- Factors affecting the efficiency and stereoselectivity of α-amino acid synthesis by the Petasis reaction
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The use of chiral secondary amines containing only one branched substituent has been shown to give optimal yields and stereoselectivities in the preparation of α-amino acids using the Petasis reaction. While the use of chiral primary amines generally give
- Southwood, Timothy J.,Curry, Merril C.,Hutton, Craig A.
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Read Online
- Novel trifluoromethyl sydnone derivatives: Design, synthesis and fungicidal activity
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Crop pathogens reduce the yield and quality of agricultural production. The development of new fungicides will help to sustain this protection and overcome fungicide resistance. Sydnone is a kind of mesoionic, which has a wide range of biological activiti
- Du, Shaoqing,Hu, Xueping,Shao, Xusheng,Qian, Xuhong
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supporting information
(2021/05/31)
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- ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITION THEREOF
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The present invention relates to alkaloid aminoester derivatives acting as muscarinic receptor antagonists, processes for their preparation, compositions comprising them and therapeutic uses thereof.
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Page/Page column 46
(2012/01/13)
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- ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITION THEREOF
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The present invention relates to alkaloid aminoester compounds which act as muscarinic receptor antagonists, processes for the preparation of such a compound, compositions which contain such a compound, and therapeutic uses of such a compound.
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- ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITION THEREOF
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The present invention relates to alkaloid aminoester derivatives acting as muscarinic receptor antagonists, to methods of preparing such derivatives, to compositions comprising them and therapeutic use thereof.
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Page/Page column 66-67
(2010/07/09)
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- A facile synthesis of substituted phenylglycines
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A convenient scaleable process for the preparation of substituted phenylglycines 2 by a modified Strecker reaction is described. Bisulfite- mediated addition of benzylamine and cyanide anion to substituted benzaldehydes 3 gave the aminonitriles 4 which were hydrolysed in two steps to the N-protected amino acid 1. Debenzylation using catalytic transfer hydrogenation gave the title compounds in good yield.
- Davies, Antony J.,Ashwood, Michael S.,Cottrell, Ian F.
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p. 1095 - 1102
(2007/10/03)
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- Phosphatase inhibitors. III. Benzylaminophosphonic acids as potent inhibitors of human prostatic acid phosphatase
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Further investigation of the structural requirements of a series of benzylphosphonic acid inhibitors of human prostatic acid phosphatase has led to the highly potent series of α-aminobenzylphosphonic acids. The α-benzylaminobenzylphosphonic acid, with an IC50 = 4 nM, exhibited a 3500-fold improvement in potency over the carbon analogue, α-phenylethyl. The enhanced potency may be due to a combination of four favorable interactions including those with the phosphate binding region, the presence the hydrophobic moieties of the benzylamino and phenylphosphonic acid, and a rigid conformer produced by an internal salt bridge between the phosphonate and the α-amino group. Replacement of the phosphonic acid moiety with a phosphinic or carboxylic acid as well as deletion of the benzyl substitution on the α-amino group led to great reductions in potency.
- Beers, Scott A.,Schwender, Charles F.,Loughney, Deborah A.,Malloy, Elizabeth,Demarest, Keith,Jordan, Jerold
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p. 1693 - 1701
(2007/10/03)
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- Reaction of Sydnones with Oxygen
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The reaction of 3-benzyl- and 3-(p-chlorobenzyl)-4-phenylsydnones (1a and 1b) and of 3-benzylsydnone (1c) with oxygen at room temperature in the dark is described.Possible rationalizations for the formation of the products obtained are suggested.
- Nakajima, Masayuki,Anselme, Jean-Pierre
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p. 1444 - 1448
(2007/10/02)
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