TOP > 外国特許検索 > METHOD OF MANUFACTURING TRIFLUOROMETHYL SUBSTITUTED SEMISQUARATE, METHOD OF MANUFACTURING TRIFLUOROMETHYL COMPOUND STARTING FROM TRIFLUOROMETHYL SUBSTITUTED SEMISQUARATE, AND TRIFLUOROMETHYL GROUP-CONTAINING COMPOUND

METHOD OF MANUFACTURING TRIFLUOROMETHYL SUBSTITUTED SEMISQUARATE, METHOD OF MANUFACTURING TRIFLUOROMETHYL COMPOUND STARTING FROM TRIFLUOROMETHYL SUBSTITUTED SEMISQUARATE, AND TRIFLUOROMETHYL GROUP-CONTAINING COMPOUND コモンズ

外国特許コード F160008860
整理番号 NU-659
掲載日 2016年9月28日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2016JP066988
国際公開番号 WO 2016199789
国際出願日 平成28年6月8日(2016.6.8)
国際公開日 平成28年12月15日(2016.12.15)
優先権データ
  • 特願2015-116151 (2015.6.8) JP
  • 特願2015-150175 (2015.7.29) JP
発明の名称 (英語) METHOD OF MANUFACTURING TRIFLUOROMETHYL SUBSTITUTED SEMISQUARATE, METHOD OF MANUFACTURING TRIFLUOROMETHYL COMPOUND STARTING FROM TRIFLUOROMETHYL SUBSTITUTED SEMISQUARATE, AND TRIFLUOROMETHYL GROUP-CONTAINING COMPOUND コモンズ
発明の概要(英語) The present invention addresses the problem of efficiently synthesizing a trifluoromethyl substituted semisquarate in a short process, in order to manufacture trifluoromethyl compounds with various functionalities. A method was developed of synthesizing a trifluoromethyl substituted semisquarate with squarate as a starting material, in the two steps of a trifluoromethylation reaction and an allyl alcohol transfer reaction. Furthermore, a method was established of manufacturing trifluoromethyl compounds with various functionalities starting from a trifluoromethyl substituted semisquarate.
従来技術、競合技術の概要(英語) BACKGROUND ART
Fluorine-containing polymers, carbon - fluorine bonds firmly for known to have high chemical stability and, as well as a medicament, functional material, such as used in the region of the pesticide. In particular, in medicine is, era Fludrocortisone is 1950, 10 - fold higher Cortisone as compared to the found to have anti-inflammatory effect (non-patent document 1, 2) since, a number of compounds have been synthesized and, are currently used in chemotherapy such as 5 - fluorouracil, fluorine-containing advanced the development of a drug (non-patent document 3, 4).
Pharmaceutical is, by introducing fluorine, polarization effects, mimic effect, block effect, referred to as hydrophobic enhancement effect which effect is known to result in (non-patent document 5, 6). Polarity effects and is, by the influence of strong electronegativity of fluorine such as the oxidation reaction or that are resistant to electrophilic reaction, to obtain a stronger interaction with protein effect. Mimic effect is, then a small radius of fluorine atom is a hydrogen atom from the atom, they are not identified and the in vivo behavior similar to the effect. Is a block effect, where the spread of the electron orbitals of the carbon fluorine close to that of, for carbon - fluorine bonds are strong, substitution reaction and the reduction, to suppress oxidative metabolism in vivo, in a stabilizing effect. In addition, oleophilic and hydrophobic enhancement effect may be acquired, in vivo absorption, such as the transportation to provide variance in the effect. Further, as a combined effect of these therapeutic action or drug absorption enhancement effect lasting effect, it is possible to improve the effect of selected known as fluorine. A high effect from these, the fluorine-containing pharmaceutical agents, to commercially available pharmaceutical products increased to 14%.
Fluorine-containing compound, and has the effect as described above, in the development of pharmaceuticals and the like, the synthesis of a fluorinated organic compound so as to play a significant role has been. Among them, aromatic trifluoromethyl compounds (Ar-CF3) is often used in medicine.
Current, a trifluoromethyl group introduction, as shown in Fig. 2 mainly divided into two by a method which is carried out. Such as trifluoroacetic acid and derivatives, compounds that possess a trifluoromethyl group, synthesis of the polymer building block method aimed at target structures (non-patent document 3, 4, 7 -11), directly introduced into the molecular skeleton unit and trifluoromethyl trifluoromethyl a method in which a direct (non-patent document 12-21, Patent Document 1) is.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
  • 発明者(英語)
  • YAMAMOTO Yoshihiko
  • KUROHARA Takashi
  • SHIBUYA Masatoshi
国際特許分類(IPC)
指定国 National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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