- Method for preparing long aliphatic chain diacid derivative and application of long aliphatic chain diacid derivative
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The invention provides a method for preparing a long aliphatic chain diacid derivative. The method comprises the following steps of: (1) carrying out a cyclization reaction on long aliphatic chain diacid, the long aliphatic chain diacid having a structure as shown in a formula (A); (2) reacting the long aliphatic chain diacid cyclization product with benzyl alcohol to obtain long aliphatic chain diacid monobenzyl ester; (3) carrying out an esterification reaction on the long aliphatic chain diacid monobenzyl ester and N-hydroxysuccinimide so as to obtain long aliphatic chain diacid succinimide benzyl ester; (4) carrying out a nucleophilic addition amidation reaction on the long aliphatic chain diacid succinimide benzyl ester and a compound as shown in a formula (B) to obtain a compound as shown in a formula (C); (5) carrying out an esterification reaction on the compound as shown in the formula (C) and N-hydroxysuccinimide again so as to obtain a compound as shown in a formula (D); and (6) carrying out a debenzylation reaction on the compound shown in the formula (D) so as to obtain a compound shown in a formula (E).
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- Synthesis method of somaglutide fatty acid side chain derivative
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The invention relates to a synthesis method of a somaglutide fatty acid side chain I. The method comprises the following steps: with octadecyl diacid as an initial raw material, carrying out esterification hydrolysis on octadecyl diacid and benzyl alcohol to obtain an intermediate I; subjecting the intermediate I to reacting with TSTU to obtain an active ester of the intermediate I, namely an intermediate II; subjecting the intermediate II to reacting with 1-benzyl-L-glutamic acid to obtain an intermediate III; subjecting the intermediate III to reacting with TSTU to obtain an active ester of the intermediate III, namely an intermediate IV; subjecting the intermediate IV to reacting with AEEA-AEEA to obtain an intermediate V; subjecting the intermediate V to reacting with TSTU to obtain an intermediate VI; and removing a benzyl group from the intermediate VI under the action of Pd/C and hydrogen to obtain the somaglutide fatty acid side chain I. The method for preparing the semaglutide fatty acid side chain I has the advantages of few reaction types, mild reaction conditions in each step, controllable quality of intermediates in each step, high overall yield, economic performance and effectiveness, and suitableness for large-scale production.
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Paragraph 0056-0063
(2021/04/21)
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- Method for preparing alkyl diacid monobenzyl ester
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The invention relates to a method for preparing an alkyl diacid monobenzyl ester, and belongs to the technical field of chemical engineering. According to the method provided by the invention, an alkyl diacid is used as a raw material and is subjected to esterification reaction with benzyl bromide or benzyl chloride in a mixed system of an organic solvent and water under the action of an alkali toobtain the alkyl diacid monobenzyl ester. The method is good in selectivity, convenient to operate, high in yield, low in cost and beneficial to implementation.
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Paragraph 0031-0032
(2019/12/25)
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- METHODS OF TREATING OR AMELIORATING METABOLIC DISORDERS USING GROWTH DIFFERENTIATION FACTOR 15 (GDF-15)
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The disclosure relates to the treatment of non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), as well as end-stage liver disease, hepatic steatosis (fatty liver), liver fibrosis, liver inflammation, liver cirrhosis, primary biliary cirrhosis (PBC), and hepatocellular carcinoma (HCC), by administering to a subject in need a GDF15 protein or a functional variant, mutation, fusion, or conjugate thereof, and to pharmaceutical compositions that contain the same.
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Paragraph 00289 - 00291
(2017/08/01)
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