52916-82-2

Upstream product

• 99-93-4 4-Hydroxyacetophenone 
• 79-44-7 N,N-Dimethylcarbamoyl chloride 
• 121-71-1 3-Hydroxyacetophenone 
• 68-12-2 N,N-dimethyl-formamide 

Downstream Products

• 92-91-1 biphenyl-4-acetaldehyde 
• 1527477-77-5 (2E,4Z)-ethyl 5-(dimethylcarbamoyloxy)-5-(4-(dimethylcarbamoyloxy)phenyl)-3-(prop-1-en-2-yl)penta-2,4-dienoate 
• 1631050-54-8 4-acetyl-2-hydroxyphenyl dimethylcarbamate 
• 460088-33-9 1-(4-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)phenyl)ethan-1-one 
• 578730-15-1 dimethylcarbamic acid 4-[1-hydroxy-3-(4-nitrophenyl)propyl]phenyl ester 
• 663184-13-2 dimethyl-carbamic acid 4-[1-bromo-3-(4-nitro-phenyl)-propyl]-phenyl ester 

Relevant academic research and scientific papers

The synthesis of phenyl carbamates catalyzed by iron (II) bromide: An oxidative approach for cross-coupling of phenols with formamides

The carbamate group is a key structural motif in many approved drugs and pro-drugs. There is increasing use of carbamates in the medicinal chemistry and agrochemical industry. We present, reagents and chemical methodologies for the synthesis of carbamates, and recent applications. The direct coupling of simple phenols with mono- and di-alkyl formamides provided the phenylcarbamate products.

Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase

Rivastigmine, a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), has been approved by U.S. Food and Drug Administration to treat Alzheimer's disease (AD) and Parkinson's disease (PD) dementia. In the current work, a bambuterol derivative lacking one of the carbamoyloxy groups on the benzene ring (BMC-1) and its analogues were synthesized using 1-(3-hydroxyphenyl) ethan-1-one and 1-(4-hydroxyphenyl) ethan-1-one as starting materials. In-vitro cholinesterase assay established that nine compounds were more potent to inhibit both electric eel AChE and equine serum BChE than rivastigmine under the same experimental conditions. Further study confirmed that among the nine carbamates, BMC-3 (IC50(AChE) = 792 nM, IC50(BChE) = 2.2 nM) and BMC-16 (IC50(AChE) = 266 nM, IC50(BChE) = 10.6 nM) were excellent cholinesterase inhibitors with potential of permeating through the blood-brain barrier. These carbamates could be used as potential dual inhibitors of AChE and BChE and to discover novel drugs for the treatment of AD and PD dementia.

Compound as well as preparation method and application thereof

The invention discloses a compound as well as a preparation method and application thereof and belongs to the field of medicines. The compound is a carbamyl ester derivative of a phenylethanolamine structure, and has a chemical structure formula (I) shown in the specification. The compound has remarkable functions of inhibiting acetylcholin esterase and butyrylcholine esterase, can be used as a double-target cholinesterase inhibitor, and can be also applied to preparation of medicines for treating diseases related to cholinesterase.

Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors

A series of novel chalcone-rivastigmine hybrids were designed, synthesized, and tested in vitro for their ability to inhibit human acetylcholinesterase and butyrylcholinesterase. Most of the target compounds showed hBChE selective activity in the micro- a

A kind of carbamate-koncar ketone choline esterase inhibitor and its preparation method and application (by machine translation)

The present invention discloses a kind of carbamate-koncar ketone choline esterase inhibitor and its preparation method and application, belongs to the field of medicinal chemistry. Cholinesterase inhibitors of the invention represented by general formula

One-Pot Synthesis of O -Aryl Carbamates

A simple, versatile, one-pot procedure for the synthesis of substituted O-aryl carbamates has been developed, and a protocol is henceforth described. N-Substituted carbamoyl chloride is formed in situ and subsequently reacted with a substituted phenol, avoiding the direct manipulation of sensitive reactants. This procedure offers an economical and efficient route to many compounds of interest.

A general approach towards catechol and pyrogallol through ruthenium- and palladium-catalyzed C-H hydroxylation by weak coordination

An efficient ruthenium(II)- and palladium(II)-catalyzed C-H hydroxylation of aryl carbamates has been developed for the facile synthesis of catechols and pyrogallols. The reaction demonstrates excellent reactivity, regio- and chemoselectivity, good functional group compatibility and high yields. The practicality of this method has been proved by a gram-scale synthesis.

Nickel-catalyzed efficient and practical Suzuki-Miyaura coupling of alkenyl and aryl carbamates with aryl boroxines

(Figure Presented) Suzuki-Miyaura coupling of unactivated alkenyl carbamates Is described to construct polysubstituted olefins. The developed process is also suitable for heteroaromatic and even electron-rich aromatic carbamates.

Design, Synthesis and Structure-Activity Relationships of Dual Inhibitors of Acetylcholinesterase and Serotonin Transporter as Potential Agents for Alzheimer's Disease

We have designed and synthesized a dual inhibitor of acetylcholinesterase (AChE) and serotonin transporter (SERT) as a novel class of treatment drugs for Alzheimer's disease on the basis of a hypothetical model of the AChE active site. Dual inhibitions of AChE and SERT would bring about greater therapeutic effects than AChE inhibition alone and avoid adverse peripheral effects caused by excessive AChE inhibition. Compound (S)-6j exhibited potent inhibitory activities against AChE (IC50 = 101 nM) and SERT (IC50 = 42 nM). Furthermore, (S)-6j showed inhibitory activities of both AChE and SERT in mice brain following oral administration.

Treatment and prophylaxis of diseases caused by parasites, or bacteria

Aromatic compounds, or prodrugs thereof, which contain an alkylating site and which are capable of alkylating the thiol group in N-acetyl-L-cysteine, in particular bis-aromatic α,β-unsaturated ketones, are used for the preparation of pharmaceutical compositions or medicated feed, food or drinking water for the treatment or prophylaxis of diseases caused by microorganisms or parasites, in particular protozoa such as Leishmannia, Trypanosoma, Toxoplasma, Plasmodium, Pneumocystis, Babesia and Theileria, intestinal protozoa such as Trichormionas and Ciardia; Coccidia such as Eimeria, Isospora, Cryptosporidium; Cappilaria, Microsporidium, Sarcocystis. Trichlodina, Trichoditella, Dacihylogurus, Pseudodacthylogurus, Acantocephalus, Ichthylophtherius, Botrecephalus; and intracellular bacteria, in particular Mycobacterium, Legionella species, Listeria and Salmonella. Preferred compounds have the formula (II): Xm --Ph--C(O)--CH=CH--Ph--Yn, wherein each phenyl group (Ph) may be mono- or polysubstituted; X and Y designate ARH or AZ, wherein A is O, S, NH or N(C1-6 alkyl), RH designates aliphatic hydrocarbyl, and Z is H or a masking group which is decomposed to liberate AH; m is 0, 1 or 2, and n is 0, 1, 2 or 3, whereby, when m is 2, then the two X are the same or different, and when n is 2 or 3, then the two or three Y are the same or different, with the proviso that n and m are not both 0. As examples of such compounds, chalcones, e.g. licochalcone A (obtainable i.a. from batches of Chinese licorice root of Glycyrrhiza species, e.g. G. uralensis or G. inflata) as well as hydroxy, alk(en)yl, and/or alk(en)yloxy analogues thereof are active in vitro and/or in vivo against i.a. L. major and P. falciparum.