683-81-8Relevant academic research and scientific papers
Fluorinating agent and synthesis method thereof
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Paragraph 0054-0056, (2020/09/16)
The invention discloses a fluorinating agent, and also discloses a preparation method of the fluorinating agent, wherein an amide corresponding to the structural formula of the product reacts with a halogenating agent to obtain corresponding alpha, alpha-dihaloamine, and the alpha, alpha-dihaloamine reacts with a fluoride to obtain the corresponding fluorinating agent. The fluorinating agent has the advantages of being stable in storage and capable of fluorinating hydroxyl with high yield, the preparation method is simple, the adopted raw materials are easy to obtain, the synthesis yield is high, and the fluorinating efficiency of the obtained product is high.
Fluorination method of florfenicol intermediate cyclic compound oxazoline
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Paragraph 0023-0024, (2020/06/05)
The invention relates to a fluorination method of florfenicol intermediate cyclic compound oxazoline, and solves the technical problems that in the prior art, a fluorination method of florfenicol intermediate cyclic compound oxazoline is large in treatment difficulty and low in yield, causes a large amount of reagent waste and environmental pressure, and is not suitable for large-batch productionof florfenicol. The invention provides the fluorination method of the florfenicol intermediate cyclic compound oxazoline; a fluorinating agent is N,N-dimethyl difluoromethylamine; N,N-dimethylformamide (DMF) generated in the florfenicol intermediate cyclization compound oxazoline fluorination process can react with carbonyl fluoride again to prepare the fluorinating agent needed by the florfenicolintermediate cyclization compound oxazoline fluorination reaction again, regeneration of the fluorinating agent is achieved, the requirement for green chemical engineering is met, and economic benefits are remarkable. The method is widely applied to the technical field of medical intermediates.
Phosphorus(V) complexes with acyclic monoaminocarbene ligands via oxidative addition
B?ttcher, Tobias,Bassil, Bassem S.,Zhechkov, Lyuben,R?schenthaler, Gerd-Volker
supporting information, p. 5651 - 5653 (2013/07/04)
(Difluoroorganyl)dimethylamines, RCF2NMe2 (R = H, Ph, tBu), can be used as carbene precursors for phosphorus trifluoride in an oxidative addition reaction. By this method, complexes of sterically nondemanding asymmetric and acyclic c
Fluorinating reactants and process for their preparation
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Page 11, (2010/02/07)
alpha,alpha-Difluoroalkylamines (I) are new. Also new are mixtures (A) containing (a) a broader class of alpha,alpha-difluoroalkylamines (I'), (b) an aprotic tertiary amine having no fluoro atoms in the alpha-position relative to nitrogen and/or a N-heteroaromatic compound and (c) hydrogen fluoride; and some specific dichloro compound intermediates. alpha,alpha-Difluoroalkylamines of formula R1-CF2-NR2R3 (I) are new. R1 = H, 1-12C alkyl, ((2-12C) alkylene-O)n-(1-12C) alkyl, 4-15C aralkyl or 3-14C heteroaryl; n = 1-5; R2, R3 = 4-15C aralkyl or 1-12C alkyl; or R2 + R3 or R1 + R2 and/or R3 = group completing a 3-12C cyclic group; the compounds 1,1-difluoromethyl-N,N-dimethylamine, 1,1-difluoromethyl-N,N-diethylamine, 1,1-difluoromethyl-N,N-diisopropylamine and 1,1-difluoro-N,N-2-trimethyl-1-propanamine are excluded. Independent claims are included for: (a) new mixtures (A) comprising (a) alpha,alpha-difluoroalkylamines of formula R4-CF2-NR5R6 (I'), (b) at least one aprotic tertiary amine having no fluoro atoms in the alpha-position relative to the nitrogen and/or at least one N-heteroaromatic compound and (c) hydrogen fluoride; (b) the preparation of (I) and (A); and (c) the following new geminal dichloro compound intermediates: 1,1-dichloromethyl-N,N-dimethylamine, 1,1-dichloromethyl-N,N-diethylamine, 1,1-dichloromethyl-N,N-diisopropylamine, 1,1-dichloro-N,N-2-trimethyl-1-propanamine, 1,1-dichloro-N,N-2,2-tetramethyl-1-propanamine (VIa), N,N-diethyl-alpha,alpha-dichloro-2,2-dimethyl-1-propanamine, N-(1,1-dichloromethyl)-morpholine, 1,1-dichloro-N,N-dimethyl-phenylmethanamine, N,N-diethyl-alpha,alpha-dichloro-3-pyridyl-methanamine and 2,2-dichloro-1,3,3-trimethylpyrrolidine. R4 = H, 1-12C alkyl, ((2-12C) alkylene-O)n-(1-12C) alkyl, 3-14C aryl or NR7R8; n = 1-5; R7, R8 = 1-8C alkyl; or NR7R8 = 4-7 membered cyclic residue with a total of 3-12C; R5, R6 = 1-12C alkyl; or R5 + R6 or R4 + R5 and/or R6 = group completing a 4-12C cyclic group.
