Fmoc-Thr(But)-O-Pha置于溶剂黄146,锌体系中,化学反应生成 Fmoc-O-叔丁基-L-苏氨酸 参考文献:Application Of T-Butyldimethylsilyl Ethers Of Serine,Threonine And Tyrosine In Peptide Syntheshsis 标题:Application Of T-Butyldimethylsilyl Ethers Of Serine,Threonine And Tyrosine In Peptide Syntheshsis 摘要:The Utility Of Tbdms (T-Butyldimethylsilyl) Ethers,Prepared Conveniently In A One-Pot Procedure From N(Alpha)-Fmoc (9-Fluorenylmethoxycarbonyl) And N(Alpha)-Z (Benzyloxycarbonyl) Hydroxyamino Acids,Is Demonstrated: Peptide Bond Formation And Esterification To 4-Alkoxybenzylalcohol Resin Are Achieved Readily With These Derivatives. The Lability Of The Tbdms Ethers To Various Reagents Enables Selective Deprotection Of The Hydroxyl Side-Chains After Peptide Chain Assembly,Desirable,E.G.,For Phosphorylation Or Glycosilation. DOI:10.1016/s0040-4039(00)60836-5
专利号:US-2023242581-A1 优先权日:2020-06-17 标题:Synthesis of a guanylate cyclase agonist by fragments based approach 发明人:SAMBASIVAM GANESH; KASTURCHAND GODHA ATUL; VENKATA BHAGYARAJ ARETI; ANNADURAI SATHYA; VEERANJANEYULU AVULA; VASANTRAO GADAKH AMOL; S JADHAV DIPAK 权利人:ANTHEM BIOSCIENCES PRIVATE LTD 摘要:The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.
专利号:US-2024067694-A1 优先权日:2021-01-04 标 题:Synthesis of teduglutide 发明人:GANGA RAMU VASANTHAKUMAR; PATIL NITIN; SUVARNA DEEPA SHANKAR 权利人:BIOCON LTD 摘要:The present invention provides for novel synthetic approach of solid phase synthesis of peptides with C-terminal Aspartic acid by anchoring the side chain carboxylic group of aspartic acid to the solid support to avoid the formation of various impurities and thus resulting in higher yield and ease the purification process. The present invention further provides the usage of free amino acids and reducing agents as antioxidants in the cleavage cocktail to negate the formation of oxidative impurities formed during the global cleavage and isolation of the peptide from solid support.
专利号:US-8722852-B2 优先权日:2006-04-28 标 题 :Cosmetic composition for stimulating the synthesis of proteins of the basement membrane 发明人:ZIEGLER HUGO; IMFELD DOMINIK; STOCKLI MARTIN; HEIDL MARC 权利人:ZIEGLER HUGO; IMFELD DOMINIK; STOCKLI MARTIN; HEIDL MARC; DSM IP ASSETS BV 摘要:Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R 1 is H, C 1 -C 20 -alkyl, cycloalkyl or aryl-C 1 -C 4 -alkyl, n is 1-4, X is —O—, —NH— or —NR 2 — and R 2 H or C 1 -C 20 -alkyl; and at least one compound corresponding to the above formula (I) but in which XR 1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is —NR 2 — and both R 1 and R 2 are different from H, and the compounds corresponding to formula (I) but in which XR 1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.
专利号:US-6316593-B1 优先权日:1996-02-09 标题:Synthesis of VIP analog 发明人:BOLIN DAVID ROBERT; DANHO WALEED; FELIX ARTHUR M 权利人:HOFFMANN LA ROCHE 摘要:This invention relates to a novel process for the synthesis of vasoactive intestinal peptide analog Ac(1-31)-NH2 from four protected peptide fragments.
专利号:EP-1960423-B1 优先权日:2004-12-30 标 题:Synthesis of peptide t-20 using peptide intermediate fragments 发明人:HAN YEUN-KWEI; JOHNSTON DAVID A; KHATRI HIRALAL N 权利人:HOFFMANN LA ROCHE 摘要:Methods for the solid phase synthesis of T-20 peptides and peptide intermediates, in particular methods involving synthesizing T-20 peptide intermediates at low loading factors to produce products having excellent purity and yield.
专利号:EP-0824103-A1 优先权日:1996-08-13 标题:Method for synthesis of Tyr-3-octreotide 发明人:SU CHANG-SHINN; LEE TE-WEI; CHANG SHIANG-RONG; CHYI SHYH-YI; SHEN LIE-HANG; TSAI ZEI-TSAN 权利人:SU CHANG SHINN; LEE TE WEI; CHANG SHIANG RONG; CHYI SHYH YI; SHEN LIE HANG; TSAI ZEI TSAN 摘要:The present invention is a novel synthesis of Tyr-3-octreotidenfor radiopharmaceuticals. In this method, thenstarting material, Fmoc-Cys(Trt)-Wang Resin, is coupled withnvarious selected amino acids to form a straight chain ofnpeptide-resin compound, D-Phe-Cys(Trt)-Tyr(tBu)-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-WangnResin. This compound thennreacts with iodine to give disulfide-containing peptidenresin ofn nCleavage of the peptide from the resin is achievednby aminolysis with threoninol, the cleavaged peptide isnfurther deprotected with trifluoroacetic acid (TFA) tonobtain the crude peptide Tyr-3-octreotide of the formulan nwhich can be purified by high performance liquidnchromatography (HPLC). The final product Tyr-3-octreotidencan be labelled by radioiodine for tumor imagingnradiopharmaceuticals.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1385/1-59259-783-1:349 摘要:Knight CG, Onley CM, Farndale RW. Peptide synthesis in the study of collagen-platelet interactions. Methods Mol Biol. 2004;273():349–64. doi: 10.1385/1-59259-783-1:349.