65873-72-5Relevant articles and documents
Simple synthetic process of 6-methoxypyridine-3-formaldehyde
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Paragraph 0033; 0046-0049; 0051; 0058-0061, (2020/03/25)
The invention relates to a synthesis process of 6-methoxypyridine-3-formaldehyde, which comprises the following steps: 1, reacting 6-bromo-3-methylpyridine with sodium methylate under the condition ofa dry protic solvent to obtain 6-methoxy-3-methylpyridine; 2, carrying out bromination reaction on the 6-methoxy-3-methylpyridine obtained in the step 1 with a bromination reagent in an aprotic solvent under the action of a catalyst to obtain 5-(dibromomethyl)-2-methoxypyridine; and 3, carrying out a hydrolysis reaction on the 5-(dibromomethyl)-2-methoxypyridine prepared in the step 2 with an alkali in a mixed solvent of an aprotic solvent and water to prepare 6-methoxypyridine-3-formaldehyde. According to the invention, 6-bromo-3-methylpyridine is used as a main raw material, and is subjected to sodium methylate substitution, bromination and alkali metal hydroxide hydrolysis, such that a target compound is obtained. The method has the advantages of simple and accessible raw materials ineach step, simple process operation and mild reaction conditions, and is suitable for industrial amplification.
Reversible Folding of a β-Hairpin Peptide by a Metal-Chelating Amino Acid
Reutzel, Jan,Diogo, Timm M.,Geyer, Armin
, p. 8450 - 8456 (2017/06/28)
5-(1-Hydroxy-pyridin-2(1H)-onyl)-l-alanine (Hop) is a N-hydroxy-1,2-pyridone functionalized α-amino acid with the desired metal-chelating properties of DOPA (3,4-dihydroxy phenylalanine) but without its unwanted redox activity. The Fmoc-protected amino acid Fmoc-l-Hop(tBu)-OH (11) was synthesized from glycine phosphonate followed by enzymatic hydrolysis of the methyl ester yielding the Hop l-isomer in 96 % ee. The amino acid 11 is used in automated peptide synthesis for the assembly of a 14mer β-hairpin peptide with the sequence [dsb1, 14]H-CHXETGKHGHKLVC-OH (X=W, l-Hop). While the 10 π electron containing indole side chain of l-Trp in peptide 14 completes the formation of a hydrophobic cluster and results in 90 % folding, the folded fraction is significantly decreased to approximately 30 % for the 6 π electron l-Hop side chain in peptide 16. Metal chelation of Ga3+ reconstitutes the folding of 16 to above 60 % due to the formation of the Ga(16)3 trimer. The chelation process of 16 is monitored by NMR spectroscopy and the subsequent release of Ga3+ by a competitive metal chelator exemplifies the reversible oligomerization of peptide epitopes by metal chelation, bearing the opportunity to synthesize protein-sized aggregates on the basis of reversible chemistry in water.
NOVEL TETRAHYDROPYRIDOPYRIMIDINES AND TETRAHYDROPYRIDOPYRIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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Page/Page column 157, (2016/07/27)
The invention provides novel compounds having the general formula (I): wherein R1, R2, R3, Q, U,W, Z, X and Y are as described herein, compositions including the compounds and methods of using the compounds. These compounds are HbsAg inhibitors and are useful as medicaments for the treatment or prophylaxis of HBV infection.