46229-47-4Relevant academic research and scientific papers
A synthetic amino acid N-methylation method and its product and application (by machine translation)
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Paragraph 0053; 0054; 0055, (2016/11/09)
The invention belongs to the technical field of amino acid polypeptide synthesis, discloses a synthetic amino acid N-methylation method and its product and application. This method passes the benzyl protection of a carboxyl group of the amino acid, trifluoroacetyl protection of the amino group, after methylation, get N-methylation of the amino acid. N obtained by the method of this invention-methyl (trifluoro-acetyl)-amino acid benzyl ester, can be directly used for polypeptide synthesis N-methyl structure having the amino acid benzyl ester product, and it has good selective deprotection of, its N the C-end-to-end and selectively deprotected. With foreign Ag 2 O/CH 3 I/Boc method (hypertoxic, high cost) and NaH / (CH 3 O) 2 SO 2 method compared with (hypertoxic), and the like, the method of the invention high yield, the use of the virulent reagent-free, safe and non-toxic, the operation is simple, common reagent to the raw material, the cost is low, and the structure strong pertinence, racemation a low possibility of the product obtained, it has broad industrial prospects. (by machine translation)
Enantioselective synthesis of 1,2,4-triazolines by chiral iron(ii)-complex catalyzed cyclization of α-isocyano esters and azodicarboxylates
Wang, Min,Liu, Xiaohua,He, Peng,Lin, Lili,Feng, Xiaoming
supporting information, p. 2572 - 2574 (2013/04/10)
Enantioselective cyclization of α-isocyano esters with azodicarboxylates catalyzed by FeII-N,N′-dioxide complexes has been developed. Under mild conditions, a variety of 1,2,4-triazoline derivatives was obtained in high yields and enantioselectivities.
Mimicking enzymatic transaminations: Attempts to understand and develop a catalytic asymmetric approach to chiral α-amino acids
Bachmann, Stephan,Knudsen, Kristian Rahbek,Jorgensen, Karl Anker
, p. 2044 - 2049 (2007/10/03)
Attempts are made to build a bridge between asymmetric catalysis and enzymatic reactions by mechanistic investigations and the development of a catalytic and enantioselective approach to amination of α-keto esters by primary amines catalyzed by chiral Lewis acids as a model for transamination enzymes. Different Lewis acids can catalyze the half-transamination of α-keto esters using primary amine nitrogen sources such as pyridoxamine and 4-picolylamine. The mechanistic studies of the Lewis-acid catalyzed half-transamination using deuterium-labelled compounds show the incorporation of deuterium atoms in several positions of the α-amino acid derivative, indicating that the enol of the α-keto ester plays an important role along the reaction path. The catalytic enantioselective reactions are dependent on the pKa-value of the solvent since enantioselectivities were only obtained in solvents with high pKa-values relative to methanol. However, stronger acidic conditions generally gave better yields, but poor enantioselectivities. A series of chiral Lewis acids were screened as catalysts for the enantioselective half-transamination reactions and moderate yields and enantioselectivities of up to 46% ee were obtained.
(α-aminophosphino) peptide derivatives, method for making same and therapeutic applications thereof
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, (2008/06/13)
The invention concerns compounds derived from (α-aminophosphino) peptides, of general formula (I), in which R1and R2each represents a hydrogen atom or taken together form an imine with the adjacent nitrogen atom; R3represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl group, a cycloalkylmethyl group or finally, a methyl group substituted by a heterocyclic, aromatic or saturated group; R4represents a phenyl group, a benzyl group, these groups capable of being substituted or not, a hydrogen atom, an alkyl group, analkenyl group or a cycloalkyl group; R5represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl, cycloalkylmethyl group or finally a methyl group substituted by a heterocyclic, aromatic or saturated group; R6, R7and R8can in particular represent a hydrogen atom, an alkyl group, a phenyl group substituted or not . . . n is equal to 0 or 1, in the form of enantiomers, diastereoisomers or racemic mixtures, their salts, their method of preparation and their therapeutic applications.
SYNTHESIS AND CHIROPTICAL PROPERTIES OF MODEL PEPTIDES SUITABLE FOR THE IMMUNOLOGICAL CHARACTERIZATION OF BRANCHED POLYPEPTIDES WITH THE GENERAL FORMULA POLYm)>
Mezoe, Gabor,Hudecz, Ferenc,Kajtar, Judit,Szekerke, Maria
, p. 803 - 812 (2007/10/02)
Over the last 10 years we have developed a new group of branched polypeptides with significant immunomodulatory activity, corresponding to the general formula poly (i 1, m ca. 3).The humoral immune response of four inbred mouse strains
