- Convenient synthesis of (R)-3-[(tert -Butoxycarbonyl)amino]piperidine and (R)-3-[(tert -Butoxycarbonyl)amino]azepane
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(R)-3-[(tert -Butoxycarbonyl)amino]piperidine and (R)-3-[(tert -butoxycarbonyl)amino]azepane were prepared in two steps starting from d -ornithine and d -lysine, respectively. In the key step, N -Boc-protected 3-aminolactams were converted into imido esters by O-alkylation and then hydrogenated to amines, under mild conditions (5 bar H 2, room temperature) and without isolation, over a standard hydrogenation catalyst (5% Pt/C).
- Kadyrov, Renat,Tok, Oleg L.
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- Besifloxacin hydrochloride key intermediate preparation method
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The invention discloses a besifloxacin hydrochloride key intermediate (R)-alpha-t-butyloxycarboryl-amino-epsilon-caprolactam preparation method. The preparation method comprises the steps of taking (R)-N-Boc-allylglycine and allyl amine as starting materials, and performing amide condensation, RCM reaction, and catalytic hydrogenation reduction to synthesize and prepare the (R)-alpha-t-butyloxycarboryl-amino-epsilon-caprolactam. The preparation method has the characteristics of high reaction selectivity, less side reactions, high total recovery and product quality, convenient and simple technological operation, and high stability and controllability, and is suitable for industrial production.
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Paragraph 0080; 0081; 0082; 0083; 0084; 0085; 0086; 0087
(2017/08/28)
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- Resolution of the Confusion in the Assignments of Configuration for the Ciliatamides, Acylated Dipeptides from Marine Sponges
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Direct comparison of authentic ciliatamide A with four synthetic isomers (1-4) by means of NMR and chiral-phase HPLC revealed that ciliatamide A possesses the 12R (d-N-MePhe residue) and 22S (l-Lys residue) configurations, which were not identical with either our previous assignment or those proposed by others through total synthesis. The absolute configuration of the methionine sulfoxide residue in ciliatamide D was also revised to be d.
- Takada, Kentaro,Irie, Raku,Suo, Rei,Matsunaga, Shigeki
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p. 2845 - 2849
(2017/11/06)
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- N-SUBSTITUTED BENZENE SULFONAMIDES
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Disclosed are N-substituted benzenesulfonamides for use intreating in treating or preventing cognitive disorders, such as Alzheimer′s Disease. Formula (I) In formula (I), R1, R2, R3, R4, R3’, R10
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Page/Page column 97
(2008/06/13)
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- Synthesis and characterization of bradykinin B2 receptor agonists containing constrained dipeptide mimics
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We have previously shown that substitution of the D-Tic-Oic dipeptide by a (3S)-[amino]-5-(carbonylmethyl)-2,3-dihydro-1,5-benzothiazepin-4(5H)-one (D-BT) moiety in the bradykinin B2 receptor antagonist HOE 140 resulted in a full potent and sel
- Amblard, Muriel,Daffix, Isabelle,Bergé, Gilbert,Calmès, Monique,Dodey, Pierre,Pruneau, Didier,Paquet, Jean-Luc,Luccarini, Jean-Michel,Bélichard, Pierre,Martinez, Jean
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p. 4193 - 4201
(2007/10/03)
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- Synthesis and dopamine receptor modulating activity of lactam conformationally constrained analogues of Pro-Leu-Gly-NH2
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A series of analogues of the potent analogue of Pro-Leu-Gly-NH2 (PLG), 2- oxo-3(R)-[(2(S)-pyrrolidinylcarbonyl)amino]-1-pyrrolidineacetamide (2) were synthesized in which the (R)-γ-lactam residue of 2 was replaced with a (R)- β-lactam, (R)-aminosuccinimide, (R)-cycloseryl, (R)-δ-lactam, (R)-ε- lactam, or (S)-ε-lactam residue to give analogues 3-8, respectively. These substitutions were made so as to vary the ψ2 torsion angle. The analogues were tested for their ability to enhance the binding of the dopamine receptor agonist ADTN to the dopamine receptor. Analogues 3-6 and 8 exhibited dose- response curves that were bell-shaped in nature with the maximum effect occurring at a concentration of 1 μM. Analogue 7 was inactive. Analogues 3 and 4 were found to be as effective as PLG, while analogues 5, 6, and 8 appeared to be more effective than PLG in terms of enhancing the binding of ADTN to dopamine receptors. The activity of analogues 3-6 and 8 with their ψ2 angles in the vicinity of that observed in a type II β-turn is consistent with the hypothesis that this type of turn is the bioactive conformation of PLG.
- Sreenivasan,Mishra,Johnson
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p. 256 - 263
(2007/10/02)
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