Duloxetine

Product Name: Duloxetine
CAS No.: 116539-59-4
Chemical Name: Duloxetine
Synonyms: DULOXETIN;DULOXETINE HCI;DULOXETINE-D3;(S)-DULOXETINE;(3S)-N-methyl-3-naphthalen-1-yloxy-3-thiophen-2-yl-propan-1-amine;CS-559;DULOXETINE;(+)-Duloxetine;Duloxetine Hcl(S);Duloxetine, >=99%
CBNumber: CB8670379
Molecular Formula: C18H19NOS
Formula Weight: 297.41
MOL File: 116539-59-4.mol

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Duloxetine Property

Boiling point:: 466.2±40.0 °C(Predicted)
Density: 1.158±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: Soluble in DMSO
pka: 10.02±0.10(Predicted)
BCS Class: 2
InChI: InChI=1/C18H19NOS.ClH/c1-19-12-11-17(18-10-5-13-21-18)20-16-9-4-7-14-6-2-3-8-15(14)16;/h2-10,13,17,19H,11-12H2,1H3;1H/t17-;/s3
InChIKey: BFFSMCNJSOPUAY-VOPAOICTNA-N
SMILES: C1(=CC=CS1)[C@H](CCNC)OC1=CC=CC2=CC=CC=C12.Cl |&1:5,r|
EPA Substance Registry System: 2-Thiophenepropanamine, N-methyl-?-(1-naphthalenyloxy)-, (?S)- (116539-59-4)

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Safety

Hazardous Substances Data: 116539-59-4(Hazardous Substances Data)

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Matrix Scientific

Product number: 094812
Product name: (S)-N-Methyl-3-(naphthalen-1-yloxy)-3-(thiophen-2-yl)propan-1-amine
Purity: 95+%
Packaging: 1g
Price: $135
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb146144
Product name: Duloxetine
Purity: >98%
Packaging: 100mg
Price: $414.8
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: RDL0017905
Product name: DULOXETINE-D3
Purity: 95.00%
Packaging: 5MG
Price: $504.27
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb146144
Product name: Duloxetine
Purity: >98%
Packaging: 250mg
Price: $615.4
Updated: 2021/12/16

Matrix Scientific

Product number: 094812
Product name: (S)-N-Methyl-3-(naphthalen-1-yloxy)-3-(thiophen-2-yl)propan-1-amine
Purity: 95+%
Packaging: 5g
Price: $360
Updated: 2021/12/16

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Duloxetine Chemical Properties,Usage,Production

Uses

Antidepressant.

Definition

ChEBI: (S)-duloxetine is a duloxetine. It is an enantiomer of a (R)-duloxetine.

brand name

Cymbalta (Lilly).

General Description

Duloxetine (Cymbalta) is a newer antidepressant. It islargely like venlafaxine, which is an SNERI (selective norepinephrinereuptake inhibitor).

Pharmacokinetics

Duloxetine appears to be fairly well absorbed after oral doses, with peak plasma levels in 6 to 10 hours and linear pharmacokinetics. The drug is extensively metabolized in the liver to active metabolites, with 72% of an oral dose primarily excreted in the urine as conjugated metabolites and up to 15% appearing in the feces.
N-demethylation to an active metabolite (CYP2D6) and hydroxylation of the naphthyl ring (CYP1A2) at either the 4-, 5-, or 6-positions are the main metabolic pathways for duloxetine. Its metabolites are primarily excreted into the urine as glucuronide, sulfate, and O-methylated conjugation products. The major metabolites found in plasma also were found in the urine. Preclinical data for 4-hydroxyduloxetine suggests it has a similar pharmacological profile to duloxetine, with selective inhibition of SERT but less activity at the NET.

Clinical Use

Duloxetine has been approved for the treatment of depression and diabetic peripheral neuropathic pain. It is another analogue in the line of fluoxetine-based products from Lilly, in which the phenyl and phenoxy groups of fluoxetine have been respectively replaced with the benzene isostere, thiophene, and a naphthyloxy group (previously described under fluoxetine). Duloxetine exhibits dual inhibition with high affinity for the SERTs and NETs, with a five times preferential inhibition of the SERT. Duloxetine appears to be a more potent in vitro blocker of SERTs and NETs than venlafaxine. In humans, duloxetine has a low affinity for the other neuroreceptors, suggesting low incidence of unwanted adverse effects.

Synthesis

Reaction of 2-acetylthiophene with paraformaldehyde and dimethylamine in ethanol gives 3-(dimethylamino)-1-(2-thienyl)- 1-propanone, which is enantioselectively reduced with a 2:1 complex of (2R,3S)-4-(dimethylamino)- 3-methyl-1,2-diphenyl-2-butanol and LiAlH4 in toluene to yield (S)-3-(dimethylamino)- 1-(2-thienyl)-1-propanol. The condensation of (S)-3-(dimethylamino)-1-(2- thienyl)-1-propanol with 1-fluoronaphthalene catalyzed by NaH in DMSO affords the corresponding naphthyl ether (S)-N,N-dimethyl-3- (naphthalen-1-yloxy)-3-(thiophen-2-yl)propan- 1-amine, which is finally monodemethylated with 2,2,2-trichloroethyl chloroformate and zinc in toluene and treated with oxalic acid .

Drug interactions

Potentially hazardous interactions with other drugs
Antibacterials: metabolism inhibited by ciprofloxacin - avoid.
Anticoagulants: possibly increased risk of bleeding with dabigatran.
Other CNS medication: enhanced effect.
Antidepressants: avoid with MAOIs, moclobemide, St John’s wort, tryptophan, venlaflaxine, amitriptyline, clomipramine and SSRIs due to increased risk of serotonin syndrome; increased risk of side effects with tricyclic antidepressants; fluvoxamine decreases the clearance of duloxetine by 77% - avoid; possible increased risk of convulsions with vortioxetine.
Antimalarials: avoid with artemether/lumefantrine and piperaquine with artenimol.
Dapoxetine: avoid concomitant use.
Methylthioninium: risk of CNS toxicity - avoid if possible.

Metabolism

Duloxetine is extensively metabolised and the metabolites are excreted principally in urine. Both cytochromes P450-2D6 and 1A2 catalyse the formation of the two major metabolites, glucuronide conjugate of 4-hydroxy duloxetine and sulphate conjugate of 5-hydroxy, 6-methoxy duloxetine. Based upon in vitro studies, the circulating metabolites of duloxetine are considered pharmacologically inactive

Duloxetine Preparation Products And Raw materials

Raw materials

1-Fluoronaphthalene

Preparation Products

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Duloxetine Suppliers

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View Lastest Price from Duloxetine manufacturers

Qingdao RENAS Polymer Material Co., Ltd.

Product: Duloxetine 116539-59-4
Price: US $0.00/kg
Min. Order: 20kg
Purity: 99%
Supply Ability: 20 tons
Release date: 2024-10-15

Shanghai Chinqesen Biotechnology Co., Ltd.

Product: Duloxetine 116539-59-4
Price: US $40.00-20.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 2000000
Release date: 2023-10-25

Hebei Yalin Technology Co., Ltd

Product: Cymbalta 116539-59-4
Price: US $20.00-9000.00/KG
Min. Order: 10KG
Purity: 99.99%
Supply Ability: 90000KG
Release date: 2023-08-29

116539-59-4, DuloxetineRelated Search:

Paroxetine Duloxetine intermediate Duloxetine intermediate AA Duloxetine hydrochoride (rs)-duloxetine hydrochloride,(rs)-n-methyl-gama-(1-naphthalenyloxy)-2-thiophenepropanamine hydrochloride (r)-duloxetine,R-DULOXETINE HCL,(r)-n-methyl-gama-(1-naphthalenyloxy)-2-thiophenepropanamine (S)-(+)-N,N-Dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine Duloxetine Duloxetine hydrochloride 4-Hydroxy Duloxetine 4-Hydroxy Duloxetine -D-Glucuronide,4-Hydroxy Duloxetine b-D-Glucuronide S-(+)-N,N-DIMETHYL-3-(1-NAPHTHLENYLOXY)-3-(2-THIENYL)-PROPANAMINE Duloxetine-d3 HCl R-DULOXETINE HYDROCHLORIDE Duloxetine-naphthyl-D7 Maleate DULOXETINE MALEATE 5-Hydroxy-6-methoxy Duloxetine 5-Hydroxy-6-methoxy duloxetine sulfate

DULOXETINE

DULOXETINE-D3

(S)-DULOXETINE

DULOXETIN

(3S)-N-methyl-3-naphthalen-1-yloxy-3-thiophen-2-yl-propan-1-amine

N-Methyl-gama-(1-naphthalenyloxy)-2-thiophenepropanamine

DULOXETINE HCI

Duloxetine & Intermediates

N-methyl-3-(1-naphthalenyloxy)-3-thiophen-2-yl-1-propanamine hydrochloride

CS-559

methyl-[(3S)-3-(1-naphthyloxy)-3-(2-thienyl)propyl]amine

(3R)-N-methyl-3-(naphthalen-1-yloxy)-3-thiophen-2-ylpropan-1-amine

(S)-N-Methyl-3-(naphthalen-1-yloxy)-3-(thiophen-2-yl)propan-1-aMine

Duloxetine Hcl(S)

Duloxetine, >=99%

Methyl[(3S)-3-(naphthalen-1-yloxy)-3-(thiophen-2-yl)propyl]aMine

2-Thiophenepropanamine, N-methyl-γ-(1-naphthalenyloxy)-, (γS)-

Duloxetine USP/EP/BP

(+)-Duloxetine

Raw Powder API Duloxetine

DuloxetinehclQ: What is Duloxetinehcl Q: What is the CAS Number of Duloxetinehcl Q: What is the storage condition of Duloxetinehcl Q: What are the applications of Duloxetinehcl

Duloxetine ((S)-Duloxetine

116539-59-4

1165399-59-4

C18H18ONSHCL

C18N19NOS

C18H19NOS

API

ACTIVE PHARMACEUTICAL INGREDIENTS