- Synthesis and conformational analysis of 1,3,2-diazaphosphorino[6,1-a] isoquinolines, a new ring system
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Through ring-closure reactions of N- or 1′-substituted 1-(2′-aminoethyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines (5a-e) with phenylphosphonyl dichloride, 1- or 3-substituted 4-phenyl-1,3,4,6,7,11b- tetrahydro-2H-1,3,2-diazaphosphorino[6,1-a]isoquinolin-4-one diastereomers (7a-e and 8a-c,e), the first representatives of a new ring system, were prepared. The diastereomeric ratios in the cyclizations and the conformer (A-E) populations of the nitrogen-bridged tricyclic systems (7 and 8) were strongly influenced by the N- and 1′-substituents of the starting diamines. The conformational analysis of compounds 7 and 8 was performed by 1H, 13C and 31P NMR methods.
- Zalán, Zita,Martinek, Tamás A.,Lázár, László,Fül?p, Ferenc
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p. 9117 - 9125
(2007/10/03)
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- Enantioselective preparation of 2-aminomethyl carboxylic acid derivatives: Solving the β2-amino acid problem with the chiral auxiliary 4-isopropyl-5,5-diphenyloxazolidin-2-one (DIOZ)
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Multigram amounts of suitably protected β2-amino acids with 17 of the 20 proteinogenic side chains are prepared by diastereoselective reactions of Li, B, or Ti enolates of the corresponding 3-acyl-4-isopropyl-5,5-diphenyloxazolidin-2-ones (acyl-DIOZ; 1) with appropriate electrophiles (amidomethylation, hydroxyalkylation, (benzyloxycarbonyl)methylation) in yields of 55-90% and with diastereoselectivities of 80 to > 97% (Scheme). The primary products 2-8 thus obtained are converted to protected β2-amino acids by standard procedures (Table 1). Many of the DIOZ derivatives are highly crystalline compounds (31 X-ray crystal structures in Table 2). The chiral auxiliary DIOZ, readily prepared in either enantiomeric form, is recovered with high yield.
- Seebach, Dieter,Schaeffer, Laurent,Gessier, Francois,Bindschaedler, Pascal,Jaeger, Corinna,Josien, Delphine,Kopp, Sascha,Lelais, Gerald,Mahajan, Yogesh R.,Micuch, Peter,Sebesta, Radovan,Schweizer, Bernd W.
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p. 1852 - 1861
(2007/10/03)
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- METHODS OF TREATING ALZHEIMER'S DISEASE USING ARYL ALKANOIC ACID AMIDES
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Disclosed are methods for treating Alzheimer’s disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula 1 (1) wherein the variables R1-R8 and X are defined herein.
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- Chartreusin derivatives and salts thereof
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This invention relates to a novel chartreusin derivative of the general formula (I): STR1 and a salt thereof. This chartreusin derivative and a salt thereof have an excellent antitumor activity, which is exhibited even when the site of cancer inoculation and the site of drug administration are different. This invention further relates to a antitumorous composition containing the above-mentioned compound as active ingredient. This invention furthermore relates to a process for producing the above-mentioned chartreusin derivative or salt thereof.
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- Chartreusin derivatives and salts thereof
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This invention relates to a novel chartreusin derivative of the general formula (I): STR1 and a salt thereof. This chartreusin derivative and a salt thereof have an excellent antitumor activity, which is exhibited even when the site of cancer inoculation
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- THE HYDROCYANATION ROUTE TO β- AND γ-AMINO ACIDS. A SYNTHESIS OF α-METHYLENE-β-ALANINE
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Hydrocyanation of several phthalimidoalkynes proceeds with good regioselection yielding products which were easily converted into unsaturated β- and γ-amino acids.
- Jackson, W. Roy,Perlmutter, Patrick,Smallridge, Andrew
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p. 1983 - 1984
(2007/10/02)
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