1130155-48-4

Usage

Uses

Used in Pharmaceutical Industry:
(E)-4-(dimethylamino)but-2-enoic acid (Hydrochloride) is used as a key intermediate in the synthesis of tricyclic nitrogen heterocyclic compounds and related heteroanalogs. These complex organic molecules have demonstrated potential in the prevention or treatment of cancer, making (E)-4-(diMethylaMino)but-2-enoic acid (Hydrochloride) a valuable building block in the development of novel anticancer drugs.
In the pharmaceutical industry, the compound serves as a crucial component in the creation of new chemical entities that target specific biological pathways and mechanisms associated with cancer. Its unique structure allows for the formation of diverse tricyclic nitrogen heterocyclic compounds, which can be further optimized for improved efficacy, selectivity, and reduced side effects.
Furthermore, the use of (E)-4-(dimethylamino)but-2-enoic acid (Hydrochloride) in the synthesis of these heterocyclic compounds enables researchers to explore a wide range of structural variations and modifications. This flexibility is essential for the discovery of new drugs with improved pharmacological properties, such as increased potency, better pharmacokinetics, and enhanced safety profiles.
Overall, the application of (E)-4-(dimethylamino)but-2-enoic acid (Hydrochloride) in the pharmaceutical industry highlights its importance in the ongoing quest for innovative and effective cancer therapies. Its role as a versatile intermediate in the synthesis of tricyclic nitrogen heterocyclic compounds and related heteroanalogs positions it as a promising candidate for further research and development in the field of medicinal chemistry.

Upstream product

• 13991-36-1 4-bromocrotonic acid 
• 124-40-3 dimethyl amine 
• 98552-51-3 ethyl 4-(dimethylamino)crotonate 
• 1259519-60-2 4-dimethylaminocrotonic acid methyl ester hydrochloride 
• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 
• 1421354-12-2 (E)-4-dimethylamino-but-2-enoic acid tert-butyl ester 
• 1255078-56-8 (E)-ethyl 4-(dimethylamino)but-2-enoate hydrochloride 
• 212776-19-7 (E)-4-(dimethylamino)-2-butenoic acid methyl ester 
• 1413945-87-5 dimethylaminoacetaldehyde-hydrogen sulphite adduct 
• 88738-78-7 bis-(2,2,2-trifluoroethyl)(methoxycarbonylmethyl)phosphonate 

Downstream Products

• 1610697-15-8 (R,E)-1-(3-(4-amino-6-fluoro-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)pyrrolidin-1-yl)-4-(dimethylamino)but-2-en-1-one 
• 1612182-63-4 (2E)-N-{3-[2-amino-6-(methylamino)pyrimidin-4-yl]phenyl}-4-(dimethylamino)but-2-enamide 
• 1345250-38-5 C₃₂H₃₀F₃N₇O₂ 
• 1345250-34-1 C₂₄H₂₆N₆O 
• 1345250-74-9 C₂₄H₂₄ClFN₆O 
• 1345250-72-7 C₂₃H₂₂Cl₂N₆O 
• 1345250-70-5 C₂₄H₂₅ClN₆O 
• 1345250-86-3 C₂₄H₂₅N₅OS 
• 1345250-68-1 C₂₄H₂₄F₂N₆O 
• 1345250-66-9 C₂₄H₂₄F₂N₆O 
• 1345250-64-7 C₂₃H₂₂ClFN₆O 
• 1345250-62-5 C₂₄H₂₅FN₆O 
• 1345250-60-3 C₂₄H₂₆N₆O₂ 

Relevant academic research and scientific papers

A EGFR molecule targeting anti-tumor pharmaceutical preparation method

The invention relates to a preparation method for an EGFR molecule targeting antitumor drug, and provides a preparation method for (E)-N-[4-(3-acetylene phenyl)amino-3-cyan-7-ethoxy-6-quinolyl]-4-(dimethyl amino)-2-butylene amide. The preparation method comprises the following steps: N-(4-chloro-3-cyan-7-ethoxy quinoline-6-yl) acetamide (a compound II) and 3-aminophenylacetylene (a compound III) are subjected to a substitution reaction, and a compound IV is obtained; under an acidic or alkaline condition, the compound IV is subjected to a hydrolysis reaction, and 3-cyan-6-amino-7-ethoxy-4-(3-acetenyl anilino) quinoline (a compound V) is obtained; after trans-4-dimethylaminocrotonic acid hydrochloride (a compound VI) and an acylation reaction reagent is subjected to an acylation reaction, the product and 3-cyan-6-amino-7-ethoxy-4-(3-acetenyl anilino) quinoline (the compound V) are subjected to condensation reaction, and the finished product is obtained. The method is advantageous in that raw materials are easily available, the technology is concise, the production cost is low, and the method is economical and environmentally friendly and is suitable for industrial production.

Chlorobenzene-pyridine compounds and application thereof

The invention relates to chlorobenzene-pyridine compounds and an application thereof. The compounds can be used for preparing a Smoothened protein inhibitor and a drug for resisting adenocarcinoma andesophagus cancer and have the structure in the general formula (I) shown in the description, wherein X is selected from the structure shown in the description, R1 is selected from H or the structureshown in the description, and R2 is selected from the structure shown in the description.

Synthetic method for (2Z)-4-(dimethylamino)but-2-enoic acid hydrochloride

The invention discloses a synthetic method for (2Z)-4-(dimethylamino)but-2-enoic acid hydrochloride. The synthetic method comprises the following steps: under an inert gas atmosphere, dissolving [bi(2,2,2-trifluoroethoxy)-phosphinyl]methyl acetate in organic solvent, adding lithium reagent, adding alkali solution, controlling the temperature to 0-30 DEG C, adding 2-(dimethylamino)acetaldehyde sulfite, and carrying out stirring reaction, carrying out acidification, extraction and column purification after reaction to obtain the (2Z)-4-(dimethylamino)but-2-enoic acid hydrochloride. The syntheticmethod has the advantages of convenience in operation and high yield, and industrial production can be realized.

QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF

Disclosed are a quinazoline derivative, a preparation method therefor, and a pharmaceutical composition and an application thereof. The present invention provides a compound represented by general formula I, a stereoisomer thereof and a pharmaceutical acceptable salt or a solvate thereof. The quinazoline derivative of the present invention has a unique chemical structure, is characterized by irreversibly inhibiting EGFR tyrosine kinase, has high biological activity, apparently improves the inhibiting effect on the EGFR tyrosine kinase, has quite strong tumor inhibiting effect on tumor cells and a transplantation tumor pathological model of animal tumors, and has good market developing prospects.

A steps Hua Tini chemical synthesis method (by machine translation)

The present invention provides a convenient steps Hua Tini chemical synthesis method, using the synthesis method adopted in the process of preparing steps Hua Tini cheap raw materials, is easy to obtain, and saves the production cost, and the adoption of the synthesis method of the high yield of the product, the whole in the preparation process of mild reaction conditions, the atom economy is high. (by machine translation)

Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors

A series of thirty two anilinopyrimidines derived from WZ4002 has been synthesized and evaluated for percentage inhibition of six different EGFR kinases using LanthaScreen binding assay method (EGFR d746 – 750) or Z'LYTE assay method (EGFR-WT, EGFR d746 – 750, EGFR T790M, EGFR T790M L858R, EGFR C797S and EGFR T790M L858R C797S). Ortho-hydroxyacetamide 10 exhibited complete inhibition of all the six kinases at 10 μM. Against the triple mutant, EGFR T790M C797S L858R, compounds 9–12 exhibited complete inhibition at 10 μM and nearly complete inhibition at 1 μM. The target compounds were also evaluated using the MTT assay to determine their cytotoxic activity against human non-small cell lung cancer cells (PC9, PC9GR and H460) and mouse leukemic cells (Ba/F3 WT and Ba/F3T 3151). Overall, 7, 9–12, 30 and 31 were found to be the most potent compounds across all five cell lines.

PYRAZOLYLAMINOPURINES AS ITK INHIBITORS

Provided are pyrazolylaminopurine compounds that are inhibitors of ITK kinase, compositions containing these compounds and methods for treating diseases mediated by ITK kinase. In particular, provided are compounds of Formula I or II, stereoisomers, tauto

A trans-4-dimethylamino crotonic acid hydrochloride preparation method (by machine translation)

A trans-4-dimethylamino crotonic acid hydrochloride preparation method, to N, N-dimethylamine base acetaldehyde bisulfite as the substrate, the phosphono acetic acid three diethlyl generating HWE reaction to obtain trans-4-dimethylamino crotonic acid hydrochloride. Through the preferred reaction conditions, the reaction to obtain HWE trans-4-dimethylamino crotonic acid hydrochloride. (by machine translation)

Preparation method for afatinib

The invention provides a preparation method for afatinib. The preparation method comprises the following steps: subjecting trans-4-dimethylaminocrotonic acid hydrochloride (III) to chlorination so as to obtain trans-4-dimethylaminocrotonyl chloride hydrochloride (IV); and reacting the compound (IV) with N4-(3-chloro-4-fluoro-phenyl)-7-((S)-tetrahydrofuran-3-yl-oxy)quinazoline-4,6-diamine (V) so as to prepare afatinib (VI). Reaction equations are described in the specification.

Pyrazolopyrimidine derivative, preparation method, pharmaceutical composition and application

The invention discloses a pyrazolopyrimidine derivative, a preparation method, a pharmaceutical composition and application. The invention provides the pyrazolopyrimidine derivative as shown in a formula I and stereoisomer or solvate or pharmaceutically acceptable salts or active metabolite or prodrug thereof. The pyrazolopyrimidine derivative as shown in the formula I has good inhibitory activity on Bruton's tyrosine kinase (Btk) and particularly has good in vitro and in vivo inhibitory activity on growth of tumor cells, and a good marketization prospect is achieved. Please see the formula I in the description.