2021-58-1Relevant articles and documents
Method for preparing 3 - (2 - thienyl) - D D-alanine
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Paragraph 0011; 0053; 0055; 0059; 0061; 0065; 0067; 0068, (2021/05/12)
The invention discloses a method for preparing 3-(2-thienyl)-D-alanine, which comprises the following steps: (1) hydantoin and 2-thiophenecarboxaldehyde carry outare subjected to condensation reactionunder the shielding of inert gas and the existence of a catalyst and water, so that 2-thiophenesubhydantoin is obtained; (2) 2-thiophenesubhydantoin carries outis subjected to hydrogenation reductionreaction under the existence of hydrogen and a catalyst, so that 2-thiophenehydantoin and N-formyl-2-thienyl-DL-alanine are obtained; (3) 2-thiophenehydantoin obtained in step (2) carries outis subjected to enzymatic conversion reaction under the effect of D-hydantoinhydrolase and carbamoylase and under the shielding of inert gas, so that 3-(2-thienyl)-D-alanine is obtained. The method is safe tooperate, highly efficient and environmentally -friendly, reaction conditions are mild, the yield of reaction is high, the quality of the product is good, and reaction amplification can also be realized.
Improved preparation of racemic 2-amino-3-(heteroaryl)propanoic acids and related compounds containing a furan or thiophene nucleus
Kitagawa, Tokujiro,Khandmaa, Dashrenchin,Fukumoto, Ayumi,Asada, Makoto
, p. 1137 - 1139 (2007/10/03)
Racemic 2-amino-3-(heteroaryl)propanoic acids (1), mostly with a furan or thiophene nucleus as a heteroaryl group, were synthesized in 48-94% yield by the reduction of 3-(heteroaryl)-2-(hydroxyimino)propanoic acids (5) with zinc dust and formic acid in the presence of a catalytic amount of iron dust at 60°C for 2 h. Under these conditions, unfavorable hydrogenolysis of bromine on the thiophene nucleus does not occur. Traditional Nformylation of the prepared 3-(heteroaryl)alanine (1) with a mixture of formic acid and acetic anhydride afforded 2-(formylamino)-3-(heteroaryl)propanoic acids (6) in 51-95% yield.
Peptides with an insulin-like action
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, (2008/06/13)
Peptides with an insulin-like action, of formula I: STR1 in which G is a hydrogen atom, an amino add residue, or a monosubstituted or polysubstituted amino acid; D is an amino acid residue, a phosphoamino acid residue, a monosaccharide residue, or a covalent bond; E is --NH--(CH2)n --NR52, a glycerol residue, or --NH--(CH2)p --R6 --R7 ; R1 is (C1 -C4)-alkyl or =O; R2 is a sulfhydryl protecting group, (C1 -C3)-alkyl, or a hydrogen atom; R3 and R4, independently of one another, are a hydrogen atom or methyl; R5, each being identical or different, is a hydrogen atom, 1 to 6 monosaccharide residues, or 1 to 6 monosubstituted or polysubstituted monosaccharide residues; R6 is O PO4 H, PO2 H, NHCOO, S or OCOO; R7 is a hydrogen atom, 1 to 6 monosaccharide residues, or 1 to 6 monosubstituted or polysubstituted monosaccharide residues; w is an integer 1 or 2; their preparation and use for treatment of diabetes mellitus or insulin-independent diabetes.
