- Chemically synthesized heterocyclic insecticide intermediate and preparation method thereof
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The invention discloses a chemically synthesized heterocyclic insecticide intermediate and a preparation method thereof. The chemically synthesized heterocyclic insecticide intermediate is prepared from the following raw materials in parts by weight: 100 to 150 parts of distilled water, 65 to 90 parts of hydroxylamine sulphate, 80 to 100 parts of ammonia water, 20 to 30 parts of acetaldehyde, 30 to 40 parts of sodium hydroxide, 35 to 50 parts of potassium permanganate, 45 to 60 parts of concentrated hydrochloric acid and 15 to 20 parts of saturated salt water. According to the chemically synthesized heterocyclic insecticide intermediate, the preparation method is relatively mature and a technology is relatively simple; a production progress, and the dosage ratio of each index are convenient to control and the raw materials for synthesizing are materials which are common in the market and are cheap and easy to obtain; the yield of the prepared intermediate methylthioacetaldoxime reaches 75 percent to 80 percent and is much higher than the average yield of an existing market; the medicinal effect is improved; the intermediate methylthioacetaldoxime has stable chemical properties and does not have viscous decomposition or deterioration problems and the like at room temperature, and the economic benefits are improved.
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Paragraph 0043
(2017/11/29)
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- ANTIBIOTIC COMPOSITIONS
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The present disclosure relates to compounds having antimicrobial activity, compositions comprising said compounds in combination with β-lactam antibiotics, and methods of using the compounds and compositions.
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Page/Page column 0158
(2017/09/02)
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- MACROCYCLIC DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
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Page/Page column 231-232
(2013/09/26)
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- Structure-Activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating mycobacterium tuberculosis
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Tuberculosis (TB) remains as a global pandemic that is aggravated by a lack of health care, the spread of HIV, and the emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDRTB) strains. New anti-TB drugs are urgently required to shorten the long 6-12 month treatment regimen and to battle drug-resistant Mtb strains. We have identified several potent quinoline-based anti-TB compounds, bearing an isoxazole containing side-chain. The most potent compounds, 7g and 13, exhibited submicromolar activity against the replicating bacteria (R-TB), with minimum inhibitory concentrations (MICs) of 0.77 and 0.95 μM, respectively. In general, these compounds also had micromolar activity against the nonreplicating persistent bacteria (NRP-TB) and did not show toxicity on Vero cells up to 128 μM concentration. Compounds 7g and 13 were shown to retain their anti-TB activity against rifampin, isoniazid, and streptomycin resistant Mtb strains. The results suggest that quinoline-isoxazole-based anti-TB compounds are promising leads for new TB drug development.
- Lilienkampf, Annamaria,Jialin, Mao,Baojie, Wan,Yuehong, Wang,Franzblau, Scott G.,Kozikowski, Alan P.
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supporting information; experimental part
p. 2109 - 2118
(2009/12/31)
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- 3-(Arylthiomethyl)isoxazole-4,5-dicarboxamides: Chemoselective Nucleophilic Chemistry and Insecticidal Activity
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A collection of 91 3-(arylthiomethyl)isoxazole-4,5-dicarboxamides was prepared starting from dimethyl 3-(chloromethyl)isoxazole-4,5-dicarboxylate. The thioether moieties in these compounds were subsequently oxidized to give the corresponding 3-(arylsulfonylmethyl)isoxazole-4,5-dicarboxamides. By carefully controlling stoichiometry and reaction conditions, the C4 and C5 carbomethoxy groups could be differentially derivatized to carboxamides. A total of 182 trisubstituted isoxazoles are reported and deposited in the National Institutes of Health Molecular Repository; an 80 compound subset was evaluated for insecticidal activity.
- Yu, Gui J.,Iwamoto, Satori,Robins, Lori I.,Fettinger, James C.,Sparks, Thomas C.,Lorsbach, Beth A.,Kurth, Mark J.
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scheme or table
p. 7422 - 7426
(2010/07/08)
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- Imidazopyridines for the treatment of neurological disorders
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Corticotropin releasing factor (CRF) antagonists of formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
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Example 7409
(2010/01/31)
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