- A synthetic amino acid N-methylation method and its product and application (by machine translation)
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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)
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Paragraph 0031; 0039; 0040; 0041
(2016/11/09)
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- Enantioselective synthesis of 1,2,4-triazolines by chiral iron(ii)-complex catalyzed cyclization of α-isocyano esters and azodicarboxylates
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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.
- Wang, Min,Liu, Xiaohua,He, Peng,Lin, Lili,Feng, Xiaoming
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supporting information
p. 2572 - 2574
(2013/04/10)
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- Concise synthesis of α-methylene-β-hydroxy-γ-carboxy- γ-lactams
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A concise protocol for the synthesis of α-methylene-β-hydroxy- γ-carboxy-γ-lactams has been described via alkylation of amino acid derived iminoesters with α-bromomethylmethacrylate, followed by allylic hydroxylation. All the synthesized compounds have been evaluated for their cytotoxicity on multiple myeloma cancer cell lines.
- Tekkam, Srinivas,Johnson, Joseph L.,Jonnalagadda, Subash C.,Mereddy, Venkatram R.
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p. 955 - 958
(2013/08/23)
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- An efficient synthesis of [2.2.1] heterobicyclic pyroglutamates
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A novel methodology for the efficient synthesis of [2.2.1] heterobicyclic pyroglutamates has been described. The key synthetic steps involve alkylation of amino acid-derived iminoesters with Baylis-Hillman bromide, RhCl 3-catalyzed exocyclic olefin isomerization, diastereoselective dihydroxylation, and regioselective lactonization. All the compounds were evaluated for their cytotoxicity using multiple myeloma cancer cell lines RPMI 8226.
- Tekkam, Srinivas,Johnson, Joseph L.,Jonnalagadda, Subash C.,Mereddy, Venkatram R.
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p. 969 - 972
(2013/08/23)
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- 4-pentenoyl groups for derivatization and protection of amino acids
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A method of separating a racemic mixture of amino acid enantiomers, which entails reacting the mixture with a 4-pentenoyl compound, thereby derivatizing the enantiomers to form two diastereomers, and separating the diastereomers.
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