- A highly enantioselective Mannich reaction of aldehydes with cyclic N-acyliminium ions by synergistic catalysis
-
Matched combinations of Bronsted or Lewis acids with suitable pro-electrophiles and secondary amine organocatalysts enable the novel enantioselective syntheses of carbamoyl dihydroquinoline and tetrahydropyridine derivatives with concomitant formation of two stereocenters. A short formal asymmetric synthesis of (2R,2′R)-threo-methylphenidate (Ritalin) is also described.
- Berti, Francesco,Malossi, Federico,Marchetti, Fabio,Pineschi, Mauro
-
supporting information
p. 13694 - 13697
(2015/09/01)
-
- Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
-
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
- -
-
-
- Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
-
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
- -
-
-
- Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
-
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer''s disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer''s disease both prophylactically and therapeutically with such pharmaceutical compositions.
- -
-
-
- Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
-
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
- -
-
-
- Compounds for inhibiting β-amyloid peptide release and/or its synthesis
-
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis.
- -
-
-
- Compounds for inhibiting β-amyloid peptide release and/or its synthesis
-
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis.
- -
-
-
- Novel peptide derivatives
-
The invention relates to lipopeptides of the formula I, STR1 in which each of Ra1 and Rb1, independently of the other, represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 7 to 21 carbon atoms that is optionally substituted by oxygen functions, or one of the radicals Ra1 --CO-- and Rb1 --CO-- represents hydrogen and the other of the radicals Ra1 --CO-- and Rb1 --CO-- represents an acyl radical, wherein Ra1 and Rb1 have the meanings given above, R2 represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 1 to 21 carbon atoms that is optionally substituted by oxygen functions, n=0 or 1, As° represents a radical of the formula --O--Kw--CO-- or --NH--Kw--CO-- wherein Kw represents an aliphatic hydrocarbon radical having a maximum of 12 carbon atoms, As1 represents a D- or L-α-amino acid, each of Z1 and Z2, independently of the other, represents hydroxy or the N-terminal radical of a D- or L-α-aminocarboxylic acid, of an amino-lower alkanesulphonic acid or of a peptide having a maximum of 6 amino acids from the group consisting of D- or L-α-aminocarboxylic acids and amino-lower alkanesulphonic acids, and Z3 represents hydrogen or --CO--Z4 wherein Z4 represents hydroxy or the N-terminal radical of a D- or L-α-amino acid, of an amino-lower alkanesulphonic acid or of a peptide having a maximum of 6 amino acids from the group consisting of D- or L-α-aminocarboxylic acids and amino-lower alkanesulphonic acids, and the amides and esters of such compounds that contain carboxy groups. The novel lipopeptides have an immunity-stimulating action.
- -
-
-
