- Pyridineacetamide derivative serving as CDK inhibitor, and preparation method and application thereof
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The invention belongs to the technical field of pyridineacetamide derivatives, and particularly relates to a pyridineacetamide derivative serving as a CDK inhibitor and a preparation method and application of the pyridine acetamide derivative. The pyridineacetamide derivative shows excellent CDK9/CDK7 enzyme inhibitory activity, and can be used for preparing drugs used for treating cancers, especially hematologic cancers including acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, follicular lymphoma and the like and solid tumors such as breast cancer, prostate cancer, ovarian cancer, hepatocellular carcinoma, pancreatic cancer, kidney cancer, stomach cancer, colorectal cancer, lung cancer and the like.
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Paragraph 0292-0296
(2021/07/28)
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- Neuropeptide Y antagonists
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The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
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Page column 23-24
(2010/02/05)
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- Microwave-assisted rapid hydrolysis and preparation of thioamides by Willgerodt-Kindler reaction
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Aldehydes and aryl alkyl ketones were efficiently transformed to thioamides with the same number of carbon atoms via Willgerodt-Kindler reaction under microwave irradiation in solvent-free conditions. The thioamides obtained were hydrolyzed to corresponding carboxylic acids with microwave dielectric heating in one minute. Both reactions are very fast and the yields are excellent.
- Matloubi Moghaddam,Ghaffarzadeh
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p. 317 - 321
(2007/10/03)
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- Enantio- and diastereoselective synthesis of all four possible stereoisomers of 2-(phenylhydroxymethyl)quinuclidine
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An enantio- and diastereoselective synthesis of all four possible stereoisomers of 2-(phenylhydroxymethyl)quinuclidine is reported. Key steps involve the use of the Sharpless dihydroxylation protocol to induce asymmetry, and stereodivergent cyclisations of the resulting diol to form the quinuclidine ring.
- Lygo, Barry,Crosby, John,Lowdon, Terence R.,Wainwright, Philip G.
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p. 2343 - 2346
(2007/10/03)
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- Enhancement of the enantioselectivity of penicillin G acylase from E. coli by 'substrate tuning'
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The efficiency of penicillin G acylase catalyzed transformations is enhanced significantly with respect to reaction velocity, and in particular, stereoselectivity by appropriate 'substrate tuning', i.e. by the introduction of a nitrogen atom into the part of the substrates which is recognized by the enzyme.
- Pohl,Waldmann
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p. 2963 - 2966
(2007/10/02)
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- Degenerate Transesterification of 3,5-Dimethylphenolate/3,5-Dimethylphenyl Esters in Weakly Polar, Aprotic Solvents. Reactions of Aggregates and Complex-Induced Proximity Effects
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The rates of exchange of the 3,5-dimethylphenolate ion between lithium 3,5-dimethylphenolate-d6 and a series of 3,5-dimethylphenyl esters have been determined in the weakly polar, aprotic solvents dioxolane, dimethoxyethane (DME), tetrahydrofuran (THF), and pyridine. The esters include the propionate, butyrate, methoxyacctate, β-methoxypropionate, 4-methoxybutyrate, 2-tetrahydrofuroate, 2-furoate, (N,N-dimethylamino)acetate, (methylthio)acetate, 2- and 4-pyridine-carboxylates, 2-pyridylacetate, 4-pyridylacetate, phenylacetate, andp-methoxy-,p-chloro-, and p-(trifluoromethyl)phenylacetates. The rates and kinetic orders of the reactions of 3,5-dimethylphenyl propionate in various solvents at 35°C gave the following second-order rate constants (104k2, L mol-1 sec-1) for the following major aggregate species: THF tetramer, 6.5; DME tetramer, 3.3 (40°C); dioxolane, 13, hexamer, 71; pyridine tetramer, 2.2, dimer, 29. For 3,5-dimethylphenyl β-methoxypropionate, the order of reactivity is dioxolane > DME > THF. These results are interpreted in terms of a preequilibrium in which a solvent on lithium in the tetramer is replaced by the ester. The rates of transesterification have been compared with the rates of hydrolysis in 30% aqueous ethanol for the above series of esters. Those esters that have a second Lewis base center proximal to the ester function show significantly increased reactivity in transesterification, which is attributed to a complex-induced proximity effect.
- Jackman,Petrei,Smith
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p. 3451 - 3458
(2007/10/02)
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- Solvent dependence of oxygen isotope effects on the decarboxylation of 4-pyridylacetic acid
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Oxygen isotope effects on the decarboxylation of 4-pyridylacetic acid have been measured by the remote-label technique. The isotope effect varies from k16/k18 = 0.995 per oxygen in 25% dioxane to 1.003 in 75% dioxane. The isotope effect reflects three contributions: An inverse isotope effect of 0.98-0.99 due to the change in carbon-oxygen bond order on going from ground state to transition state, an effect of 1.01-1.02 due to desolvation of the carboxyl group, and an effect of approximately 1.01 due to the acid-base equilibrium of the carboxyl group. Thus, oxygen isotope effects on decarboxylation should be a useful probe for carboxyl desolvation in enzymatic decarboxylations.
- Headley, George W.,O'Leary, Marion H.
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p. 1894 - 1896
(2007/10/02)
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- GAS-PHASE REPLACEMENT ?0 SUBSTITUENT CONSTANTS OF HETEROARYL GROUPS
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Hammett replacement ?0 substituent constants of pyridyl, thienyl, and furyl groups are reported for the first time from gas-phase eliminations of their t-butyl and isopropyl heteroarylcarboxylate esters.
- Al-Awadi, Nouria A.,Al-Bashir, Rasha F.,ElDusouqui, Osman M. E.
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p. 1699 - 1702
(2007/10/02)
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