- Method using amide ester to prepare diamine derivative
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The invention provides a method using amide ester to prepare a diamine derivative. The method is characterized in that ester groups in amide esters containing both amide and ester functional groups are substituted to prepare the diamine derivative, and one of the diamine groups of the diamine derivative is carboxylic acid amide reserved from the amide ester raw materials. The method is cheap in raw material, easy in raw material obtaining, low in catalyst use amount, simple in reaction conditions and high in product stereoselectivity.
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Paragraph 0064; 0083; 0084; 0085
(2018/10/19)
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- Syntheses of chiral β- And γ-amino ethers, morpholines, and their homologues via nucleophilic ring-opening of chiral activated aziridines and azetidines
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Figure Persented: Lewis acid catalyzed quaternary ammonium salt mediated highly regioselective ring-opening of chiral activated aziridines and azetidines with alcohols to nonracemic β- and γ-amino ethers has been developed. The reaction mainly proceeds vi
- Ghorai, Manas K.,Shukla, Dipti,Bhattacharyya, Aditya
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supporting information; scheme or table
p. 3740 - 3753
(2012/06/18)
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- MUSCARINIC AGONISTS
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The present invention relates to compounds of Formula (I): which are agonists of the M-1 muscarinic receptor.
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- Stereoselective Aldol Reaction with Chiral Secondary Acetamides
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The deprotonated acetamides 4a - c and 5a - c are added to prochiral carbonyl compounds.The influence of the solvent, of the reaction temperature, and of the enolate gegenion on the ratio of the isomeric products 8/9, 18/19, and 26/27, respectively, are studied.The highest degree of diastereoselectivity are observed, when the titanium enolate of the acetamide 4a or the threefold deprotonated N-acetyl-α-phenylglycinol (5a) is used.The diastereomers 18a - d, formed in excess in the addition of 5a to aldehydes, are isolated in pure from by a single recrystallization, and afford the enantiomerically pure β-hydroxy carboxylic acids 3a - d.Thereby, the chiral auxiliary, α-phenylglycinol (14), is recovered.
- Devant, Ralf,Braun, Manfred
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p. 2191 - 2207
(2007/10/02)
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- On Amino Acid Antagonists,IV.-Separation and Determination of the Configurations of the Stereoisomeric N-Acetyl-2-(2'-cyclohexenyl)glycines
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The D-(+)-(1-phenylethyl)amides 5 as well as the D-(-)-O-acetyl-α-phenylglycinolamides 7 of the title compounds were separated on silica gel into the four diastereomeric compounds.All attempts failed to hydrolyze 5 and 7 to the corresponding acids.In contrast the diastereomeric D-(-)-N-acetyl-α-phenylglycinol esters 10 which were separated on silica gel were hydrolysed to the optically active acids 3a-d.The absolute configurations at C-2 in 3 were determined by correlation with the saturated glycine derivatives of known stereochemistry.The relative configurationsand hence the absolute configurations at C-1' in 3a-d were deduced from the NMR- and CD-spectra and were confirmed by X-ray analysis of 3a.Only the amino acid 3b with the (2S,1'R)-configuration exhibits biological activity.
- Santoso, Sentot,Kemmer, Thorsten,Trowitzsch, Wolfram
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p. 642 - 657
(2007/10/02)
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