- Efficient access to (1H)-isoindolin-1-one-3-carboxylic acid derivatives by orthopalladation and carbonylation of methyl arylglycinate substrates
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The orthopalladation of methyl arylglycinate derivatives has been studied. The reaction proceeds efficiently for different electron-withdrawing and electron-releasing substituents at the aryl ring. The carbonylation of the orthopalladated complexes affords, in a single step, substituted (1H)-isoindolin-1-one-3-carboxylates. These compounds constitute valuable synthetic intermediates and can be transformed diastereoselectively into octahydroisoindole-1-carboxylic acid derivatives, an important scaffold in the synthesis of many biologically active compounds.
- Nieto, Sonia,Sayago, Francisco J.,Laborda, Pedro,Soler, Tatiana,Cativiela, Carlos,Urriolabeitia, Esteban P.
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experimental part
p. 4185 - 4191
(2011/07/08)
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- SPIRO-CONDENSED IMIDAZOLONE DERIVATIVES INHIBITING THE GLYCINE TRANSPORTER
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Compounds of formula (I) and salts thereof are provided: formula (I), wherein the groups are as defined in the specification. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
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Page/Page column 44-45
(2009/04/25)
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- Chemistry of unprotected amino acids in aqueous solution: Direct bromination of aromatic amino acids with bromoisocyanuric acid sodium salt under strong acidic condition
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Brominations of unprotected aromatic amino acids such as phenylalanine, tyrosine, and glycine, with bromoisocyanuric acid mono sodium salt (BICA-Na) were conducted in 60% aq. H2SO4 at 0°C to give a mixture of mono-brominated products in good yield. Unexpectedly, meta-bromophenylglycine was obtained as main product accompanied by ortho- and para-substituted products, while phenylalanine gave only ortho- and para-substituted products. Bromination of 2-phenylethylamine or benzylamine showed a tendency similar to the corresponding amino acids.
- Yokoyama, Yuusaku,Yamaguchi, Tomotsugu,Sato, Masanori,Kobayashi, Eri,Murakami, Yasuoki,Okuno, Hiroaki
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p. 1715 - 1719
(2007/10/03)
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- Carboxylic acid amides having antithrombotic activity
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Compounds with antithrombotic activity and factor Xa-inhibiting activity of the general formula: Exemplary are: (1) (L)-2-(5-carbamimidoyl-2-hydroxy-phenyl)-N-[3-methyl-4-(2-aminocarbonyl-pyrrolidin-1-yl-carbonyl)-phenyl]-acetamide, (2) 2-(5-carbamimidoyl
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- Synthesis of Antiproteolytically Active Nα-Arylsulphonylated Amidinophenylglycinamides
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Several Nα-arylsulphonylated p- and m-amidinophenylglycinamides were prepared for the purpose of testing their efficacy as serine proteinase inhibitors.These compounds were obtained from the bromophenylhydantoins 1 and 2 via the bromophenylglycines 3 and
- Wagner, G.,Voigt, B.,Lischke, Ingrid
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p. 467 - 470
(2007/10/02)
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