专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-6063919-A 优先权日:1998-08-14 标题:Process for the synthesis of exochelins 发明人:GAUDIOSO LARRY A; WEGLARZ MICHAEL A 权利人:KEYSTONE BIOMEDICAL INC 摘要:A process for the synthesis of an Exochelin comprising the steps of generating L-N-[(2-benzyloxy-(benzoyl)] serine or L-N-[2-benzyloxy (benzoyl)] threonine, creating L-N-t-Boc- epsilon -hydroxynorleucine and reacting same to produce L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester, providing a dicarboxylic acid and forming an O-benzyl methyl hydroxamate from the dicarboxylic acid, coupling the O-benzyl methyl hydroxamate with the L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester to give an L-N2-Boc-N6-methyl,N6-(benzyloxy) lysine 2-trimethylsilylethyl ester which incorporates the dicarboxylic acid as modified above, removing the N-tert-butoxycarbonyl protecting group from the L-N2-Boc-N6-methyl, N6-(benzyloxy) lysine 2-trimethylsilylethyl ester to yield a substituted lysine, and coupling the same with the L-N-[2-benzyloxy (benzoyl) serine or -threonine to yield a 2-trimethyl silylethyl ester of dibenzyl Exochelic acid, transforming the 2-trimethyl silylethyl ester of dibenzyl Exochelic acid to dibenzyl Exochelic acid, preparing benzyl epi-cobactin, forming an ester bond between the dibenzyl Exochelic acid and benzyl epi-cobactin to form an intermediate, and, hydrogenolytically removing three benzyl groups from said intermediate, resulting in the synthesized Exochelin. More particularly, a synthesis for Exochelin 786SM (R) is disclosed wherein the dicarboxylic acid is suberic acid and the serine form is utilized.
专利号:US-9433605-B2 优先权日:2006-03-23 标 题 :Method for promoting synthesis of tissue collagen 发明人:KAMIYA TOSHIKAZU; KAMIMURA AYAKO; KAWADA YOKO 权利人:KYOWA HAKKO BIO CO LTD 摘要:An object of the present invention is to provide an oral preparation for promoting synthesis of tissue collagen, an oral preparation for promoting healing of skin wounds or an oral preparation for preventing or improving skin wrinkles or sagging, which is safe and has an excellent effect. The present invention can provide an oral preparation for promoting synthesis of tissue collagen, an oral preparation for promoting healing of skin wounds or an oral preparation for preventing or improving skin wrinkles or sagging, which comprises hydroxyproline or a salt thereof as an active ingredient.
专利号:WO-2017080770-A1 优先权日:2015-11-10 标题 :Synthesis of (z)-endoxifen hydrochloride 发明人:HEINKELE GEORG; MUERDTER THOMAS; SCHWAB MATTHIAS 权利人:ROBERT BOSCH GES FÜR MEDIZINISCHE FORSCHUNG MBH 摘要:The invention relates to the synthesis of tamoxifen, endoxifen and derivatives thereof. Starting from a substituted benzoic acid derivative and 2-phenoxyethyl halide, the intermediate product of general formula (I) is obtained. The compound of general formula (VI) or a salt thereof is obtained from the compound of general formula (I), via isomer purification of the compound of general formula (I) by obtaining the (Z)-isomers and reacting the (Z)-isomers with an amine of formula HNR 6 R 7 . Alternatively, the compound of general formula (I) is reacted with a compound of formula HNR 6 R 7 , and the amine thus obtained is then subjected to isomer purification, wherein the compound of general formula (VI) or a salt thereof is obtained.
专利号:US-10604479-B2 优先权日:2013-11-18 标 题:Continuous process for the one-pot synthesis of metal salts and metal complexes 发明人:LEONARDI GIULIANO; GASPERONI GIOVANNI 权利人:VOLARE & CONNECTING LLC; LEONARDI GIULIANO; NOVUS INT INC 摘要:A continuous process is described for the one-pot synthesis of compounds, such as metal salts and metal complexes, as well as optionally for the protection of the compounds thus obtained by coating and/or impregnation with suitable compounds.
专利号:US-5405949-A 优先权日:1993-03-29 标题 :Process for the synthesis of glycosaminoglycans with heparin or heparan structure modified in position 2 of the α-L-iduronic-2-O-sulfate acid 发明人:UNGARELLI FABRIZIO; PIANI SILVANO 权利人:ALFA WASSERMANN SPA 摘要:A process for the synthesis of glycosaminoglycans with heparin or heparan structure modified in position 2 of the α-L-iduronic-2-O-sulfate acid in which the sulfate group is, entirely or in part, substituted with a nucleophilic group, is described. The process is carried out by treating glycosaminoglycans having heparin or heparan structure with a nucleophilic reagent in alkaline solution.
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合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 摘要:Compound: Benzoic acid, 4-hydroxy-, homopolymer 摘要:HANSCH,C ET AL. (1995) 参考文献:10.1097/00000539-199911000-00023|10.1213/00000539-199911000-00023 摘要:Goudas LC, Langlade A, Serrie A, Matson W, Milbury P, Thurel C, Sandouk P, Carr DB. Acute Decreases in Cerebrospinal Fluid Glutathione Levels after Intracerebroventricular Morphine for Cancer Pain. Anesthesia & Analgesia. 1999 Nov;89(5):1209 1215. doi: 10.1097/00000539-199911000-00023.