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Agomelatine 138112-76-2
Cas No: 138112-76-2
USD $ 1550.0-1550.0 / Kilogram 1 Kilogram 200 Kilogram/Week ShangHai Soyoung Biotechnology Inc Contact Supplier
Agomelatine factory supply
Cas No: 138112-76-2
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Agomelatine Nootropics powder
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Agomelatine 138112-76-2
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USD $ 100.0-600.0 / Gram 10 Gram 500 Metric Ton/Day GZ HONESTCHEM CO., LTD Contact Supplier
Chemical Powder CAS:138112-76-2 Agomelatine
Cas No: 138112-76-2
USD $ 0.02-0.02 / Metric Ton 1 Metric Ton 6000 Kilogram/Day Wuhan Kanal Technology Co., Ltd. Contact Supplier
AGOMELATINE
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Agomelatine
Cas No: 138112-76-2
USD $ 1.0-1.0 / Gram 1 Gram 1 Metric Ton/Month Nanjing chemipioneer pharmaceutical & technology Co., LTD Contact Supplier
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USD $ 3.0-3.0 / Kilogram 1 Kilogram 1-100 Metric Ton/Month Dayang Chem (Hangzhou) Co.,Ltd. Contact Supplier
High purity Agomelatine CAS:138112-76-2
Cas No: 138112-76-2
USD $ 1.0-5.0 / Kilogram 1 Kilogram 99999 Kilogram/Year Hangzhou Dingyan Chem Co., Ltd Contact Supplier
High quality Agomelatine supplier in China
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138112-76-2 Usage

Health risk

October 30, 2012, the British Medicines and Healthcare Products Agency (MHRA) released agomelatine (agomelatine, Valdoxan/Thymanax) security information. MHRA found that several cases appears serious reports of liver toxicity with agomelatine, including six cases of liver failure patients within worldwide report. Agomelatine's drug information already includes in the recommendations that all patients need liver function tests at the start of treatment and during treatment. Now liver function tests should also be recommended when the drug dose is increased. MHRA recommends that if the patients have potential liver damage symptoms or signs, or that the increases of serum transaminase beyond the upper limit of normal (ULN) three times is found in the function tests, it should be immediately suspended.

Patent cases

The earliest agomelatine compound patent is French Patent FR902393, which is applied in February 27, 1990. This patent has the same patent family in Europe, USA, Canada, Japan and Australia. But there is no Chinese patent. The above patents were all authorized after January 1, 1993. Therefore China is also ineligible for administrative protection. Agomelatine has both technology patent and polymorph patent in China. But it also can be avoided.

Antidepressants

Agomelatine, which is developed by the French Servier company, is the world's first melatonin receptors MT1 and MT2 agonist class of antidepressants. It applies to the treatment of adult patients with severe depressive. We know that melatonin is an endogenous neural hormones. It is only produced by the pineal gland anterior pituitary at night, and acts on the melatonin receptor that focuses on the presence of hypothalamic suprachiasmatic nucleus (SCN). It is involved in mediating the circadian rhythms in mammals. It is the well-known time guardian in the body, which can regulate the biological clock that is modulated by external circadian cycle. However, since that melatonin has high catabolism rate in vivo which mikes its half-life shorter and the selectivity of its receptor located in the SCN poorer, the treatment of circadian rhythms disorders is limited. Therefore, in order to overcome these drawbacks of melatonin, the researchers designed a series of melatonin analogues. Molecular modeling studies have shown that indole ring of melatonin is the structure sites of catabolic inactivation. Indole ring is an ideal site of isosteric modifications. Agomelatine developed by Servier company is melatonin’s naphthalene biological (electronic) isostere analogs. Indole ring is substituted by naphthalene nucleus, which leads it have more metabolic stability than melatonin.

Pharmacological effects

The listing of agomelatine is a new breakthrough in the field of the treatment of depression. It is melatonin MT1/MT2 receptor agonist and serotonin 2c (5-HT2C) receptor antagonist. It can make depressed patients’ biological rhythm disorders return to normal through the synergy between the two and then result in antidepressant efficacy. Its unique mechanism of action has opened up an innovative way to treat depression. Agomelatine’s mechanism of drug action is completely different with antidepressants that are commonly used today, such as selective serotonin reuptake inhibitors (SSRI) and serotonin-norepinephrine reuptake inhibitors (SNRI). SSRI and SNRI antidepressants achieve antidepressant efficacy by increasing concentration of serotonin. But it also brings a lot of side effects, such as weight changes, sexual dysfunction, withdrawal syndrome and the like. The molecular structure of agomelatine directly combines with serotonin 2c (5HT2c) receptor of post-synaptic membrane so as to exert its antidepressant efficacy without increasing serotonin concentration in the synaptic cleft. This unique mechanism of action makes agomelatine quickly and effectively exert its antidepressant efficacy at the same time, and avoid the occurrence of adverse drug reactions to an extreme. Another unique targets of agomelatine is in melatonin receptors. MT1 and MT2 receptors densely distribute in the human suprachiasmatic nucleus. The nucleus mainly control human sleep rhythm. Agomelatine can well improve the quality of patients’ sleep by agonism on MT1 MT2 receptors, and improve patients’ wakefulness during the day. The quality of sleep has both cause and effect relationship with depression outcomes state. It is reported that 80% of patients with depression have the problems of sleep disorders at different levels. The improvement of sleep quality can directly contribute to the improvement of the overall clinical condition of patients with depression. The above information is edited by the Chemicalbook of Ge Qian.

Chemical Properties

White Solid

Uses

Agomelatine is an antidepressant drug. It is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. Activation of 5-HT2C receptors by serotonin inhibits dopamine and norepinephrine release. Antagonism of

Uses

Melatonin drugs.

Uses

Agomelatine is a melatoninergic agonist and selective antagonist of 5-HT2C receptors, and has been shown to be active in several animal models of depression. Agomelatine (S20098) displayed pKi values of 6.4 and 6.2 at native (porcine) and cloned, human (h)5-hydroxytryptamine (5-HT)2C receptors, respectively.
InChI:InChI=1/C11H14N4O2.CH4O3S/c1-5-2-9(16)7-3-8(14-15-11(12)13)10(17)4-6(5)7;1-5(2,3)4/h3-5,9,16H,2H2,1H3,(H4,12,13,15);1H3,(H,2,3,4)/b14-8-;

138112-76-2 Well-known Company Product Price

Brand (Code)Product description CAS number Packaging Price Detail
TCI America (A2606)  Agomelatine  >98.0%(HPLC)(N) 138112-76-2 1g 1,390.00CNY Detail
Sigma (A1362)  Agomelatine  ≥98% (HPLC) 138112-76-2 A1362-5MG 700.83CNY Detail
Sigma (A1362)  Agomelatine  ≥98% (HPLC) 138112-76-2 A1362-25MG 2,819.70CNY Detail

138112-76-2SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 10, 2017

Revision Date: Aug 10, 2017

1.Identification

1.1 GHS Product identifier

Product name Agomelatine

1.2 Other means of identification

Product number -
Other names N-[2-(7-Methoxy-1-naphthalenyl)ethyl]-acetamide S-20098

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:138112-76-2 SDS

138112-76-2Synthetic route

2-(7-methoxynaphthalen-1-yl)ethanamine hydrochloride
139525-77-2

2-(7-methoxynaphthalen-1-yl)ethanamine hydrochloride

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With sodium acetate In ethanol for 1h; Reflux;99.5%
With sodium acetate In Isopropyl acetate99%
With sodium acetate In ethanol for 1h; Reflux;95%
2-(2-methoxynaphthalen-8-yl)acetaldehyde oxime
1331869-01-2

2-(2-methoxynaphthalen-8-yl)acetaldehyde oxime

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With hydrogen; acetic anhydride In tetrahydrofuran at 50℃; under 7500.75 Torr; for 6h; Autoclave; Inert atmosphere;98%
N,N-dibenzyl-2-(7-methoxynaphthalen-1-yl)ethanamine

N,N-dibenzyl-2-(7-methoxynaphthalen-1-yl)ethanamine

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
Stage #1: N,N-dibenzyl-2-(7-methoxynaphthalen-1-yl)ethanamine With 20% palladium hydroxide-activated charcoal; hydrogen In ethanol; water; ethyl acetate under 3750.38 Torr; for 30h; Autoclave;
Stage #2: acetic anhydride With sodium acetate for 4h;
98%
2-(7-methoxynaphth-1-yl)ethylamine
138113-09-4

2-(7-methoxynaphth-1-yl)ethylamine

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
In tetrahydrofuran at 0 - 20℃; for 6h; Concentration; Temperature;97.5%
With sodium acetate In ethanol at 65℃; Green chemistry;92%
With triethylamine In toluene at 20 - 30℃;90%
2-(7-methoxynaphth-1-yl)ethylamine
138113-09-4

2-(7-methoxynaphth-1-yl)ethylamine

acetyl chloride
75-36-5

acetyl chloride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With triethylamine In dichloromethane at 0 - 5℃;95%
In pyridine92%
With pyridine for 0.5h; Product distribution / selectivity; Cooling with ice;92%
dimethyl sulfate
77-78-1

dimethyl sulfate

N-[2-(7-Hydroxy-1-naphthyl)ethyl]-acetamide
152302-45-9

N-[2-(7-Hydroxy-1-naphthyl)ethyl]-acetamide

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With potassium carbonate In acetone for 5h; Reflux;94.5%
1-(2-nitroethyl)-7-methoxynaphthalene
1424944-40-0

1-(2-nitroethyl)-7-methoxynaphthalene

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With 5%-palladium/activated carbon; hydrogen In water; ethyl acetate at 20℃;92%
1-[2-(7-methoxynahthalen-1-yl)-ethyl]-2λ5-triaz-1-en-2-yne
1384536-35-9

1-[2-(7-methoxynahthalen-1-yl)-ethyl]-2λ5-triaz-1-en-2-yne

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With palladium 10% on activated carbon; hydrogen In water; ethyl acetate at 20℃;92%
N-[2-(7-methoxy-3,4-dihydro-naphthalen-1-yl)ethyl]acetamide
1352139-51-5

N-[2-(7-methoxy-3,4-dihydro-naphthalen-1-yl)ethyl]acetamide

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With 2,3-dicyano-5,6-dichloro-p-benzoquinone In dichloromethane at 20℃;91.8%
With 2,3-dicyano-5,6-dichloro-p-benzoquinone for 4h; Product distribution / selectivity; Reflux;90%
With 2,3-dicyano-5,6-dichloro-p-benzoquinone In tetrahydrofuran at 20℃; Product distribution / selectivity;80%
2-(7-methoxynaphthalen-1-yl)ethanamine hydrochloride
139525-77-2

2-(7-methoxynaphthalen-1-yl)ethanamine hydrochloride

acetyl chloride
75-36-5

acetyl chloride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With potassium carbonate In dichloromethane; water at 0 - 20℃; for 2h;91%
Stage #1: 2-(7-methoxynaphthalen-1-yl)ethanamine hydrochloride With triethylamine In dichloromethane at 25 - 35℃; for 0.5h;
Stage #2: acetyl chloride In dichloromethane at 10 - 20℃; for 1h;
90%
With potassium carbonate In chloroform; water for 0.5h; Ambient temperature;89%
With potassium carbonate In chloroform; water at 0℃;
Stage #1: 2-(7-methoxynaphthalen-1-yl)ethanamine hydrochloride With potassium carbonate In water; ethyl acetate at 20℃; Schotten-Baumann reaction;
Stage #2: acetyl chloride In water; ethyl acetate at 0 - 20℃; for 1h; Schotten-Baumann reaction;
2-(7-methoxynaphthalen-1-yl)ethanamine carbon dioxide adduct

2-(7-methoxynaphthalen-1-yl)ethanamine carbon dioxide adduct

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With sodium acetate In methanol Reflux;91%
With sodium acetate In methanol Reflux;91%
With sodium acetate In methanol Reflux;91%
acetic anhydride
108-24-7

acetic anhydride

(7-methoxy-1-naphthyl)acetonitrile
138113-08-3

(7-methoxy-1-naphthyl)acetonitrile

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With hydrogen; Raney nickel In ethanol; water at 70℃; under 22502.3 Torr;89%
With hydrogen In ethanol; water at 70℃; under 22502.3 Torr;89%
With hydrogen In ethanol; water at 70℃; under 22502.3 Torr; for 1h;89%
With hydrogen In ethanol at 60℃; under 37503.8 Torr; for 4h;
Stage #1: (7-methoxy-1-naphthyl)acetonitrile With hydrogen; sodium hydroxide In methanol; water at 30℃; under 3000.3 Torr;
Stage #2: acetic anhydride In methanol at 15 - 25℃;
2-(7-methoxynaphthalen-1-yl)ethen-1-amine

2-(7-methoxynaphthalen-1-yl)ethen-1-amine

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With sodium acetate In ethanol; acetic anhydride at 25℃; for 1h; Temperature;88.1%
1-[2-(acetylamino)ethyl]-7-methoxynaphthalen-2-yl propane-1-sulphonate

1-[2-(acetylamino)ethyl]-7-methoxynaphthalen-2-yl propane-1-sulphonate

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With palladium 10% on activated carbon; ammonium acetate; magnesium In ethanol for 16h;87%
N-[2-(1-hydroxyl-7-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)ethyl]-acetamide
1352139-49-1

N-[2-(1-hydroxyl-7-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)ethyl]-acetamide

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With acetic acid; 2,3-dicyano-5,6-dichloro-p-benzoquinone In toluene at 40℃; for 5h;85%
With acetic acid; 2,3-dicyano-5,6-dichloro-p-benzoquinone In toluene at 40℃; for 5h;
Multi-step reaction with 2 steps
1: hydrogenchloride / ethyl acetate; water / 2 h / 20 °C
2: 2,3-dicyano-5,6-dichloro-p-benzoquinone / dichloromethane / 20 °C
View Scheme
2-(2-(7-methoxynaphthalen-1-yl)ethyl) isoindoline-1,3-dione
1206788-15-9

2-(2-(7-methoxynaphthalen-1-yl)ethyl) isoindoline-1,3-dione

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
Stage #1: 2-(2-(7-methoxynaphthalen-1-yl)ethyl) isoindoline-1,3-dione With hydrazine hydrate In methanol; dichloromethane at 30℃; for 14h;
Stage #2: acetic anhydride With triethylamine In methanol; dichloromethane; toluene at 25℃; for 0.333333h;
85%
1-[2-(acetylamino)ethyl]-7-methoxynaphthalen-2-yl-4-methylbenzenesulphonate

1-[2-(acetylamino)ethyl]-7-methoxynaphthalen-2-yl-4-methylbenzenesulphonate

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With methanol; sodium tetrahydroborate; nickel dichloride at 20℃; for 0.5h; Sealed tube; Inert atmosphere;80%
2-(2-methoxynaphthalen-8-yl)acetamide
138113-07-2

2-(2-methoxynaphthalen-8-yl)acetamide

acetic acid
64-19-7

acetic acid

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With sodium tetrahydroborate In 1,4-dioxane at 95 - 98℃; for 22h;76.3%
acetic anhydride
108-24-7

acetic anhydride

2-(7-methoxynaphthalen-1-yl)ethyl methanesulphonate
185336-04-3

2-(7-methoxynaphthalen-1-yl)ethyl methanesulphonate

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
Stage #1: 2-(7-methoxynaphthalen-1-yl)ethyl methanesulphonate With ammonia In water; acetonitrile at 110℃; for 3h;
Stage #2: acetic anhydride With sodium acetate for 1h;
74%
N-[2-(4-chloro-7-methoxy-1,2-dihydro-1-naphthyl)ethyl]acetamide
1384261-25-9

N-[2-(4-chloro-7-methoxy-1,2-dihydro-1-naphthyl)ethyl]acetamide

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With potassium tert-butylate In tert-butyl alcohol for 3h; Reflux;68%
N-[2-(4-bromo-7-methoxy-1,2-dihydro-1-naphthyl)ethyl]acetamide
1384261-27-1

N-[2-(4-bromo-7-methoxy-1,2-dihydro-1-naphthyl)ethyl]acetamide

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With potassium tert-butylate In tert-butyl alcohol for 3h; Reflux;68%
(E)-7-methoxy-1-(2-nitrovinyl)naphthalene
1415243-95-6

(E)-7-methoxy-1-(2-nitrovinyl)naphthalene

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With palladium 10% on activated carbon; acetic acid65%
2-(7-methoxynaphth-1-yl)ethylamine
138113-09-4

2-(7-methoxynaphth-1-yl)ethylamine

sodium acetate
127-09-3

sodium acetate

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With acetic anhydride In ethanol at 20℃; for 1h;61%
N-[2-(7-methoxy-1,2-dihydro-1-naphthyl)ethyl]acetamide
1384261-23-7

N-[2-(7-methoxy-1,2-dihydro-1-naphthyl)ethyl]acetamide

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With 2,3-dicyano-5,6-dichloro-p-benzoquinone In dichloromethane for 48h;48%
1-[2-(2,5-dioxopyrrolidin-1-yl)ethyl]-7-methoxynaphthalen-2-yl propane-1-sulphonate

1-[2-(2,5-dioxopyrrolidin-1-yl)ethyl]-7-methoxynaphthalen-2-yl propane-1-sulphonate

acetic anhydride
108-24-7

acetic anhydride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
Stage #1: 1-[2-(2,5-dioxopyrrolidin-1-yl)ethyl]-7-methoxynaphthalen-2-yl propane-1-sulphonate With palladium 10% on activated carbon; ammonium acetate; magnesium In methanol at 30℃; for 12h;
Stage #2: acetic anhydride With sodium acetate; sodium hydroxide In ethanol; water for 1h; Sealed tube;
37%
2-(7-methoxynaphth-1-yl)ethylamine
138113-09-4

2-(7-methoxynaphth-1-yl)ethylamine

[14C]acetyl-CoA

[14C]acetyl-CoA

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
With sheep pineal supernatant (serotonin-N-acetyl transferase); Pargyline In phosphate buffer at 37℃; for 0.166667h; pH=6.8; Enzyme kinetics;
2-(7-methoxynaphthalen-1-yl)acetic acid
6836-22-2

2-(7-methoxynaphthalen-1-yl)acetic acid

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: thionyl chloride / CHCl3
2: aq. NH4OH / diethyl ether / 0 °C
3: AlH4 / diethyl ether
4: K2CO3 / H2O; CHCl3 / 0 °C
View Scheme
Multi-step reaction with 5 steps
1: thionyl chloride / CHCl3
2: aq. NH4OH / diethyl ether / 0 °C
3: (CF3CO)2O / tetrahydrofuran / 0 °C
4: H2, HCl / Ni Raney / diethyl ether
5: K2CO3 / H2O; CHCl3 / 0 °C
View Scheme
Multi-step reaction with 5 steps
1.1: thionyl chloride / dichloromethane / 2 h / Reflux
2.1: ammonia / ethyl acetate; water / Cooling with ice
3.1: triethylamine; trifluoroacetic anhydride / tetrahydrofuran / 20 °C / Cooling with ice
4.1: hydrogen; ammonia / ethanol; water / 12 h / 60 °C / 228015 Torr / Autoclave
5.1: pyridine / 40 °C
5.2: 20 °C / Cooling with ice
View Scheme
2-(2-methoxynaphthalen-8-yl)acetamide
138113-07-2

2-(2-methoxynaphthalen-8-yl)acetamide

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: AlH4 / diethyl ether
2: K2CO3 / H2O; CHCl3 / 0 °C
View Scheme
Multi-step reaction with 3 steps
1: (CF3CO)2O / tetrahydrofuran / 0 °C
2: H2, HCl / Ni Raney / diethyl ether
3: K2CO3 / H2O; CHCl3 / 0 °C
View Scheme
Multi-step reaction with 3 steps
1.1: triethylamine; trifluoroacetic anhydride / tetrahydrofuran / 20 °C / Cooling with ice
2.1: hydrogen; ammonia / ethanol; water / 12 h / 60 °C / 228015 Torr / Autoclave
3.1: pyridine / 40 °C
3.2: 20 °C / Cooling with ice
View Scheme
Multi-step reaction with 3 steps
1.1: trichlorophosphate / dichloromethane; N,N-dimethyl-formamide / 2 h / 85 °C
2.1: sodium hydroxide; hydrogen / water; methanol; isopropyl alcohol / 25 - 30 °C / 7500.75 Torr
2.2: 1 h / 50 - 55 °C
3.1: sodium hydroxide / water; toluene / 0.25 h / 20 - 25 °C
3.2: 35 - 40 °C
View Scheme
(7-methoxy-1-naphthyl)acetonitrile
138113-08-3

(7-methoxy-1-naphthyl)acetonitrile

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: H2, HCl / Ni Raney / diethyl ether
2: K2CO3 / H2O; CHCl3 / 0 °C
View Scheme
Multi-step reaction with 2 steps
1.1: hydrogen; ammonia / ethanol; water / 12 h / 60 °C / 228015 Torr / Autoclave
2.1: pyridine / 40 °C
2.2: 20 °C / Cooling with ice
View Scheme
Multi-step reaction with 2 steps
1.1: sodium hydroxide; hydrogen / water; methanol; isopropyl alcohol / 25 - 30 °C / 7500.75 Torr
1.2: 1 h / 50 - 55 °C
2.1: sodium hydroxide / water; toluene / 0.25 h / 20 - 25 °C
2.2: 35 - 40 °C
View Scheme
Multi-step reaction with 2 steps
1.1: ammonia; hydrogen / methanol / 15 - 55 °C / 3750.38 Torr / Autoclave
1.2: 1 h / 0 - 5 °C
2.1: triethylamine / dichloromethane / 0.5 h / 25 - 35 °C
2.2: 1 h / 10 - 20 °C
View Scheme
Multi-step reaction with 2 steps
1: ammonia; hydrogen / ethanol / 24 h / 30 - 40 °C / 2250.23 - 3000.3 Torr / Autoclave
2: triethylamine / toluene / 0.5 h / 0 - 30 °C
View Scheme
(7-methoxy-1-naphthyl)acetic acid chloride
6836-23-3

(7-methoxy-1-naphthyl)acetic acid chloride

agomelatine
138112-76-2

agomelatine

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: aq. NH4OH / diethyl ether / 0 °C
2: AlH4 / diethyl ether
3: K2CO3 / H2O; CHCl3 / 0 °C
View Scheme
Multi-step reaction with 4 steps
1: aq. NH4OH / diethyl ether / 0 °C
2: (CF3CO)2O / tetrahydrofuran / 0 °C
3: H2, HCl / Ni Raney / diethyl ether
4: K2CO3 / H2O; CHCl3 / 0 °C
View Scheme
Multi-step reaction with 4 steps
1.1: ammonia / ethyl acetate; water / Cooling with ice
2.1: triethylamine; trifluoroacetic anhydride / tetrahydrofuran / 20 °C / Cooling with ice
3.1: hydrogen; ammonia / ethanol; water / 12 h / 60 °C / 228015 Torr / Autoclave
4.1: pyridine / 40 °C
4.2: 20 °C / Cooling with ice
View Scheme
Multi-step reaction with 4 steps
1.1: ammonia / toluene / 0 - 5 °C / pH 10 - 11
2.1: trichlorophosphate / dichloromethane; N,N-dimethyl-formamide / 2 h / 85 °C
3.1: sodium hydroxide; hydrogen / water; methanol; isopropyl alcohol / 25 - 30 °C / 7500.75 Torr
3.2: 1 h / 50 - 55 °C
4.1: sodium hydroxide / water; toluene / 0.25 h / 20 - 25 °C
4.2: 35 - 40 °C
View Scheme
agomelatine
138112-76-2

agomelatine

maleic acid
110-16-7

maleic acid

agomelatine maleic acid
1403960-82-6

agomelatine maleic acid

Conditions
ConditionsYield
In ethanol for 0.75h;100%
In methanol; ethyl acetate at 20℃; for 168h; Product distribution / selectivity;
for 1h;
agomelatine
138112-76-2

agomelatine

citric acid
77-92-9

citric acid

agomelatine citric acid
1403960-81-5

agomelatine citric acid

Conditions
ConditionsYield
In acetone at 20℃;100%
In methanol; ethyl acetate at 2 - 5℃; Product distribution / selectivity; Reflux;
In methanol at 20℃; for 20h; Product distribution / selectivity;
2,5-dihydroxybenzoic acid.
490-79-9

2,5-dihydroxybenzoic acid.

agomelatine
138112-76-2

agomelatine

agomelatine gentisic acid
1419379-42-2

agomelatine gentisic acid

Conditions
ConditionsYield
In toluene for 0.75h;100%
ethylene glycol
107-21-1

ethylene glycol

agomelatine
138112-76-2

agomelatine

C2H6O2*C15H17NO2
1259393-47-9

C2H6O2*C15H17NO2

Conditions
ConditionsYield
at 110 - 130℃; for 5h;98%
isonicotinamide
1453-82-3

isonicotinamide

agomelatine
138112-76-2

agomelatine

agomelatine isonicotinamide adduct
1366181-84-1

agomelatine isonicotinamide adduct

Conditions
ConditionsYield
at 135℃; Neat (no solvent);98%
methyl 4-hydroxylbenzoate
99-76-3

methyl 4-hydroxylbenzoate

agomelatine
138112-76-2

agomelatine

agomelatine methyl 4-hydroxybenzoate adduct
1366181-85-2

agomelatine methyl 4-hydroxybenzoate adduct

Conditions
ConditionsYield
at 110℃; Neat (no solvent);98%
agomelatine
138112-76-2

agomelatine

N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide hydrogen sulfate

N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide hydrogen sulfate

Conditions
ConditionsYield
With sulfuric acid In acetone at 10 - 20℃; Solvent; Temperature;96.9%
With sulfuric acid In acetone at 10 - 20℃; Solvent; Temperature;13.6 g
With sulfuric acid In ethyl acetate at 20℃;
acetic acid
64-19-7

acetic acid

agomelatine
138112-76-2

agomelatine

agomelatine 1:1 cocrystal with acetic acid
1259393-46-8

agomelatine 1:1 cocrystal with acetic acid

Conditions
ConditionsYield
In diethyl ether for 48h;96%
at 20 - 45℃; for 480h; Sealed tube;
agomelatine
138112-76-2

agomelatine

urea
57-13-6

urea

agomelatine urea adduct
1366181-82-9

agomelatine urea adduct

Conditions
ConditionsYield
at 120℃; for 0.333333h; Neat (no solvent);96%
In ethanol at 20℃; for 2h; Time;70%
In isopropyl alcohol at 20℃; for 20h;41%
agomelatine
138112-76-2

agomelatine

benzenesulfonic acid
98-11-3

benzenesulfonic acid

N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide benzenesulfonic acid
1402317-73-0

N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide benzenesulfonic acid

Conditions
ConditionsYield
In acetone at 25℃; Solvent; Temperature;95.8%
In methanol; ethyl acetate at 2 - 20℃; Product distribution / selectivity;
In dichloromethane at 10 - 20℃; Solvent; Temperature;15.6 g
In methanol; ethyl acetate Heating;
toluene-4-sulfonic acid
104-15-4

toluene-4-sulfonic acid

agomelatine
138112-76-2

agomelatine

agomelatine p-toluenesulfonic acid monohydrate

agomelatine p-toluenesulfonic acid monohydrate

Conditions
ConditionsYield
In tetrahydrofuran; hexane for 0.5h; Solvent; Temperature; Reflux;95.8%
agomelatine
138112-76-2

agomelatine

N-[2-(7-Hydroxy-1-naphthyl)ethyl]-acetamide
152302-45-9

N-[2-(7-Hydroxy-1-naphthyl)ethyl]-acetamide

Conditions
ConditionsYield
With boron tribromide In dichloromethane at -10 - 20℃; for 2h;93.3%
Stage #1: agomelatine With boron tribromide In dichloromethane at 0℃; for 2h;
Stage #2: With water In dichloromethane at 0℃;
80%
With hydrogenchloride In water at 80℃;74.8%
glycolic Acid
79-14-1

glycolic Acid

agomelatine
138112-76-2

agomelatine

agomelatine glycolic acid adduct
1366181-83-0

agomelatine glycolic acid adduct

Conditions
ConditionsYield
In acetonitrile for 2h; Reflux;93%
for 0.25h;
agomelatine
138112-76-2

agomelatine

N [2-(7-methoxynaphthalen-1-yl)ethyl]acetamide hydrochloride
1176316-99-6

N [2-(7-methoxynaphthalen-1-yl)ethyl]acetamide hydrochloride

Conditions
ConditionsYield
With hydrogenchloride In water; ethyl acetate at 10℃; Product distribution / selectivity;88.7%
With hydrogenchloride In water; ethyl acetate at 10℃; for 1h;88.7%
With hydrogenchloride In water; ethyl acetate at 10℃; for 1h;88.7%
toluene-4-sulfonic acid
104-15-4

toluene-4-sulfonic acid

agomelatine
138112-76-2

agomelatine

agomelatine p-toluenesulfonic acid

agomelatine p-toluenesulfonic acid

Conditions
ConditionsYield
In acetone at 0 - 10℃;88.2%
In acetone at 0 - 10℃;1.5 g
agomelatine
138112-76-2

agomelatine

N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide hydrobromide
1176317-02-4

N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide hydrobromide

Conditions
ConditionsYield
With hydrogen bromide In water; ethyl acetate at 20℃; for 1h; Product distribution / selectivity;85.3%
With hydrogen bromide In water; ethyl acetate at 20℃; for 1h; Temperature;85.3%
With hydrogen bromide In water; ethyl acetate for 1h;85.3%

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AGOMELATINE (cas 138112-76-2) treatment corrects symptoms of depression and anxiety by restoring the disrupted melatonin circadian rhythms of rats exposed to chronic constant light08/25/2019

Desynchronization of circadian rhythms is a hallmark of depression. The antidepressant agomelatine, which is an MT1/MT2 melatonin receptor agonist/5-HT2C serotonin receptor antagonist has advantages compared to the selective serotonin reuptake inhibitors as a circadian phase-shifting agent. The ...detailed

Mucoadhesive olaminosomes: A novel prolonged release nanocarrier of AGOMELATINE (cas 138112-76-2) for the treatment of ocular hypertension08/24/2019

Mucoadhesive olaminosomes are novel nanocarriers designed to control agomelatine release and enhance its bioavailability. Olaminosomes were prepared using oleic acid, oleylamine and sorbitan monooleate adopting thin film hydration technique. Chitosan HCl was added to impart the mucoadhesive prop...detailed

Behavioural pharmacologyStudies on the reproductive effects of chronic treatment with AGOMELATINE (cas 138112-76-2) in the rat08/23/2019

Agomelatine is an antidepressant with a novel mechanism of action. It is a melatonergic agonist for MT1 and MT2 receptors and a serotonin (5-HT2C) receptor antagonist. Agomelatine has been suggested not to have adverse effects on sexual functions. However, the effects of chronic agomelatine admi...detailed

Research paperEffect of AGOMELATINE (cas 138112-76-2) 25–50 mg on functional outcomes in patients with major depressive disorder08/22/2019

PurposeThe purpose of this work is to investigate the effect of agomelatine on functioning compared with placebo in patients suffering from Major Depressive Disorder (MDD).detailed

Spike–Wave Discharges and Sleep–Wake States during Circadian Desynchronization: No Effects of AGOMELATINE (cas 138112-76-2) upon Re-Entrainment08/21/2019

Rapid changes in the light–dark cycle cause circadian desynchronization between rhythms of spike–wave discharges (SWDs) and motor activity in genetic epileptic rats, and this is accompanied by an increase in epileptic activity. Given the close relationship between absence seizures and sleep–w...detailed

Effects of AGOMELATINE (cas 138112-76-2) on electrocorticogram activity on penicillin-induced seizure model of rats08/18/2019

Agomelatine is a new antidepressant drug acting as an antagonist of 5-hydroxytryptamine receptor 2C (5-HTR2C) and agonist of melatonergic receptors 1 and 2 (MT1 and MT2). Because of this dual action, it is an atypical antidepressant. The aim of this study was to investigate chronic anticonvulsan...detailed

Selective crystallization of AGOMELATINE (cas 138112-76-2) from molten state induced by polymer08/17/2019

In this study, agomelatine Form I was selectively recrystallized from molten state induced by ethyl cellulose (EC). It was found EC could effectively inhibit the transformation process of Form I to Form II. The effect of EC on the recrystallization of agomelatine from molten state was studied in...detailed

Research articleEffects of AGOMELATINE (cas 138112-76-2) in rotenone-induced Parkinson’s disease in rats08/16/2019

The effects of melatonin and melatonin analogs in experimental Parkinson’s disease (PD) models remain controversial. Agomelatine, a novel analog of melatonin, is both agonists for melatonin-1 and melatonin-2 receptors and antagonist of 5-HT2C receptors. While agomelatine has been commonly used ...detailed

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