570-08-1

Usage

Chemical Properties

Colorless liquid

Uses

Diethyl acetylmalonate is used as pharmaceutical intermediates.

InChI:InChI=1/C9H14O5/c1-3-5(4-2)7(10)6(8(11)12)9(13)14/h5-6H,3-4H2,1-2H3,(H,11,12)(H,13,14)/p-2

Upstream product

• 541-41-3 chloroformic acid ethyl ester 
• 1007476-32-5 sodium ethyl acetylacetate enolate 
• 60-29-7 diethyl ether 
• 996-82-7 sodium diethylmalonate 
• 75-36-5 acetyl chloride 
• 105-53-3 diethyl malonate 
• 463-51-4 Ketene 
• 108-22-5 Isopropenyl acetate 
• 109572-65-8 BrMgCH(CO₂Et)2 
• 73453-43-7 Ethyl Acetyl-N-cyclohexylmalonamate 
• 7647-01-0 hydrogenchloride 
• 542-05-2 acetonedicarboxylic acid 
• 64-17-5 ethanol 
• 3044-06-2 diethyl 2-(1-ethoxyethylidene)malonate 

Downstream Products

• 72959-49-0 (1-acetoxy-ethylidene)-malonic acid diethyl ester 
• 21712-92-5 2-ethoxycarbonylmethyl-2-hydroxy-4-oxo-6-phenyl-cyclohexane-1,3,5-tricarboxylic acid triethyl ester 
• 17797-55-6 1-ethyl-4-hydroxy-2,6-diphenyl-1,2,3,6-tetrahydro-pyridine-3,5-dicarboxylic acid diethyl ester 
• 17797-56-7 (+/-)-1-ethyl-4-oxo-2t,6t-diphenyl-piperidine-3r,5c-dicarboxylic acid diethyl ester 
• 21272-30-0 5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid ethyl ester 
• 13514-79-9 6-methyl-2-phenyl-3H-pyrimidin-4-one 
• 19900-25-5 (6-oxo-2-phenyl-1,6-dihydro-pyrimidin-4-yl)-acetic acid ethyl ester 
• 148516-28-3 3-oxo-2-phenylhydrazono-glutaric acid diethyl ester 
• 6943-68-6 (2-amino-6-oxo-1,6-dihydro-pyrimidin-4-yl)-acetic acid 
• 148516-30-7 2-(4-nitro-phenylhydrazono)-3-oxo-glutaric acid diethyl ester 
• 125732-40-3 4-ethoxycarbonyl-3-methyl-3-pyrazolin-5-one 
• 146037-86-7 3-methyl-5-oxo-2,5-dihydro-isoxazole-4-carboxylic acid ethyl ester 
• 58979-86-5 (5-oxo-2,5-dihydro-1H-pyrazol-3-yl)-acetic acid hydrazide 
• 18457-90-4 Thioacetyl-malonsaeure-diaethylester 

Relevant academic research and scientific papers

A facile synthesis of dispersable NaCl nanocrystals

During the classical malonic ester synthesis, sodium chloride is eliminated. Sodium diethyl malonate was reacted either with phenacyl chloride or acetyl chloride, both in toluene solution and without solvent. NaCl nanocrystals with a size of 100-300 nm were obtained that could be easily redispersed in organic solvents if phenacyl chloride was used as reagent. The dispersion in dichloromethane was stable for at least two weeks without sedimentation or agglomeration. The Royal Society of Chemistry 2009.

1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES

The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.

Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan

Inspired by the well-known PPARγ partial agonism of angiotensin II type 1 receptor (AT1R) antagonists exemplified by an antihypertensive drug, Telmisartan, efforts to identify compounds with the dual activities have been pursued in order to control the two major metabolic disorders, hypertension and hyperglycemia simultaneously. Lead compound 18 derived from the AT1R antagonist, Fimasartan, has successfully presented the possibility to control the medical conditions by a single molecule.

Synthesis of β-arylacyl / β-heteroarylacyl-β-alkylidene malonates and their application in substituted pyridone synthesis

A novel approach has been developed for the synthesis of β-arylacyl/β-heteroarylacyl-β-alkylidine malonates in moderate to good yields by the reaction of Stork aryl and heteroaryl enamine with β-chloroalkylidene malonates. The reaction involves conjugate

Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors

A structure-activity relationship study of 4-anilinopyrimidines for dual EGFR/Her-2 inhibitor has resulted in the identification of 4-anilino-5-alkenyl or 5-alkynyl-6-methylpyrimidine derivatives that have exhibited effective inhibitory activity against both enzymes. The presence of 5-alkenyl or 5-alkynyl moiety bearing terminal hydrophilic group played important role for inhibition of these enzymes. Selected compounds in the series demonstrated some activity against Her-2 dependent cell line (BT474).

Synthesis of novel 5-alkyl/aryl/heteroaryl substituted diethyl 3,4-dihydro-2H-pyrrole-4,4-dicarboxylates by aziridine ring expansion of 2-[(aziridin-1-yl)-1-alkyl/aryl/heteroaryl-methylene]malonic acid diethyl esters

A novel synthetic methodology has been developed for the synthesis of diethyl 5-alkyl/aryl/heteroaryl substituted 3,4-dihydro-2H-pyrrole-4,4- dicarboxylates (also called 2-substituted pyrroline-4,5-dihydro-3,3-dicarboxylic acid diethyl esters) by iodide i

PYRAZOLOOXAZOLE COMPOUND

A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism. wherein R1 and R2 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, a C1-6 alkyl group substituted with a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, etc; R3, R4 and R5 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C1-6 alkoxy-C1-6 alkyl group, a C3-6 cycloalkoxy-C1-6 alkyl group or a halogen atom; R6 is a hydrogen atom or a C1-6 alkyl group; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkylthio group.

Zinc-mediated alkylation and acylation of 1,3-dicarbonyl compounds

1,3-Dicarbonyl compounds undergo smooth allylation, benzylation, propargylation, and acylation with halides using metallic zinc in DMF at 60 °C to afford the corresponding allyl, benzyl, 2-propynyl, and acylated 1,3-diesters in good yields. In the case of cyclic 1,3-diketones, the corresponding enol ethers are obtained as sole products instead of C-alkylation.

PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PDE4 INHIBITORS

The present invention provides a compound of formula (I) or a salt thereof (in particular, a pharmaceutically acceptable salt thereof): The invention also provides the use of the compounds or salts as inhibitors of phosphodiesterase type IV (PDE4) and/or

PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS

The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x): and wherein: Q1 is NH or NMe, in which case Q2 is -C(O)-, -S(O)2-, -C(O)NH- or -C(O)NMe-; or Q1 is a bond o