- Raney-co mediated reductive cyclization of an α,β-unsaturated nitrile
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(Chemical Equation Presented) An expedient, five step synthesis of caprolactam 1 is reported starting from natural L-homoserine. The key step is a chemoselective reductive cyclization of α,β-unsaturated nitrile 10 mediated by Raney-Co type metals. This hydrogenation is extensively investigated in order to account for the observed product distribution and yields.
- Janey, Jacob M.,Orella, Charles J.,Njolito, Eugenia,Baxter, Jenny M.,Rosen, Jonathan D.,Palucki, Michael,Sidler, Rick R.,Li, Wenjie,Kowal, Jason J.,Davies, Ian W.
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p. 3212 - 3217
(2008/09/19)
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- Synthesis of δ-amino acids with an ether linkage in the main chain and nucleobases on the side chain as monomer units for oxy-peptide nucleic acids
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Syntheses of four N-Fmoc δ-amino acids with an ether linkage in the main chain and four different nucleobases on the side chain, Fmoc-NH- C*H(CH2-CH2-B)-CH2-O-CH2-COOH (B=thymine, uracil, N4-benzoylcytosine, and N2-isobutyrylguanine) are described. The δ-amino acids were prepared through 8-12 step synthesis starting from L-homoserine and could be linked together to form novel peptide nucleic acids (oxy-PNAs = OPNAs).
- Kuwahara, Masayasu,Arimitsu, Miki,Sisido, Masahiko
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p. 10067 - 10078
(2007/10/03)
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- Aldehyde derivatives and their use as calpain inhibitors
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Aldehyde derivatives with a specific calpain inhibiting activity and a platelet-aggregation inhibiting effect with formula (I) or formula (II): wherein R1 represents an aromatic hydrocarbon group, a heterocyclic group, or a group of-X-R3 in which X represents O,-S(O)m-(m = 0, 1, or 2), and R3 represents an aromatic hydrocarbon group, a heterocyclic group, or an alkyl group; Z represents R?-Y-or R?O-CH(R?)-in which Y represents a 3-to 7-membered nitrogen-containing saturated heterocyclic group, or a single cyclic saturated hydrocarbon group, R? represents an alkyl group, an alkenyl group, an alkynyl group, an acyl group, a sulfonyl group, an alkoxycarbonyl group, a carbamoyl group, or a thiocarbamoyl group, R? represents hydrogen, an alkyl group, or an aromatic hydrocarbon group, and R? represents an acyl group, a carbamoyl group, a thiocarbamoyl group, or an alkyl group; and n is an integer of 1 to 5. wherein R?, R?, R?, and R1? are defined in the specification.
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