TL;DR: In this paper, the secondary amine SA (dimethylamine DMA, diethylamine DEA, pyrrolidine Pyr, piperidine Pip, morpholine Mor) to pentafluoropropene PFP gives rise to generation of mixtures of two products (1-dialkylamine-1, 3,3,3-3, 3-tetrafluorOPropene and N,N-dialkyl-1.
TL;DR: In this paper, a series of 3-(mono-, di-, trifluoro)methyl-substituted N-benzylpyrrolidinones 5a, c was synthesized by deoxyfluorination of corresponding 3-functionalized N-brenzyl pyrrolidsinones.
TL;DR: The reaction of polyfluorinated acids with the Ishikawa Reagent (FAR) in the presence of NaF gives 59-91% isolated yields of HF free polyflorinated acyl fluorides as mentioned in this paper.
TL;DR: In this paper, a chiral synthesis method of a special chloramphenicol broad-spectrum antibiotic florfenicol for animals is described, in which thioanisole used as the initial raw material is sequentially subjected to acylation, bromization, synthesis of substituent-group-containing azairidine, chiral catalytic reduction, oxidation reaction, fluorization ring-opening, deprotection and acylization reaction to obtain the qualified product which conforms to the requirements of Food and Drug Administration.
Abstract: The invention relates to a chiral synthesis method of a special chloramphenicol broad-spectrum antibiotic florfenicol for animals. In the invention, thioanisole used as the initial raw material is sequentially subjected to acylation, bromization, synthesis of substituent-group-containing azairidine, chiral catalytic reduction, oxidation reaction, fluorization ring-opening, deprotection and acylation reaction to obtain the qualified product which conforms to the requirements of Food and Drug Administration. The chiral catalytic reduction is implemented by carrying out hydrogenation reduction on [1-substituted-aziridiyl-2-yl][4-(methylthio)phenyl]ketone under the action of a synthetic catalyst trans-RuCl2[(R)-xylbinap][(S)-DPEN], to obtain [1-substituted-aziridiyl-2-yl][4-(methylthio)phenyl]methanol with high ee value and de value; and in addition, the fluorization uses cheap and accessible potassium fluoride as the fluorization reagent instead of the industrially common expensive Ishikawa reagent at present, thereby lowering the production cost.
TL;DR: In this article, a novel synthetic process of high-purity florfenicol was proposed, which consists of the following steps: by taking a compound D-threo form-2-(dichloromethyl)-4,5-dihydro-5-[p-(methylsulfonyl)phenyl]-4-oxazole methanol as an initial raw material, carrying out fluoro-substitution by using an Ishikawa reagent; crystallizing and purifying to obtain a high-Purity fluoro product (
Abstract: The invention provides a novel synthetic process of high-purity florfenicol The process comprises the following steps: by taking a compound D-threo form-2-(dichloromethyl)-4,5-dihydro-5-[p-(methylsulfonyl)phenyl]-4-oxazole methanol as an initial raw material, carrying out fluoro-substitution by using an Ishikawa reagent; crystallizing and purifying to obtain a high-purity fluoro product (4S,5S)-2-(dichloracetyl)-4-(methyl fluoride)-5-[4-(methylsulfonyl)phenyl]-4, 5-dihydrooxazole; and further carrying out a hydrolysis reaction directly on the high-purity fluoro product without being added into an organic solvent to directly obtain a high purity florfenicol product According to the production process, the fluoro intermediate product is crystallized and purified to obtain a high purity product by adopting a direct hydrolysis process without using the organic solvent, so that the novel synthetic method is simple in process operation, environmental friendly, high in product purity, few in impurity, free from solvent residue and low in cost