- Ring opening reactions of cyclic sulfamidates. Synthesis of β-fluoroaryl alanines and derivatives of 4,4-difluoroglutamic acid
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Ring opening reactions of 1 with copper complex formed between Cu, TMEDA and BrCF2CO2Et lead to optically active 4,4-difluoroglutamic acid derivatives 11a-d in moderate yields. Reaction of cyclic sulfamidates 1 with fluoro substituted arylmagnesium chlorides proceed via copper catalyzed 1,4-addition of Grignard reagent to dehydroalanine 2, formed in situ. Fluorinated organoznic derivatives were unreactive towards 1 regardless of the reaction conditions; instead product of reaction of 1 with DMF was isolated.
- Bolek, Sylwia,Ignatowska, Jolanta
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- Preparation method of 2, 2-difluoroacetamide derivative
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The invention discloses a preparation method of a 2,2-difluoroacetamide derivative. The preparation method is characterized in that a 2,2-dichloroacetamide derivative is subjected to potassium fluoride fluorination under the action of a catalyst N-[di(diethylamino)methylene]-N-ethyl-ethane ammonium halide and an organic solvent to generate the 2,2-difluoroacetamide derivative. The preparation method of the 2,2-difluoroacetamide derivative disclosed by the invention is simple in production process and high in yield, the catalyst can be repeatedly used, the production cost can be effectively reduced, and the preparation method is suitable for large-scale industrial production.
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Paragraph 0036-0038
(2020/05/05)
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- Substituted Nitrogen Heterocycles and Synthesis and Uses Thereof
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The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.
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Page/Page column 27-28
(2009/10/06)
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