- Amino-protected (R) - 3-amino-piperidine preparation method
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The invention discloses a preparation method of amino protection (R)-3-amino piperidine, and the preparation method comprises the following steps: (1) in the presence of a first solvent or absence of a solvent, reacting a compound of formula V with benzylamine to obtain a compound of formula VI; (2) in the presence of a second solvent, performing catalytic hydrogenation of the compound of formula VI to remove benzyl to obtain the amino protection (R)-3-amino piperidine. According to the method, the defects of use of expensive metal catalysts and use of high-pressure hydrogenation and various splitting for synthesis of a chiral amino piperidine ring can be avoided, at the same time, the synthetic route is short, the process is simple, the yield is high, and the method is suitable for industrial mass production.
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Paragraph 0044-0046
(2017/03/18)
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- Controlling the position of functional groups at the liquid/solid interface: Impact of molecular symmetry and chirality
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With the aim of controlling the position of functional groups in a substrate-supported monolayer, a new family of functionalized linear alkyl chains was designed and synthesized, aided by molecular mechanics and dynamics simulations of its two-dimensional self-assembly on graphite. The self-assembly of these amino functionalized diamides at the liquid/solid interface was investigated with scanning tunneling microscopy. Intermolecular hydrogen-bonding interactions involving amides, combined with the effect of molecular symmetry and chirality, were found to guide the self-assembly. Control of the relative position and orientation of the amine groups was achieved, in the case of enantiopure compounds. Interestingly, racemates led to both racemic conglomerate and solid solution formation, with a concomitant loss of positional and orientational control of the amino groups as a result.
- De Cat, Inge,Gobbo, Cristian,Van Averbeke, Bernard,Lazzaroni, Roberto,De Feyter, Steven,Van Esch, Jan
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supporting information; experimental part
p. 20942 - 20950
(2012/02/13)
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- Highly diastereoselective monoalkylation and Michael addition of N- (diphenylmethylene)glycinesultam under solid-liquid phase-transfer catalysis conditions using potassium carbonate as base
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Treatment of a sultam-derived N-(diphenylmethylene)glycinate equivalent 1 with activated (allylic and propargylic) organic bromides and with Michael acceptors under solid-liquid phase-transfer catalysis conditions, using potassium carbonate as base, affords the monoalkylated compounds with high diastereoselectivity (>97% d.e.).
- Lopez, Anna,Pleixats, Roser
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p. 1967 - 1977
(2007/10/03)
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- Peptide Synthesis at High Pressure: Activation Volume of a Peptide Coupling, Synthesis of a Glutathione Derivative
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From the pressure-induced rate enhancement the activation volume of the peptide coupling 1 with the sodium salt of glycine 2 leading to the corresponding dipeptide derivative 3 was determined to be strongly negative (ΔV≠ = -(19.3 ± 0.5) cm
- Klaerner, Frank-Gerrit,Kalthof, Ulrike,Gante, Joachim
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p. 359 - 364
(2007/10/03)
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- Fatty acid analogs and prodrugs
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Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure STR1 in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L--Ala, L--Ile, L--Phe, L--Trp, L--Thr or an amide such as NHCH2 C6 H5 or NH(CH2)2 C6 H5,
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- Asymmetric Catalysis by Vitamin B12: The Isomerization of Achiral Aziridines to Optically Active Allylic Amines
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Achiral N-acylaziridines are isomerized to optically active N-acyl-allylamines in ee's of up to 95percent by catalytic amounts of cob(I)alamin in MeOH.
- Zhang, Zhong da,Scheffold, Rolf
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p. 2602 - 2615
(2007/10/02)
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