81654-47-9

Upstream product

• 55-81-2 4-Methoxyphenethylamine 
• 407-25-0 trifluoroacetic anhydride 

Downstream Products

• 81654-48-0 N-<2-(4-methoxy-3-nitrophenyl)ethyl>-2,2,2-trifluoroacetamide 
• 144818-94-0 5-<2-(trifluoroacetylamino)ethyl>-2-methoxybenzenesulfonyl chloride 
• 125960-59-0 2-Methoxy-5-(2-(2,2,2-trifluoroacetamido)ethyl)benzenesulfonamide 
• 308336-31-4 5-(2-aminoethyl)-2-methoxybenzenesulfonamide 
• 705279-04-5 2,2,2-trifluoro-N-(2-{4-methoxy-3-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}ethyl) acetamide 

Relevant academic research and scientific papers

N2-(2-METHOXYPHENYL)PYRIMIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION FOR CANCER PREVENTION OR TREATMENT CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.

PYRIMIDINE-2,4-DIAMINE DERIVATIVE AND ANTICANCER PHARMACEUTICAL COMPOSITION COMPRISING SAME AS EFFECTIVE INGREDIENT

The present invention relates to a pyrimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for prevention or treatment of cancer comprising the same as an effective ingredient. A compound according

Discovery of novel tetrahydroisoquinoline-containing pyrimidines as ALK inhibitors

Exploration of the two-position side chain of pyrimidine in LDK378 with tetrahydroisoquinolines (THIQs) led to discovery of 8 and 17 as highly potent ALK inhibitors. THIQs 8 and 17 showed encouraging in vitro and in vivo xenograft efficacies, comparable w

Hexamethyldisilazane as an acylation generator for perfluorocarboxylic acids in quantitative derivatization of primary phenylalkyl amines confirmed by GC/MS and computations

A novel, selective acylation of primary phenylalkyl amines (PPAAs) using hexamethyldisilazane (HMDS) and perfluorocarboxylic acids (PFCAs) is noted. Couples, like HMDS and trifluoroacetic acid, HMDS and pentafluoropropionic acid, or HMDS and heptafluorobutyric acid trigger PPAAs' quantitative acylation. Processes' selectivity was characterized by applying all couples to derivatize benzyl, 2-phenylethyl, 3-phenylpropyl, 4-phenylbutyl amines, and their relevant substituted versions. Aliphatic amines were unreactive. Identification, quantification, proportionality, and stoichiometry in derivatization processes were determined by gas chromatography/mass spectrometry. Reaction conditions were optimized depending on reagents' molar ratios, solvents, and temperatures applied. The new acylation method, in comparison to the traditional ones, obtained with trifluoroacetic anhydride, heptafluorobutyric anhydride, and N-methyl-bis(trifluoroacetamide), offers numerous advantages. Derivatives, provided by couples, can be directly injected onto the column, avoiding loss of species, saving time, work, and cost in the preparation process. Due to traditional reagents' excess evaporation by nitrogen drying, the loss of trifluoroacylated species proved to be 65% or less. Regarding heptafluorobutyryl species, their losses varied between 25% and 5%. Unified huge responses, obtained with the HMDS and PFCA couples are attributable to their direct injection onto the column and to fragments sourced from the molecular ions and from their self-chemical ionization ([M]?+, [M+147]+, i.e., [M+(CH3)2-Si=O-Si-(CH3)3]+). The reaction mechanism, due to the HMDS symmetrical structure, acting HMDS as acylation generator for PFCAs, was confirmed by density functional theory (DFT) computation.

PYRIMIDINE DERIVATIVES USED AS ITK INHIBITORS

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular ltk activity.

ANILINOPYRAZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF DIABETES

The present invention relates to anilinopyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.

Acylaminoalkyl-substituted benzenesulfonamide derivatives, their preparation, their use and pharmaceutical preparations comprising them

One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1in which A, R(1), R(2), X, Y, and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salt

Cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives, processes for their preparation, their use, and pharmaceutical preparations comprising them

The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula I in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y, and Z have the meanings indicated in the claims. Compounds of formula I are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death, or for improving decreased contractility of the heart. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, and pharmaceutical preparations comprising them.

Preparation of 1,2,3,4-tetrahydroisoquinolines lacking electron donating groups - An intramolecular cyclization complementary to the Pictet-Spengler reaction

The synthesis of 1,2,3,4-tetrahydroisoquinolines via an intramolecular cyclization of N-trifluoroacylated phenethylamines devoid of electron donating groups, with paraformaldehyde mediated by acetic/sulfuric acid milieu is described.

Photochemical trifluoromethylation of tyramine and L-tyrosine derivatives

Ultraviolet irradation (254 nm) of methanolic solutions of trifluoromethyl iodide (CF3I) in the presence of side-chain-protected tyramine and L-tyrosine results in trifluoromethylation of the aromatic ring.The presence of an amine base to neutralize HI formed during the reaction is essential.The electrophilic trifluoromethyl radical preferentially attacks the ring ortho to the phenolic group, and 3-trifluoromethyltyramine and 3-trifluoromethyl-L-tyrosine derivatives were obtained in yields of 27percent and 33percent, respectively.