95437-43-7Relevant academic research and scientific papers
Regioselective Fluorination of α-Hydroxy-β-aminophosphonates by Using PyFluor
Ka?mierczak, Marcin,Kubicki, Maciej,Koroniak, Henryk
, p. 3844 - 3852 (2018/07/31)
We report a simple protocol for the synthesis of α-fluoro-β-aminophosphonates by the regioselective fluorination of α-hydroxy-β-aminophosphonates under mild conditions. The fluorination reactions were mediated by the PyFluor reagent and occurred with the retention of configuration. The main products of this reaction were a series of α-fluoro-β-aminophosphonates, which can be used as precursors in the preparation of medicinally important compounds (e.g., dipeptide analogues).
A silver-promoted solid-phase guanidylation process enables the first total synthesis of stictamide A
Li, Xiang,Li, Yu-Lei,Chen, Yan,Zou, Yan,Zhuo, Xiao-Bin,Wu, Qiu-Ye,Zhao, Qing-Jie,Hu, Hong-Gang
, p. 94654 - 94657 (2015/11/24)
The first total synthesis of stictamide A, a structurally unique peptide with a statine motif and a N-prenyl modified arginine in the side chain, is disclosed. The requisite statine was achieved via stereoselective hydrogenation of a functionalized ketone. The N-prenyl modified arginine was constructed by a novel silver-promoted solid-phase strategy for the first time. This synthetic method can be generally applied to the efficient synthesis of peptides containing statine and/or arginine N-alkylation groups.
Chiral Pool-Based Synthesis of Naphtho-Fused Isocoumarins
Raza, Abdul Rauf,Saddiqa, Aisha,?akmak, Osman
, p. 951 - 957 (2015/11/16)
A variety of chiral derivatives of benzo[d]naphtho[1,2-b]pyran-6-one were prepared in a single step by Et3N-mediated condensation of homophthalic anhydride with different derivatives of (S)-amino acid chlorides at -5 °C by employing a chiral pool methodology. Chirality 27:951-957, 2015.
Chiron based synthesis of isocoumarins: Reactivity of α-substituted carboxylic acids
Saddiqa, Aisha,Raza, Abdul R.,Black, David Stc.,Kumar, Naresh
, p. 736 - 743 (2014/06/09)
The asymmetric synthesis of a novel (S)-isocoumarin has been attempted in a single step by the coupling of homophthalic acid with (S)-N-protected amino acids and α-chloroacids at high temperature by exploiting a chiral pool methodology. The coupling of homophthalic acid with N-protected (S)-amino acids gave exclusion of the carboxyl/alkyl group. However, coupling of homophthalic acid with α-chloroacids afforded asymmetric isocoumarins in high yield.
An Efficient Synthesis of a Hydroxyethylamine (HEA) Isostere and Its α-Aminophosphonate and Phosphoramidate Derivatives as Potential Anti-HIV Agents
Bhattacharya, Asish K.,Rana, Kalpeshkumar C.,Pannecouque, Christophe,DeClercq, Eric
, p. 1601 - 1611 (2012/10/29)
HIV protease is a promising drug target for AIDS therapy, and several potent HIV-1 protease inhibitors have been reported to date. Although existing inhibitors exhibit high selectivity, they have also been associated with severe side effects and the possi
Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
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Page column 22, (2010/01/30)
Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Process for producing 3-amino-2-oxo-1-halogenopropane derivatives
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, (2008/06/13)
Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.
Solid phase reductive alkylation of secondary amines
Khan, Nawaz M.,Arumugam, Vijayalakshmi,Balasubramanian, Shankar
, p. 4819 - 4822 (2007/10/03)
Solid phase reductive alkylation of secondary amines has been carried out in excellent yields using borane-pyridine complex (BAP). Various aldehydes and ketones have been reacted with L-proline substituted on high-capacity Wang Resin.
