- 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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- SPIRO-INDOLINES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION (RSV)
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Benzimidazoles of formula (I): wherein: one of X and Y is an N atom or a substituted C atom, and the other is CH; L is a single bond, C1-3 alkylene, C2-3 alkenylene or C2-3 alkynylene; R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, 3- to 10-membered cycloalkyl, 5- to 10-membered heterocyclyl or 5- to 12- membered heteroaryl, each of which is unsubstituted or substituted; Z is halo, C1-6 haloalkyl, nitro, -CN, -N(R2)2, -OR2, -SR2, -S(=0)R2, or -S(=0)2R2; each R2 is independently hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; and m is 0 or 1; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
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Page/Page column 29; 30
(2016/05/02)
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- Discovery of novel (4-piperidinyl)-piperazines as potent and orally active acetyl-CoA carboxylase 1/2 non-selective inhibitors: F-Boc and triF-Boc groups are acid-stable bioisosteres for the Boc group
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Novel (4-piperidinyl)-piperazine derivatives were synthesized and evaluated as ACC1/2 non-selective inhibitors. Optimization of the substituents on the nitrogen of the piperidine ring led to the identification of the fluorine substituted tert-butoxycarbonyl group. Advanced analog, 1,1,1-trifluoro-2- methylpropan-2-yl 4-{4-[(2-amino-6-methyl-1-benzothiophen-3-yl)carbonyl] piperazin-1-yl}piperidine-1-carboxylate (12c) showed potent inhibitory activities in enzyme-assay and cell-based assays. Compound 12c also exhibited reduction of hepatic de novo fatty acid synthesis in rats after oral administration.
- Chonan, Tomomichi,Wakasugi, Daisuke,Yamamoto, Daisuke,Yashiro, Miyoko,Oi, Takahiro,Tanaka, Hiroaki,Ohoka-Sugita, Ayumi,Io, Fusayo,Koretsune, Hiroko,Hiratate, Akira
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supporting information; experimental part
p. 1580 - 1593
(2011/04/17)
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- CARBOXYLIC ACID COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
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A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.
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Page/Page column 43
(2008/06/13)
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