- Bitopertin synthetic method and intermediate
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The present invention discloses a new synthesis method and intermediates of Bitopertin. According to the Bitopertin synthesis method, 5-methylsulfonyl-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]benzoic acid is adopted as a raw material, and continuous multi-step operations such as chlorination, acylation, deprotection, condensation and re-crystallization are subjected to performed to obtain the Bitopertin, wherein the intermediates in each step do not require further purification, and the total yield can achieve more than or equal to 80%.
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Paragraph 0061; 0064; 0065
(2018/03/26)
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- SYNTHESIS OF GLYT-1 INHIBITORS
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The present invention relates to a process for preparation of a compound of formula I wherein Het, R1, R2, R3, and n are as defined herein and pharmaceutically acceptable acid addition salts thereof, which comprises reacting a compound of formula 21 with a compound of formula 8 to obtain a compound of formula 11 and coupling the compound of formula 11 in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula 15 to obtain a compound of formula I.
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Page/Page column 6; 9
(2008/12/08)
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- Process for the preparation of fluorinated pyridine derivatives
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In accordance with a novel process, 2,3-difluoropyridines of formula I STR1 wherein X is halogen or trifluoromethyl, are prepared by diazotising a 3-amino-2-halopyridine of formula II STR2 wherein X is as defined for formula I and Y is bromine, chlorine or fluorine, in the presence of hydrogen fluroide, to give a 3-fluoro-2-halopyridine of formula III STR3 wherein X and Y are as defined for formula II, and treating resultant 3-fluoro-2-halopyridines of formula III, wherein Y is bromine or chlorine, with a fluorinating agent. The 2,3-difluoropyridines prepared by the novel process are valuable intermediates for the preparation of 2-[4-(3-fluoropyridin-2-yloxy)-phenoxy]propionic acid derivatives which are known as herbicides.
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- 2,3-difluoro-5-(trifluoromethyl)pyridine
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Novel 2,3-difluoro-5-(trifluoromethyl)pyridine is prepared by fluorinating 3-chloro-2-fluoro-5-(trifluoromethyl)pyridine under favorable conditions. The compound is useful as a chemical intermediate in the preparation of herbicides.
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- 2,3-Difluoro-5-(trifluoromethyl)pyridine and methods of making and using the same
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Novel 2,3-difluoro-5-(trifluoromethyl)pyridine is prepared by fluorinating 3-chloro-2-fluoro-5-(trifluoromethyl)pyridine under favorable conditions. The compound is useful as a chemical intermediate in the preparation of herbicides.
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