An optimized protocol for the multigram synthesis of 3-(trifluoromethyl) bicyclo [1.1. 1] pent-1-ylglycine (CF 3-Bpg)

…, NM Voievoda, S Afonin, AS Ulrich, IV Komarov

Index: Mykhailiuk, Pavel K.; Voievoda, Nataliia M.; Afonin, Sergii; Ulrich, Anne S.; Komarov, Igor V. Journal of Fluorine Chemistry, 2010 , vol. 131, # 2 p. 217 - 220

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Citation Number: 20

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, 100g of optically ...