35513-41-8

Upstream product

• 108-31-6 maleic anhydride 
• 108-88-3 toluene 
• 1777-53-3 1-(p-tolyl)-2-(triphenylphosphoranylidene)ethanone 
• 619-41-0 4-(bromoacetyl)toluene 
• 2689-61-4 (2-oxo-2-p-tolylethyl)triphenylphosphonium bromide 
• 124658-44-2 C₁₃H₁₄O₃ 

Downstream Products

• 127574-07-6 β-(p-methylbenzoyl)-α-<3-methyl-5(4H)-oxo-1-phenyl>propionic acid 
• 155373-13-0 4-(p-toluoyl)-3,4-dihydro-5,6-benzocoumarin 
• 13863-26-8 9-Carboxy-10-p-toluoyl-Δ^4a(4b)-dodecahydro-phenanthren 
• 847410-27-9 2,3-dibromo-4-oxo-4-p-tolyl-butyric acid 
• 470485-36-0 2-[4-(4-methoxy-phenyl)-3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-6-ylsulfanyl]-4-oxo-4-p-tolyl-butyric acid 
• 2166-32-7 6-(4-methylphenyl)-3(2H)-pyridazinone 
• 127574-09-8 6,9,9a,9b-tetrahydro-8-(p-methylphenyl)-1-methyl-3-phenyl-3H-pyrazolo<3,4-c>pyridazino<4,3-e>pyridazine 
• 127574-13-4 6,9b-dihydro-8-(4-methylphenyl)-9-<(4-methoxyphenyl)methyl>-1-methyl-3-phenyl-3H-pyrazolo<3,4-c>pyridazino<4,3-e>pyridazine 
• 1606167-98-9 C₁₅H₁₄NO⁽¹⁺⁾*Br^(1-) 
• 1606168-01-7 C₂₈H₂₄OP⁽¹⁺⁾*Br^(1-) 
• 147674-85-9 [4-(5-Hydrazino-1,3-diphenyl-1H-pyrazol-4-yl)-6-p-tolyl-pyridazin-3-yl]-hydrazine 

Relevant academic research and scientific papers

A method for preparing [...] (by machine translation)

The invention discloses a method for synthesizing [...], existing technology with the different is, first of all the toluene with maleic anhydride Friedel-crafts reaction to obtain the 4 - oxo - 4 - (4 - methyl phenyl) - 2 - butenoic, then the same halogen addition to obtain the 3 - halo - 4 - oxo - 4 - (4 - methyl phenyl) - butyric acid, the esterification reaction, the ring, to obtain 2 - (6 - methyl - 2 - P-imidazole [1, 2 - α] pyridine - 3 - yl) acetate, the hydrolysis, acidifying the resulting [...]. The method of the invention, obtaining the high-purity [...], the whole synthetic route less steps, high yield, low cost, less impurities, is suitable for industrial production. (by machine translation)

Synthesis of 1,5-benzodiazepine derivatives using p-toluenesulfonic acid as catalyst

A series of substituted ethyl 4-oxo-4-phenylbut-2-enoates were prepared and reacted with substituted o-phenylenediamine, undergone Michael addition reactions and cyclodehydration to provide novel 4-phenyl-2,3-dihydro-1,5-benzodiazepine-2-carboxylate derivatives with excellent yields. The synthetic protocol fulfilled many green-chemical requirements by using simple catalyst p-toluenesulfonic acid as activator and ethanol as solvent at room temperature.

Structure-activity relationship, cytotoxicity and mode of action of 2-ester-substituted 1,5-benzothiazepines as potent antifungal agents

Our studies examined the structural features responsible for the antifungal activity of 2-ethoxycarbonyl-1,5-benzothiazepine (7a). Three series of 1,5-benzothiazepine derivatives were synthesized and screened for their antifungal activity. The results suggested that the ethoxycarbonyl group at the 2 position and the imine moiety on the seven-membered ring are essential for activity. The most potent of the synthesized analogues (7a, 7b) were further studied by evaluating their cytotoxicity and mode of action (for 7a). The results showed that compounds 7a and 7b were relatively safe for BV2 cells, but compound 7a interfered with Cryptococcus neoformans cell wall integrity by increasing the chitinase activity. Therefore, compound 7a was considered safe as an antifungal agent for animal cells. Three series of 1,5-benzothiazepine derivatives were synthesized and their antifungal activities were evaluated to determine the structure-activity relationships with respect to the antifungal activity of 2-ester-substituted 1,5-benzothiazepines. The effective antifungal compounds 7a and 7b were further studied for their antifungal activity, cytotoxicity and mechanism of action (for compound 7a). The results provided important information about this class of benzothiazepines. Copyright

Synthesis and evaluation of anticancer activity of some novel 6-aryl-2-(p-sulfamylphenyl)-pyridazin-3(2H)-ones

A series of novel pyridazinone derivatives bearing benzenesulfonamide moiety (2a-h) has been synthesized by the condensation of appropriate aroylacrylic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol. Five derivatives (2a, 2b, 2d, 2g and 2h) were evaluated for their anticancer activity toward human cancer cell lines by the National Cancer Institute. The 2h showed remarkable activity against SR (leukemia) and NCI-H522 (non-small cell lung) with a GI50 value of less than 0.1 μM. It also displayed good activity against leukemia (CCRF-CEM, HL-60 (TB), K-562, MOLT-4, RPMI-8226), non-small cell lung cancer (NCI-H460), colon (HCT-116, HCT-15, HT29, KMI2, SW-620), CNS (SF-295), melanoma (MALME-3M, M14, MDA-MB-435 SK-MEL-5), ovarian (OVCAR-3, NCI/ADR-RES) and breast (MCF7) cancer cell lines with a GI 50 less than 1.0 μM. The acute toxicity study of 2h indicated that it is well tolerated intra-peritoneally (400 mg/kg) by athymic nude mice. The 2h may possibly be used as lead compound for developing new anticancer agents.

Syntheses of 1,5-Benzothiazepines: Part II - Synthesis of 4-Aryl-2-carboxy-2,3-dihydro-1,5-benzothiazepines

β-Aroylacrylic acids (II) react with 2-aminothiophenols (I) in ethanol containing gl.acetic acid to give 4-aryl-2-carboxy-2,3-dihydro-1,5-benzothiazepines (VII).Their structures have been established by elemental analyses and spectral data (IR, PMR, 13C NMR and mass).