专利号:US-12162849-B2 优先权日:2018-12-21 标题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:The present invention relates to a method of synthesis of compound (I), wherein R1 represents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant.
专利号:US-2024294464-A1 优先权日:2021-10-27 标题 :Synthesis of restrained complexing agents 发明人:WONG NICHOLAS; GOSSELIN FRANCIS 权利人:GENENTECH INC 摘要:Improved methods of synthesis of a restrained complexing agent are described herein. Compounds, including salts and solvates thereof, and compositions relevant to the improved methods are also described.
专利号:US-10918627-B2 优先权日:2016-05-11 标 题:Convergent and enantioselective total synthesis of Communesin analogs 发明人:MOVASSAGHI MOHAMMAD; LATHROP STEPHEN PAUL; POMPEO MATTHEW W; CHANG WEN-TAU TIMOTHY 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A highly convergent biomimetic synthesis of a complex polycyclic scaffold has been successfully implemented. From these efforts, compounds having a structure of Formula (I): n nor a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R 1 -R 8 and m, n, r, s, t, and u are as defined herein, is provided. Methods of making such compounds are also disclosed as are methods for the treatment of cancer, various infectious diseases, and abnormal cardiovascular function.
专利号:WO-2017033128-A1 优先权日:2015-08-25 标题 :Biphenyl-substitued 4-amino-butyric acid derivatives and their use in the synthesis of nep inhibitors 发明人:HOOK DAVID; KU JIE; ZHOU JIANGUANG 权利人:NOVARTIS AG; HOOK DAVID; KU JIE; ZHOU JIANGUANG 摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors and prodrugs thereof.
专利号:WO-0012747-A1 优先权日:1998-08-31 标 题 :Method for enzymatic synthesis of glycosides, disaccharides, and oligosaccharides 发明人:NILSSON KURT 权利人:NILSSON KURT 摘要:The present invention describes a method for enzymatic synthesis of glucosides, disaccharides, oligosaccharides, modified disaccharides and oligosaccharides, preferably of the kind found in glycoproteins and especially of Lacto-N-tetraose (LNT) and of Lacto-N-neotetraose (LNnT).
专利号:US-7820795-B2 优先权日:2004-03-30 标 题:Lactobacillus fermentum N-desoxyribosyl transferases and the use thereof for enzymatic synthesis of 2′, 3′—didesoxynucleosides and 2′,3′- didehydro-2′,3′- didesoxynucleosides 发明人:KAMINSKI PIERRE-ALEXANDRE 权利人:PASTEUR INSTITUT 摘要:N-deoxyribosyl transferases of Lactobacillus fermentum and their analogues, as well their use for the enzymatic synthesis of 2′,3′-dideoxynucleosides and 2′,3′-didehydro-2′,3′-dideoxynucleosides. These transferases and their analogues include a N-deoxyribosyl transferase protein (DTP) that has at least 70%-95% identity with the polypeptide of SEQ ID NO: 2 or SEQ ID NO: 4, that retains residues Y13, D77, D97, E103, and M312 which respectively correspond to positions 13, 77, 97, 103, and 132 of SEQ ID NO: 2; and that has threonine at a position corresponding to position 15 of SEQ ID NO: 2 or SEQ ID NO: 4. Polynucleotides, vectors and host cells encoding these N-deoxyribosyl transferases and their analogues.
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合成参考文献
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