Intermediate of API

120014-06-4

  • Product Name：Donepezil base
  • Molecular Formula：C24H29NO3
  • Specifications：99%
  • Molecular Weight：379.499
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Product Details;

CasNo： 120014-06-4

Molecular Formula： C24H29NO3

Appearance： white or almost white crystal powder

High Quality Donepezil base 120014-06-4 Powder In Stock

  • Molecular Formula:C24H29NO3
  • Molecular Weight:379.499
  • Appearance/Colour:white or almost white crystal powder 
  • Vapor Pressure:3.11E-11mmHg at 25°C 
  • Melting Point:207 ºC 
  • Refractive Index:1.578 
  • Boiling Point:527.9 ºC at 760 mmHg 
  • PKA:8.84±0.10(Predicted) 
  • Flash Point:273.1 ºC 
  • PSA：38.77000 
  • Density:1.141 g/cm3 
  • LogP:4.29900 

2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one(Cas 120014-06-4) Usage

Description

Donepezil is a specific and potent acetylcholinesterase inhibitor according to in vitro data. It displays primarily noncompetitive inhibitory activity. Donepezil is another “nonclassic,” centrally acting, reversible, noncompetitive AChEI that was approved in 1997 for treatment of mild-to-moderate AD and dementia. Its selectivity for AChE is 570- to 1,250-fold that for butyrylcholinesterase, and it also exhibits greater affinity for brain AChE than for AChE in the periphery. 2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one is a chemical compound that is not approved for use in humans. Therefore, its safety and efficacy have not been established. It is important to note that the safety of any chemical compound depends on various factors, including the dosage, route of administration, and individual factors such as age, health status, and medical history.

Uses

 Donepezil works by increasing the levels of a neurotransmitter called acetylcholine in the brain, which can help improve cognitive function and memory. Donepezil is available in various forms, including tablets and orally disintegrating tablets, and is typically taken once daily. As with any medication, it is important to follow your doctor's instructions carefully and to report any side effects or concerns.

Definition

ChEBI: Donepezil is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.

Brand name

Aricept (Eisai Medical Research).

Isomeric SMILES: COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC  
InChIKey: ADEBPBSSDYVVLD-UHFFFAOYSA-N  
InChI: InChI=1S/C24H29NO3/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18/h3-7,14-15,17,20H,8-13,16H2,1-2H3  

120014-06-4 Relevant articles

Effect of fatty acids on the transdermal delivery of donepezil: In vitro and in vivo evaluation

Joonho Choi a, Min-Koo Choi b, Saeho Chong a, Suk-Jae Chung a, Chang-Koo Shim a, Dae-Duk Kim a

, International Journal of Pharmaceutics Volume 422, Issues 1–2, 17 January 2012, Pages 83-90

The relative in vitro skin permeation rate of donepezil (DP) through the hairless mouse skin showed a parabolic relationship with increased carbon length of the fatty acid enhancers.

Donepezil for dementia due to Alzheimer's disease

JS Birks, RJ Harvey

, Jacqueline S BirksRichard J Harvey

Our main analysis compared the safety and efficacy of donepezil 10 mg/day with placebo at 24 to 26 weeks of treatment. This can be done by a group of drugs known as cholinesterase inhibitors. Donepezil is a cholinesterase inhibitor.

New synthesis of donepezil through palladium-catalyzed hydrogenation approach

Elati, Chandrashekar R.,Kolla, Naveenkumar,Chalamala, Subrahmanyeswara Rao,Vankawala, Pravinchandra J.,Sundaram, Venkataraman,Vurimidi, Himabindu,Mathad, Vijayavitthal T.

, p. 169 - 174 (2006)

A new, economical, and efficient process...

Bisulfite Addition Compounds as Substrates for Reductive Aminations in Water

Bailey, J. Daniel,Iyer, Karthik S.,Leahy, David K.,Li, Xiaohan,Lipshutz, Bruce H.,Thakore, Ruchita R.

, p. 7205 - 7208 (2021/09/22)

Highly valued products resulting from re...

A metal-free method for the facile synthesis of indanonesviathe intramolecular hydroacylation of 2-vinylbenzaldehyde

He, Guoxue,Ma, Jinyu,Zhou, Jianhui,Li, Chunpu,Liu, Hong,Zhou, Yu

supporting information, p. 1036 - 1040 (2021/02/09)

A facile method for the synthesis of ind...

Can Heteroarenes/Arenes Be Hydrogenated Over Catalytic Pd/C Under Ambient Conditions?

Tanaka, Nao,Usuki, Toyonobu

, p. 5514 - 5522 (2020/07/24)

Hydrogenation of over a dozen aromatic c...

120014-06-4 Process route

benzyl bromide
100-39-0

benzyl bromide

debenzyldonepezil
120014-30-4

debenzyldonepezil

donepezil
120014-06-4,142057-79-2,142057-80-5,142698-19-9

donepezil

Conditions
Conditions Yield
With sodium carbonate; In ethanol; at 50 - 60 ℃; for 6h;
92.3%
With triethylamine; In dichloromethane; for 4h; Heating / reflux;
 
benzyl bromide; debenzyldonepezil; With tetrabutylammomium bromide; potassium carbonate; In dichloromethane; water; at 20 ℃;
With hydrogenchloride; In methanol;
 
With sodium carbonate; In methanol; isopropyl alcohol; at 55 - 60 ℃; for 11h;
 
benzyl bromide; debenzyldonepezil; With potassium carbonate; acetic acid; palladium 10% on activated carbon; In water; ethyl acetate; at 25 - 30 ℃; for 4h;
With sodium hydroxide; In water; ethyl acetate;
 
With sodium carbonate; In isopropyl alcohol; at 50 ℃; for 12h;
32.3 mg
5,6-dimethoxy-1-indanone
2107-69-9

5,6-dimethoxy-1-indanone

1-benzyl-4-piperidinemethanol
67686-01-5

1-benzyl-4-piperidinemethanol

donepezil
120014-06-4,142057-79-2,142057-80-5,142698-19-9

donepezil

Conditions
Conditions Yield
With bis(μ-chloro)-bis[1,3-di(2-pyridyl)-4,6-dimethylbenzene-N,C(2'),N-iridium chloride]; caesium carbonate; In tert-Amyl alcohol; for 12h; Reflux;
85%
With [Ir(dpyx-N,C,N)Cl(i-Cl)]2; caesium carbonate; In tert-Amyl alcohol; at 130 ℃; for 2h; Reagent/catalyst;
85%
With potassium phosphate tribasic trihydrate; C39H32Cl2N5PRu; In tert-Amyl alcohol; at 120 ℃; for 4h; Inert atmosphere; Schlenk technique;
83%
With C39H32Cl2N5PRu; potassium tert-butylate; In tert-Amyl alcohol; at 120 ℃; for 12h; Solvent; Reagent/catalyst; Inert atmosphere; Schlenk technique;
83%
With [(Cp*IrCl)2(4,4′,6,6′-tetrahydroxy-2,2′-bipyrimidine)][Cl]2; potassium hydroxide; In water; at 100 ℃; for 12h; Green chemistry;
82%
With [(Cp*IrCl)2(4,4′,6,6′-tetrahydroxy-2,2′-bipyrimidine)][Cl]2; potassium hydroxide; In water; at 130 ℃; for 12h; Reagent/catalyst;
82%
With trifuran-2-yl-phosphane; C48H34F6N4O4Pd2; lithium hydroxide; In neat (no solvent); at 100 ℃; for 48h; Inert atmosphere; Schlenk technique; Sealed tube;
46%
With 1,10-Phenanthroline; potassium tert-butylate; nickel dibromide; In toluene; at 140 ℃; for 36h; Schlenk technique; Sealed tube; Inert atmosphere;
46%
With [bis(2-methylallyl)cycloocta-1,5-diene]ruthenium(II); 1,3-bis((R)-1-(naphthalen-1-yl)ethyl)-4,5-dihydro-1H-imidazol-3-ium tetrafluoroborate; potassium tert-butylate; lithium tert-butoxide; In hexane; pentan-1-ol; at 100 ℃; for 24h;
40%
With 1,10-Phenanthroline; bis(acetylacetonato)manganese(II); potassium tert-butylate; In toluene; at 140 ℃; for 36h; Schlenk technique; Inert atmosphere;
40%
With diiron nonacarbonyl; potassium tert-butylate; In toluene; at 140 ℃; for 24h; Schlenk technique; Inert atmosphere;
36%

120014-06-4 Upstream products

  • 848610-96-8
    848610-96-8

    5-[(1-benzyl-4-piperidyl)methyl]-5-(3,4-dimethoxybenzyl)-2,2-dimethyl-1,3-dioxane-4,6-dione

  • 100-39-0
    100-39-0

    benzyl bromide

  • 120014-30-4
    120014-30-4

    debenzyldonepezil

  • 145546-80-1
    145546-80-1

    (E)-2-((1-benzylpiperidine-4-yl)methylene)-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one

120014-06-4 Downstream products

  • 120012-04-6
    120012-04-6

    1-benzyl-4-[(5,6-dimethoxy-1-indanol)-2-yl]methylpiperidine

  • 142057-77-0
    142057-77-0

    donepezil hydrochloride

  • 130927-68-3
    130927-68-3

    1-Benzyl-4-[(5,6-dimethoxyinden)-2-yl]methylpiperidine hydrochloride

  • 884740-09-4
    884740-09-4

    1-benzyl-4-((5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine hydrochloride monohydrate

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