Title of article
An optimized protocol for the multigram synthesis of 3-(trifluoromethyl)bicyclo[1.1.1]pent-1-ylglycine (CF3-Bpg)
Author/Authors
Pavel K. Mykhailiuk، نويسنده , , Pavel K. and Voievoda، نويسنده , , Nataliia M. and Afonin، نويسنده , , Sergii and Ulrich، نويسنده , , Anne S. and Komarov، نويسنده , , Igor V.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2010
Pages
4
From page
217
To page
220
Abstract
An optimized procedure for the multigram synthesis of 3-(trifluoromethyl)bicyclo[1.1.1]pent-1-ylglycine (CF3-Bpg) has been developed. The overall yield of the synthesis for the optimized up-scaling was increased from 35% to 53%. Moreover, conditions for separating the key isomeric aminonitriles 7 and 8 by crystallization were found, which greatly facilitated the isolation of 8 on a multigram scale. Following this optimized protocol, 100 g of optically pure CF3-Bpg have been synthesized.
Keywords
Large-scale synthesis , Conformational rigidity , fluorine , amino acids
Journal title
Journal of Fluorine Chemistry
Serial Year
2010
Journal title
Journal of Fluorine Chemistry
Record number
1610796
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