- Preparation method of 3-nitro-4-fluorophenylacetate
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The invention discloses a method for preparing 3-nitro-4-fluorophenylacetate by using a microreactor, and belongs to the technical field of organic matter synthesis, the microreactor comprises precooling modules and a mixing module, and the method specifically comprises the following steps: (1) preparing raw materials: preparing a mixed solution of 4-fluorophenylacetate and concentrated sulfuric acid and a nitric acid solution; (2) pre-cooling: cooling the pre-cooling modules and the mixing module to a reaction temperature in advance, and then respectively adding the mixed solution of 4-fluorophenylacetate and concentrated sulfuric acid and the nitric acid solution into different pre-cooling modules; (3) mixing: after the raw materials are pre-cooled, adding the pre-cooled raw materials into the mixing module for mixing reaction; and (4) performing quenching and post-processing. The method provided by the invention can effectively control the heat release problem of the nitration reaction, and is high in safety; and the 3-nitro-4-fluorophenylacetate can be prepared with high selectivity, the conversion rate of the 4-fluorophenylacetate can reach 98.4%, and the selectivity can reach99: 1.
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Paragraph 0033-0040; 0052-0061
(2020/02/27)
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- Method for synthesizing 2-bromo-4-fluoro-5-aminoethyl phenylacetate
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The invention belongs to the technical field of preparation of intermediates of a dihydronaphthyridine compound, and particularly relates to a method for synthesizing 2-bromo-4-fluoro-5-aminoethyl phenylacetate. The method comprises the following steps: 1
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Paragraph 0036-0038; 0042-0044
(2020/03/09)
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- SUBSTITUTED HETEROCYCLIC ACETAMIDES AS KAPPA OPIOID RECEPTOR (KOR) AGONISTS
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The present invention relates to a series of substituted compounds having the general formula (I), including their ste reoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3. R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
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Page/Page column 59
(2013/09/26)
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- Synthesis of azide-fluoro-dehydrocoelenterazine analog as a photoaffinity-labeling probe and photolysis of azide-fluoro-coelenterazine
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A photosensitive azide-fluoro-dehydrocoelenterazine analog (Az-F-DCT) was synthesized, starting from 4-fluorophenylacetic acid, as a photoaffinity- labeling probe in order to analyze symplectin active site. To examine the photo-reactivity of Az-F-DCT, azi
- Kuse, Masaki,Doi, Issei,Kondo, Nobuhiro,Kageyama, Yukari,Isobe, Minoru
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p. 5754 - 5762
(2007/10/03)
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