one (2976-86-5) + (E)-4-chloro-3-buten-2-one (4643-20-3) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

ethyl 3-(2-methyl-5-pyridinyl)-3-oxopropanoate (21683-58-9) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
With sulfuric acid for 2h; Heating; Yield given;
With sulfuric acid; water for 2h; Product distribution / selectivity; Heating / reflux;

methylmagnesium chloride (676-58-4) + N-methoxy-N-methyl-6-methylnicotinamide (221615-71-0) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
In tetrahydrofuran Substitution;

2-methyl-5-<α-oxy-ethyl>-pyridine → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
With chromic acid; acetic acid

3-(1-hydroxyethyl)-6-methylpyridine (56019-64-8, 100189-16-0, 110338-86-8) + acetic acid (64-19-7) + chromic acid → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

sodium salt of oxymethylenacetone → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
With ammonium acetate; diethyl ether; acetic acid
With ammonium acetate; diethyl ether; acetic acid

6-methyl-nicotinoyl chloride (51598-76-6) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Multi-step reaction with 2 steps 1: Et3N / CH2Cl2 2: tetrahydrofuran View Scheme

ethyl 6-methylnicotinate (21684-59-3) + ethyl acetate (141-78-6) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Stage #1: ethyl 6-methylnicotinate; ethyl acetate With sodium hydride In N,N-dimethyl-formamide; toluene at 80℃; for 2.5h; Stage #2: With sulfuric acid; water for 2h; Heating / reflux; Stage #3: With water; potassium carbonate at 0℃; Product distribution / selectivity;

methylmagnesium bromide (75-16-1) + N-methoxy-N-methyl-6-methylnicotinamide (221615-71-0) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
In tetrahydrofuran; hexane at 0 - 20℃; for 16h;

Methyl 6-methylnicotinate (5470-70-2) + N,N-dimethyl-formamide (68-12-2, 33513-42-7) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Stage #1: Methyl 6-methylnicotinate; N,N-dimethyl-formamide With lithium hexamethyldisilazane In tetrahydrofuran; ethyl acetate at -50 - 20℃; for 1h; Stage #2: With sulfuric acid In tetrahydrofuran; ethyl acetate at 0℃; for 4h; Reflux;

(6-methylpyridin-3-yl)trifluoromethanesulfonate (111770-91-3) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Multi-step reaction with 2 steps 1.1: piperidine; Tri(p-tolyl)phosphine / palladium diacetate / toluene; 1-methyl-pyrrolidin-2-one / Inert atmosphere 1.2: 40 °C 1.3: 2 h / Reflux 2.1: sulfuric acid / toluene / 50 °C View Scheme
Multi-step reaction with 2 steps 1.1: piperidine / palladium diacetate; Tri(p-tolyl)phosphine / toluene; 1-methyl-pyrrolidin-2-one / 40 °C / Inert atmosphere 1.2: 2 h / Reflux 2.1: sulfuric acid / toluene / 50 °C View Scheme
Multi-step reaction with 3 steps 1: piperidine; palladium diacetate; Tri(p-tolyl)phosphine / toluene; 1-methyl-pyrrolidin-2-one / 16 h / 40 °C / Inert atmosphere 2: sodium hydroxide / toluene / 2 h / Inert atmosphere; Reflux 3: sulfuric acid / toluene / 3 h / 80 °C / Inert atmosphere View Scheme

5-Hydroxy-2-methylpyridine (1121-78-4) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Multi-step reaction with 3 steps 1.1: pyridine / dichloromethane / 1.5 h / 0 °C 2.1: piperidine; Tri(p-tolyl)phosphine / palladium diacetate / toluene; 1-methyl-pyrrolidin-2-one / Inert atmosphere 2.2: 40 °C 2.3: 2 h / Reflux 3.1: sulfuric acid / toluene / 50 °C View Scheme
Multi-step reaction with 3 steps 1.1: pyridine / dichloromethane / 1.5 h / 0 °C 2.1: piperidine / palladium diacetate; Tri(p-tolyl)phosphine / toluene; 1-methyl-pyrrolidin-2-one / 40 °C / Inert atmosphere 2.2: 2 h / Reflux 3.1: sulfuric acid / toluene / 50 °C View Scheme
Multi-step reaction with 4 steps 1: pyridine / dichloromethane / 1.5 h / 0 °C / Inert atmosphere 2: piperidine; palladium diacetate; Tri(p-tolyl)phosphine / toluene; 1-methyl-pyrrolidin-2-one / 16 h / 40 °C / Inert atmosphere 3: sodium hydroxide / toluene / 2 h / Inert atmosphere; Reflux 4: sulfuric acid / toluene / 3 h / 80 °C / Inert atmosphere View Scheme

2-methyl-4-(6-methylpyridin-3-yl)but-3-yn-2-ol (52535-35-0) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Multi-step reaction with 2 steps 1: sodium hydroxide / toluene / 2 h / Inert atmosphere; Reflux 2: sulfuric acid / toluene / 3 h / 80 °C / Inert atmosphere View Scheme

5-bromo-2-methylpyridine (3430-13-5) + 1-(trimethylsilyl)ethanone (13411-48-8) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
With tetrakis(triphenylphosphine) palladium(0); cesium fluoride In 1,2-dichloro-ethane at 75℃; for 6h; Inert atmosphere; Sealed tube;	73 %Spectr.

6-methylnicotinic acid (3222-47-7) → 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7)

Conditions	Yield
Multi-step reaction with 2 steps 1: O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; triethylamine / N,N-dimethyl-formamide / 12 h / 20 °C 2: tetrahydrofuran; hexane / 16 h / 0 - 20 °C View Scheme

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 2,2,2-trideuterio-1-(6-methylpyridin-3-yl)ethanone

Conditions	Yield
With chloroform-d1; 1,3,4,6,7,8-hexahydro-2H-pyrimido[1,2-a]pyrimidine at 22℃; for 0.5h;	99%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + oxalic acid diethyl ester (95-92-1) → lithium (Z)-1-ethoxy-4-(6-methylpyridin-3-yl)-1,4-dioxobut-2-en-2-olate

Conditions	Yield
Stage #1: 1-(6-methyl-pyridin-3-yl)-ethanone With lithium hexamethyldisilazane In tetrahydrofuran for 1h; Cooling; Stage #2: oxalic acid diethyl ester In tetrahydrofuran at 20℃; for 4h; Cooling;	94%

morpholine (110-91-8) + 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 4-[(6-methyl-pyridin-3-yl)-thioacetyl]-morpholine (19733-95-0)

Conditions	Yield
With sulfur for 17h; Reflux;	93.3%
With sulfur In water; ethyl acetate at 110℃; for 7h;
With sulfur at 110℃; for 7h;

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + ethylene glycol (107-21-1) → 3-(2-methyl-1,3-dioxolan-2-yl)-6-methylpyridine (184766-45-8)

Conditions	Yield
With toluene-4-sulfonic acid In toluene for 8h; Heating;	92%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + 4-bromoohenyl methyl sulfone (3466-32-8) → 1-(6-methyl-3-pyridinyl)-2-[4-(methylsulfonyl)phenyl]ethanone (221615-75-4)

Conditions	Yield
With potassium phosphate; palladium(II) acetylacetonate; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene In 1-methyl-pyrrolidin-2-one at 100℃; for 18h; Product distribution / selectivity; Inert atmosphere;	91%
With tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; sodium t-butanolate In toluene for 5h; Concentration; Inert atmosphere; Reflux;	75%
With tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; sodium t-butanolate In toluene for 4h; Concentration; Inert atmosphere; Reflux;	75%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 3-(1-hydroxyethyl)-6-methylpyridine (56019-64-8, 100189-16-0, 110338-86-8)

Conditions	Yield
With sodium tetrahydroborate In ethanol at 0℃; for 1.5h;	90%
With sodium tetrahydroborate In ethanol for 0.5h;	76%
With water; platinum Hydrogenation;

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + N,N-dimethyl-formamide dimethyl acetal (4637-24-5) → 3-dimethylamino-1-(6-methyl-pyridin-3-yl)-2-propen-1-one

Conditions	Yield
for 18h; Heating / reflux;	90%

morpholine (110-91-8) + 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 6-methyl-3-pyridylthioacetmorpholide hydrochloride

Conditions	Yield
Stage #1: morpholine; 1-(6-methyl-pyridin-3-yl)-ethanone With sulfur for 16h; Reflux; Stage #2: With hydrogenchloride In tetrahydrofuran; water	87.9%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 1-(6-methyl-[3]pyridyl)-ethanone oxime (5470-72-4)

Conditions	Yield
With hydroxylamine hydrochloride; sodium acetate In ethanol at 25℃; for 7h;	85%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → C8H13NO (1613133-67-7)

Conditions	Yield
With diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate; C40H38I2N4(2+)*2CF3O3S(1-) In dichloromethane at 20℃; for 48h; Inert atmosphere;	83%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 6-methylnicotinic acid (3222-47-7)

Conditions	Yield
With nitric acid for 5h; Heating;	75.4%
With nitric acid

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + α-bromoacetophenone (70-11-1) → 5-Acetyl-2-methyl-1-(2-oxo-2-phenyl-ethyl)-pyridinium; bromide (111861-59-7)

Conditions	Yield
In butanone for 15h; Heating;	72%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + 4-bromoohenyl methyl sulfone (3466-32-8) → 1-(6-methylpyridin-3-yl)-2-[(4-methylsulfonyl)-phenyl]-ethanone hydrochloride (1456699-02-7)

Conditions	Yield
Stage #1: 1-(6-methyl-pyridin-3-yl)-ethanone; 4-bromoohenyl methyl sulfone With tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene; sodium t-butanolate In toluene at 60℃; for 3h; Inert atmosphere; Reflux; Stage #2: With hydrogenchloride In water; toluene at 25℃;	70%
Stage #1: 1-(6-methyl-pyridin-3-yl)-ethanone; 4-bromoohenyl methyl sulfone With tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene; sodium t-butanolate In toluene for 3h; Inert atmosphere; Reflux; Stage #2: With hydrogenchloride Reflux;	70%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + 4-bromoohenyl methyl sulfone (3466-32-8) → 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)-phenyl]-ethanone hydrochloride salt

Conditions	Yield
Stage #1: 1-(6-methyl-pyridin-3-yl)-ethanone; 4-bromoohenyl methyl sulfone With tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; sodium t-butanolate In toluene at 60℃; Inert atmosphere; Reflux; Stage #2: With hydrogenchloride In water; toluene Reflux;	70%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + 4-chlorophenyl methyl sulfone (98-57-7) → 1-(6-methyl-3-pyridinyl)-2-[4-(methylsulfonyl)phenyl]ethanone (221615-75-4)

Conditions	Yield
With palladium(II) acetylacetonate; potassium phosphate; 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene In dimethyl sulfoxide at 150℃; for 16h; Inert atmosphere;	69%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + ethyl Pentafluoropropionate (426-65-3) → 4,4,5,5,5-pentafluoro-3-hydroxy-1-(6-methyl-3-pyridyl)pent-2-en-1-one

Conditions	Yield
With lithium hydride In tetrahydrofuran Claisen Condensation;	69%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + cyclohexylhydrazine (6498-34-6) → ethyl 1-cyclohexyl-5-(6-methylpyridin-3-yl)-1H-pyrazole-3-carboxylate

Conditions	Yield
In ethanol at 90℃; for 5h;	62%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + (S)-2-methylpropane-2-sulfinamide (343338-28-3) → (S)-2-methyl-N-[(1R)-1-(6-methylpyridin-3-yl)ethyl]propane-2-sulfinamide

Conditions	Yield
Stage #1: 1-(6-methyl-pyridin-3-yl)-ethanone; (S)-2-methylpropane-2-sulfinamide In tetrahydrofuran at 80℃; for 2h; Stage #2: With L-Selectride In tetrahydrofuran at -78 - -70℃; for 1.5h;	34%

Dimethyl oxalate (553-90-2) + 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 2-hydroxy-4-(6-methylpyridin-3-yl)-4-oxo-but-2-enoic acid methyl ester (1276115-80-0)

Conditions	Yield
Stage #1: Dimethyl oxalate With sodium methylate In methanol for 0.25h; Claisen condensation; Stage #2: 1-(6-methyl-pyridin-3-yl)-ethanone In methanol at 30℃; for 0.0833333h; Claisen condensation; Microwave irradiation;	16%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 1-[6-(bromomethyl)-3-pyridinyl]ethanone

Conditions	Yield
With N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile) In tetrachloromethane at 90℃; for 12h;	16%

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 2-(6-methyl-pyridin-3-yl)-acetamide (19733-98-3)

Conditions	Yield
Stage #1: 1-(6-methyl-pyridin-3-yl)-ethanone With pyridine; ammonia for 0.5h; Stage #2: With sulfur at 160℃; for 17h;	15%

furfural (98-01-1) + 1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) → 3-furan-2-yl-1-(6-methyl-pyridin-3-yl)-propenone (91718-59-1)

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + methyl magnesium iodide (917-64-6) → 2-(6-methylpyridin-3-yl)propan-2-ol (40472-90-0)

Conditions	Yield
With diethyl ether

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + hydrogen cyanide (74-90-8) → 2-hydroxy-2-(6-methyl-[3]pyridyl)-propionitrile

1-(6-methyl-pyridin-3-yl)-ethanone (36357-38-7) + hydrogen cyanide (74-90-8) → 2-hydroxy-2-(6-methyl-[3]pyridyl)-propionic acid

Upstream product

• 5436-21-5 acetylacetaldehyde dimethyl acetal 
• 2976-86-5 1-amino-1-buten-3-one 
• 4643-20-3 (E)-4-chloro-3-buten-2-one 
• 21683-58-9 ethyl 3-(2-methyl-5-pyridinyl)-3-oxopropanoate 
• 676-58-4 methylmagnesium chloride 
• 221615-71-0 N-methoxy-N-methyl-6-methylnicotinamide 
• 56019-64-8 5-(1-hydroxyethyl)-2-methylpyridine 
• 64-19-7 acetic acid 
• 51598-76-6 6-methyl-nicotinoyl chloride 
• 5470-70-2 Methyl 6-methylnicotinate 
• 104-90-5 5-ethyl-2-methyl-pyridine 
• 21684-59-3 ethyl 6-methylnicotinate 
• 141-78-6 ethyl acetate 
• 75-16-1 methylmagnesium bromide 

Downstream Products

• 107456-54-2 1-(6-methyl-[3]pyridyl)-1-phenyl-ethanol 
• 56019-64-8 5-(1-hydroxyethyl)-2-methylpyridine 
• 3222-47-7 6-methylnicotinic acid 
• 100189-17-1 2-(6-methylpyridin-3-yl) ethan-1-ol 
• 19733-96-1 2-(6-methylpyridin-3-yl)acetic acid 
• 111861-59-7 5-Acetyl-2-methyl-1-(2-oxo-2-phenyl-ethyl)-pyridinium; bromide 
• 184766-45-8 3-(2-methyl-1,3-dioxolan-2-yl)-6-methylpyridine 
• 88844-62-6 2-Methyl-5-cinnamoyl-pyridin 
• 63843-17-4 3-(2-Methyl-5-pyridinyl)-2-cyclohexen-1-one 
• 63843-21-0 3-(2-Methyl-5-pyridyl)-2-cyclohexen-1-one oxime 
• 95931-50-3 5-(3-Acetamidophenyl)-2-methylpyridine 
• 40035-78-7 5-(3-Aminophenyl)-2-methylpyridine 
• 91843-27-5 ethyl (6-methylpyridin-3-yl)acetate 
• 56703-83-4 1-(6-methyl-3-pyridinyl)-1,3-butanedione 

Relevant academic research and scientific papers

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SUSTAINED RELEASE COMPOSITION CONTAINING TETRAHYDROPYRIDO Y4, 3-b¨INDOLE DERIVATIVE AND PREPARATION METHOD OF DERIVATIVE

The present invention relates to a sustained-release composition containing 2,3,4,5-tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridyl)ethyl]-1H-pyrido[4,3-b]indole or a pharmaceutically acceptable salt thereof as an active ingredient, preparation thereof and the compound. The composition is suitable for oral administration by one time per day, and achieves the peak plasma concentration at 1.0 to 3 hours after oral administration. The composition is suitable for manufacturing a medicament for treatment of cognitive dysfunction syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, or senile dementia.

SYNTHESIS OF 9-(ARYLALKYL)-1,2,3,4-TETRAHYDRO-Υ-CARBOLINE AND ANALOGUES AND INTERMEDIATES

The present invention pertains generally to methods of preparing certain 9-(arylalkyl)- 1,2,3,4-tetrahydro-Υ-carboline compounds and their analogues, and especially to methods of preparing dimebon. The present invention also pertains to methods of preparing certain intermediate compounds which find use in the synthesis of the 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline compounds.

METHODS AND COMPOSITIONS RELATED TO WRAPPING OF DEHYDRONS

This application describes a novel technology in drug discovery and drug-based imaging/detection: the wrapping technology. This technology is based on identified singularities in the structure of soluble proteins. In contrast with drug-design approaches based on standard structural considerations, the packing of a protein, or more precisely, its dehydron pattern, may be used as a selectivity filter to design small-molecule inhibitors. The wrapping technology described herein is a novel form of rational drug design for avoiding side effects in drug therapy and sharpening the inhibitory impact of drugs on the oncokinome.