专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-7193103-B2 优先权日:2000-05-19 标题:Synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester using oxazolidinone derivatives 发明人:PRAKASH INDRA 权利人:NUTRASWEET CO 摘要:Synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester by treating N-(3,3-dimethylbutyl)-L-aspartic acid with ketones to give oxazolidinone derivatives, which are condensed with L-phenylalanine methyl ester.
专利号:US-5554725-A 优先权日:1994-09-14 标题:Synthesis of dolastatin 15 发明人:PETTIT GEORGE R 权利人:UNIV ARIZONA 摘要:The present invention relates to the synthesis of natural (-)- dolastatin and the elucidation of the absolute configuration of this important sea hare constituent. A segment synthetic strategy was utilized for obtaining the Dolabella auricularia (Indian Ocean sea hare) depsipeptide dolastatin 15. Reaction of protected (S)-Hiva-(S)-Phe (2c) with isopropenyl chloroformate followed by Meldrum's ester, cyclization (2c→3a) of the product in toluene and finally methylation afforded the key (S)-dolapyrrolidine (Dpy) derivative (3b). Condensation of tripeptide (8) with the three unit Dpy segment (5b) followed by deprotection and coupling (diethyl phosphorocyanidate) led to dolastatin 15 in 11% overall yield. The powerful and selective activity of dolastatin 15 against the U.S. National Cancer Institute's panel of human cell lines is reported.
专利号:US-10829792-B2 优先权日:2017-03-21 标 题 :Biocatalytic synthesis of strained carbocycles 发明人:CHEN KAI; HUANG XIONGYI; KAN S B JENNIFER 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein are methods for producing products containing strained carbocycles, such as cyclopropene moieties and/or bicyclobutane moieties. The methods include combining an alkyne and a carbene precursor in the presence of a heme protein, e.g., a cytochrome P450, under conditions sufficient to form the strained carbocycle. Reaction mixtures for producing strained carbocycles are also described, as well as whole-cell catalysts comprising heme proteins and variants thereof for forming cyclopropenes, bicyclobutanes, and related products.
专利号:WO-2024075813-A1 优先权日:2022-10-07 标 题:Polypeptide synthesis using diketopiperazine compound 发明人:YAMAMOTO HISASHI; MITSUDA MASARU; HATTORI TOMOHIRO 权利人:CHUBU UNIV EDUCATIONAL FOUNDATION 摘要:Provided are: a novel diketopiperazine compound for rapid and easy synthesis of various polypeptides; and a method for manufacturing the same. The diketopiperazine compound is represented by general formula (1). (In the formula, R 1 , R 2 , R 3 , R 4 , and R 5 are each independently a hydrogen atom, a substituted or unsubstituted hydrocarbon group, or a substituted or unsubstituted heterocyclic group. R 1 and R 2 , R 1 and R 5 , R 2 and R 5 , and/or R 3 and R 4 are each optionally bonded to form a ring. PGE represents an electron-withdrawing protective group.)
专利号:US-5350681-A 优先权日:1986-08-18 标题 :Enzymatic membrane method for the synthesis and separation of peptides 发明人:IACOBUCCI GUILLERMO A; BROSE DANIEL J; RAY RODERICK J; VAN EIKEREN PAUL 权利人:COCA COLA CO 摘要:The present invention discloses a method for the enzymatic synthesis of a peptide. A protected peptide having a C-terminal carboxylate group or a protected, N-acyl amino acid having an alpha carboxylate group is reacted with a protected peptide having an N-terminal ammonium group or a protected amino acid having an alpha ammonium group in the presence of a condensation enzyme under conditions in which the carboxylate group and the ammonium group condense to form a protected, uncharged, peptide product. This peptide product is transported across a water-immiscible hydrophobic phase into an aqueous product phase and prevented from back diffusing across the water-immiscible hydrophobic phase. The peptide product can be converted, chemically or enzymatically, to a charged species that cannot back diffuse across the water-immiscible phase into the aqueous reaction phase. The water-immiscible hydrophobic phase is an ion rejection membrane separating the aqueous reaction phase from the product phase creating oil/water interfaces with each of the aqueous phases.
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合成参考文献
参考文献:10.1007/bf01388178 摘要:Döbler C, Kreuzfeld HJ, Fischer C, Michalik M. Asymmetric hydrogenation of dehydrodipeptide esters bearing different protective groups. Amino Acids. 1999;16(3-4):391–401. doi: 10.1007/bf01388178.