- Preparation method of beta-alanyl-L-histidine
-
The invention relates to the technical field of polypeptide synthesis, in particular to a preparation method of beta-alanyl-L-histidine. The preparation method of the beta-alanyl-L-histidine provided by the invention comprises the following steps: carrying out a reaction on beta-alanine and solid triphosgene to prepare 1, 3-oxazinane-2, 6-diketone, and then carrying out ring opening to prepare the beta-alanyl-L-histidine. The route of the method is shortened to two steps, the raw material conversion rate is high, the post-treatment is simple, and the purity of the obtained product is high.
- -
-
Paragraph 0062-0074
(2022/03/27)
-
- Synthesis method of cosmetic dipeptide
-
The invention discloses a synthesis method of cosmetic dipeptide and belongs to the technical field of polypeptide synthesis. The synthesis method comprises the following steps: protecting alanine byphthalic anhydride to prepare phthaloyl-protected alanine; then reacting with an acyl chlorination reagent to generate a corresponding acyl chloride product; enabling histamine and hexamethyldisilazane to react to obtain a silane protection object of histamine; then reacting with the acyl chloride product to obtain phthaloyl-protected dipeptide; finally, carrying out deprotection under a specificcondition to obtain the cosmetic dipeptide, wherein the cosmetic dipeptide is decarboxycarnosine. The synthesis method provided by the invention does not utilize a condensing agent and has the advantages of cheap and easy-to-obtain raw materials, few byproducts and high yield (the total yield is 78.6 to 86.4 percent); the dipeptide with high purity (the purity is higher than 99 percent) is easy toobtain; the cost is reduced and the synthesis method is suitable for large-batch production.
- -
-
-
- Carbonic anhydrase activators: Amino acyl/dipeptidyl histamine derivatives bind with high affinity to isozymes I, II and IV and act as efficient activators
-
Reaction of histamine (Hst) with tetrabromophthalic anhydride and protection of its imidazole moiety with tritylsulfenyl chloride, followed by hydrazinolysis, afforded N-1-tritylsulfenyl-histamine, a key intermediate which was further derivatized at its aminoethyl moiety. Reaction of the key intermediate with N-Boc-amino acids/dipeptides (Boc-AA) in the presence of carbodiimides afforded, after deprotection of the imidazolic and amino moieties, a series of compounds with the general formula AA-Hst (AA=amino acyl; dipeptidyl). The new derivatives were assayed as activators of three carbonic anhydrase (CA) isozymes, hCA I, hCA II (cytosolic forms) and bCA IV (membrane-bound form). Efficient activation was observed against all three isozymes, but especially against hCA I and bCA IV, with affinities in the nanomolar range for the best compounds. hCA II was, on the other hand, activatable with affinities around 10-20 nM. This new class of CA activators might lead to the development of drugs/diagnostic agents for the CA deficiency syndrome, a genetic disease of bone, brain and kidneys. Copyright (C) 1999 Elsevier Science Ltd.
- Supuran, Claudiu T.,Scozzafava, Andrea
-
p. 2915 - 2923
(2007/10/03)
-
- Models for Visual Pigments. The Effect of the Imidazolyl Group on the Absorption Maxima of the Retinal Schiff Base
-
The title effect has been investigated with the imidazolyl group either externally added or intramolecularly combined.N-Retinylidenebutylamine was protonated with imidazole derivatives under neutral conditions and was absorbed at longer wavelengths compared with carboxylic acids.The absorption peak with the imidazolyl group intramolecularly combined was highly affected by the structure, protonated Nα-retinylidene-L-histidine octadecylamide having an absorption maximum at 494 nm caused by the inductive effect and the polar imidazolyl group.
- Nanasawa, Masato,Kamogawa, Hiroyoshi
-
p. 1101 - 1104
(2007/10/02)
-