- Asymmetric synthesis of Boc-β2-homophenylglycine
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Enantiomerically pure Boc-β2-homophenylglycine has been prepared in five steps starting from Oppolzer's sultam. The key step of this route is the acylation of metalated phenylacetonitrile with sultam carbonyl chloride. Subsequent reactions (reduction, N-Boc protection, oxidation of the Boc- amino alcohol) led to Boc-(S)-β2-HPhg starting from (+)-sultam.
- Ponsinet, Rachel,Chassaing, Gerard,Lavielle, Solange
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- Copper-catalyzed borylative aminomethylation of C-C double and triple bonds withN,O-acetal
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A copper-catalyzed borylaminomethylation of multiple carbon-carbon bonds withN,O-acetal and bis(pinacolato)diboron has been disclosed that offers efficient and expedient access to γ-amino boronates. The products contain a valuable amine and boronate, whic
- Qiu, Xianfan,Xu, Liugen,Wang, Shuxia,Dai, Ying,Feng, Yunqiu,Gong, Chang,Tao, Chuanzhou
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p. 3279 - 3282
(2021/04/07)
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- A Heterodinuclear asymmetric catalyst for conjugate additions of α-hydroxyketones to β-substituted nitroalkenes
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(Chemical Equation Presented) The bis-ProPhenol ligand was designed to facilitate formation of hetereodinuclear complexes based upon the large difference in pKa of the one phenolic OH group to the tertiary OH groups. In exploring the first exam
- Trost, Barry M.,Hisaindee, Soleiman
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p. 6003 - 6005
(2007/10/03)
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- Nucleoside derivatives for library preparation
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Nucleoside derivatives as building blocks for templated libraries are described.
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- Palladium-catalysed asymmetric allylic substitution: Synthesis of α- and β-amino acids
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Methodology has been established for the formation of enantiomerically enriched α-amino acids using palladium-catalysed allylic amination. The formation of enantiomerically enriched allylamines has been achieved with high enantioselectivity. Oxidative cleavage of the allylamines provides arylglycine and glutamic acid derivatives. Additionally, enantiomerically enriched β-amino acids have been prepared in high enantiomeric excess. Palladium-catalysed asymmetric allylic substitution is used as the key synthetic transformation.
- Bower, Justin F.,Jumnah, Roshan,Williams, Andrew C.,Williams, Jonathan M. J.
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p. 1411 - 1420
(2007/10/03)
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- Acetic acid derivatives
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Acetic acid derivatives of formula and hydrates, solvates and physiologically acceptable salts thereof are useful to inhibit the binding of adhesive proteins to blood platelets and also to inhibit blood platelet aggregation and cell-cell adhesion.
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- Isoindolone derivatives, their preparation and the pharmaceutical compositions containing them
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This invention relates to isoindolone derivatives of general formula (I) in which the radicals R are hydrogen atoms or together form a bond, the symbols R'' are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, X is an oxygen or sulphur atom or a radical N--R 3, R 3 being H, optionally substituted alkyl or dialkylamino, R 1 is optionally substituted phenyl or cyclohexadienyl, naphthyl or a heterocycle and R 2 is H, halogen, OH, alkyl, amionoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, carboxyl, optionally substituted alkoxycarbonyl, benzyloxycarbonyl, amino or acylamino, in their (3aR,7aR) forms or in the (3aRS,7aRS) form or their mixtures, and if appropriate their salts where such exist, and their preparation.The new derivatives according to the invention are particularly valuable as antagonists of substance P. STR1
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