- Preparation of enantiopure chiral amino- [D1]methyllithium compounds and determination of their micro- and macroscopic configurational stabilities
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Chiral amino-[D1]methyllithiums have been tested with regard to their microscopic and macroscopic configurational stabilities. The N-Boc-N-diethoxyphosphinyl-sub-stituted analogue immediately rearranged, showing complete retention of configuration at up t
- Kapeller, Dagmar C.,Hammerschmidt, Friedrich
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experimental part
p. 5729 - 5739
(2009/12/29)
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- Reactions of 1,2- and 1,3-amino-alcohols with imidate salts and with ortho esters
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ω-Hydroxy-N-substituted amidines have been shown to be the intermediates in the formation of 2-oxazolines and 5,6-dihydro-4H-1,3-oxazines from the reactions of imidates and 1,2- and 1,3-amino-alcohols respectively, 1,2- and 1,3-Amino-alcohols also react with ortho esters to give 2-oxazolines and 5,6-dihydro-4H-1,3-oxazines, but N-acylamino-alcohols give rise to oxazolidines with ortho esters.
- Butt, Mohammed I.,Neilson, Douglas G.,Watson, Kathleen M.,Zakir-Ullah
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p. 2328 - 2332
(2007/10/04)
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- Antimalarials. Synthesis and antimalarial activity of 1 (4 methoxycinnamoyl) 4 (5 phenyl 4 oxo 2 oxazolin 2 yl)piperazine and derivatives
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The preparation and activity against Plasmodium berghei of derivatives of 1 (4 methoxycinnamoyl) 4 (5 phenyl 4 oxo 2 oxazolin 2 yl)piperazine are described. Replacement of the cinnamoyl group was accomplished by acylation or alkylation of 1 (5 phenyl 4 oxo 2 oxazolin 2 yl)piperazine. Modifications of the 5 phenyl group were prepared either by a sequence of reactions involving mandelic ester pemoline piperazine pemoline or by the reaction of 5 aryl 2 thio 2,4 oxazolidinedione with piperazine or N substituted piperazines. In a similar manner, pemoline was allowed to react with N arylpiperazine, hexahydro 1H 1,4 diazepine, and 2,6 dimethylpiperazine to provide N arylpiperazine pemoline derivatives and variations in the piperazine moiety. Several compounds in which the 2 oxazolin 4 one ring was replaced with other heterocyclic rings were prepared as were several open chain analogs. Five compounds (three of them substituted in the para position of the 5 phenyl group and two N arylpiperazine pemoline derivatives) were found to be active against Plasmodium berghei. The remaining active compound possessed changes in the cinnamoyl group and substitution on the 5 phenyl group.
- Herrin,Pauvlik,Schuber,Geiszler
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p. 1216 - 1223
(2007/10/04)
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