N-Cbz-甘氨酸乙酯置于水,Potassium Carbonate体系中,用 乙醇 用作溶剂,化学反应生成N-苄氧羰基甘氨酸 参考文献:Novel Inhibitor Compounds Specific Of Secreted Non-Pancreatic Human A2Phospholipase Of Group Ii 标题:Novel Inhibitor Compounds Specific Of Secreted Non-Pancreatic Human A2Phospholipase Of Group Ii 摘要:本发明涉及以下式(i)的化合物以及含有该化合物的药物组合物:其中d,Y,A,B,P,Q,W和r的含义与规范中定义的含义相同.
专利号:US-2022298204-A1 优先权日:2019-07-05 标题 :Synthesis of a-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:EP-3792250-A1 优先权日:2019-09-13 标题:Synthesis of alpha-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:US-5488131-A 优先权日:1994-03-23 标题:Synthesis of compounds with predetermined chirality 发明人:MYERS ANDREW G 权利人:CALIFORNIA INST OF TECHN 摘要:A method for synthesizing enantiomerically enriched chemical intermediates with predetermined chirality is described. The method comprises formation of a pseudoephedrine amide, followed by stereoselective alkylation at the alpha carbon. The chiral auxiliary can then be cleaved off, affording chiral end products useful for further transformations. The enantiomeric enrichment of the chiral end products may exceed 98%, and the chiral auxiliary can be recovered. Novel amides of pseudoephedrine used in this method are also disclosed.
专利号:US-2014066609-A1 优先权日:2012-09-05 标题 :Synthesis method of glyco-drug radiotracer precursor 发明人:LU KUEI-LIN; CHANG YU; HSU CHENG-FANG; WANG MEI-HUI; LIN WUU-JYH 权利人:LU KUEI-LIN; CHANG YU; HSU CHENG-FANG; WANG MEI-HUI; LIN WUU-JYH; ATOMIC ENERGY COUNCIL 摘要:A novel synthesis method of Glyco-drug radiotracer precursor is revealed. After completing synthesis of Z-Gly-ah (main structure), galactosamine GalNAc(OAc) 4 is added to have coupling reaction. Then a product is separated directly from dichloromethane. Thus loss of galactosamine during extraction with liquid chromatography is reduced. Moreover, instead of trifluoroacetyl group, carbobenzoxy (abbreviated as Cbz or Z) is used as a protecting group to ensure uniformity of the phase. The cost and synthesis time are also dramatically reduced.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
1: Fiammengo R, Licini G, Nicotra A, Modena G, Pasquato L, Scrimin P, Broxterman QB, Kaptein B. Duality of mechanism in the tetramethylfluoroformamidinium hexafluorophosphate-mediated synthesis of N-benzyloxycarbonylamino acid fluorides. J Org Chem. 2001 Aug 24;66(17):5905-10. Review. French. French. 11: Szawelski RJ, Wharton CW. Kinetic solvent isotope effects on the deacylation of specific acyl-papains. Proton inventory studies on the papain-catalysed hydrolyses of specific ester substrates: analysis of possible transition state structures. Biochem J. 1981 Dec 1;199(3):681-92. 12: Yuthavong Y, Suttimool W. Rate constants of individual steps in papain-catalysed reactions. Biochim Biophys Acta. 1978 Mar 14;523(1):198-206.
合成参考文献
摘要:Croft, R. A.; Bull, J. A., Science of Synthesis Knowledge Updates, (2018) 4, 416. 摘要:Wessjohann, L. A.; Kaluđerović, G. N.; Neves Filho, R. A. W.; Morejon, M. C.; Lemanski, G.; Ziegler, T., Science of Synthesis: Multicomponent Reactions, (2013) 1, 423. 摘要:Wessjohann, L. A.; Kaluđerović, G. N.; Neves Filho, R. A. W.; Morejon, M. C.; Lemanski, G.; Ziegler, T., Science of Synthesis: Multicomponent Reactions, (2013) 1, 425. 摘要:Journal of Pharmaceutical Sciences., 68(696), 1979 [] 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).