Synthetic method of monoamino inhibitor intermediate monoethyl 2-acetylamino-2-benzylmalonate
The invention discloses a synthetic method of a monoamino inhibitor intermediate monoethyl 2-acetylamino-2-benzylmalonate. The method comprises the following steps: 1, carrying out amino protection on a compound I diethyl aminomalonate and di-tert-butyl d
-
(2017/09/01)
Towards a universal organocatalyst for the synthesis of enantioenriched phenylalanine derivatives by enantioselective decarboxylative protonation
Access to enantioenriched non-proteogenic phenylalanine derivatives is described using the enantioselective decarboxylative protonation reaction of amidohemimalonate esters catalysed by various cinchona-based compounds. This study compares the catalytic efficiency as well as the enantioselectivity induced by three types of common organocatalysts, namely thioureas, squaramides and bis-cinchona squaramides. One of the main outcome of this work is the observation of a significant influence of the N-protecting group of the hemimalonate on its interaction with the catalyst. This methodology carried out under mild conditions exhibits good substrate scope and functional group tolerance. A substoichiometric amount of catalyst can also be used in certain cases while affording good yields and selectivities.
Pigeaux, Morgane,Laporte, Romain,Harrowven, David C.,Baudoux, Jér?me,Rouden, Jacques
supporting information
p. 4599 - 4603
(2016/09/23)
More Articles about upstream products of 59223-84-6