861968-39-0Relevant academic research and scientific papers
waylen apperception HIV reverse transcriptase inhibitors in accordance with the law of the process for the asymmetric synthesis of one-pot synthesis (by machine translation)
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Paragraph 0140; 0141; 0142, (2016/10/07)
The invention relates to a novel one pot method asymmetric synthesis process of a (S)-6-chlorine-4-cylopropyl ethylnen-4-trifluoromethyl-1,4-dihydro-2H-1,3-benzoxazine-2-ketone (Efavirenz) compound, the compound can be used as an reverse transcriptase inhibitor for human immunodeficiency virus (HIV). The invention also relates to a novel aminoalcohol ligand used for the process.
Chiral tertiary amine/L-proline cocatalyzed enantioselective Morita-Baylis-Hillman (MBH) reaction
Tang, Hongying,Zhao, Guofeng,Zhou, Zhenghong,Gao, Peng,He, Liangnian,Tang, Chuchi
, p. 126 - 135 (2008/09/18)
Four types of chiral amines have been synthesized starting from readily available chiral sources. These chiral amines in combination with L-proline have been found to be efficient cocatalysts for the asymmetric Morita-Baylis-Hillman (MBH) reaction between methyl vinyl ketone (MVK) and aromatic aldehydes. The corresponding adducts were formed in reasonable chemical yields and with good enantioselectivities (up to 83 % ee). Moreover, parallel cocatalytic reactions with the two enantiomers of chiral amine 4 and L-proline revealed that it is the proline stereochemistry that determines the configuration of the newly formed chiral center. In addition, the existence of the free hydroxy group in amine 4a enhanced the enantioselectivity of the reaction. Based on these findings, a plausible mechanism for this cocatalytic MBH reaction has been proposed. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
AN AMINO ALCOHOL LIGAND AND ITS USE IN PREPARATION OF CHIRAL PROPARGLIC TERTIARY ALKOHOLS AND TERTIARY AMINES VIA ENANTIOSELECTIVE ADDITON REACTION
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Page/Page column 12, (2010/11/08)
The invention disclosed a new process of asymmetric alkynylation of ketone or ketimine, involving the chiral ligand-mediated asymmetric addition of zinc or copper acetylide to a trifluoromethyl ketone or ketimine intermediate to give a chiral tertiary pro
