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CAS号74124-79-1 N,N'-二琥珀酰亚胺基碳酸酯 | CAS号2916-68-9 2-(三甲硅基)乙醇 | CAS号32315-10-9 三光气 | CAS号6066-82-6 N-羟基琥珀酰亚胺 | CAS号20160-60-5 2-三甲基甲硅烷基乙氧基羰酰氯合成工艺路线路线简述
- 合成目标产物 1-(2-(Trimethylsilyl)Ethoxycarbonyloxy)& 主要起始原料 N,N'-Disuccinimidyl Carbonate And 2-(Trimethylsilyl)Ethanol
- (文献来源)合成步骤主要原料 N,N'-Disuccinimidyl Carbonate 和 2-(Trimethylsilyl)Ethanol
2-(三甲硅基)乙醇置于potassium Carbonate,三乙胺体系中,用 甲苯,乙腈 作为反应溶剂,化学反应 1.75H,反应生成 N-[2-(三甲基硅基)乙氧羰氧基]琥珀酰亚胺
参考文献:Synthesis And Evaluation Of Novel Activated Mixed Carbonate Reagents For The Introduction Of The 2-(Trimethylsilyl)Ethoxycarbonyl(Teoc)-Protecting Group
标题:Synthesis And Evaluation Of Novel Activated Mixed Carbonate Reagents For The Introduction Of The 2-(Trimethylsilyl)Ethoxycarbonyl(Teoc)-Protecting Group
摘要:报告了1-[2-(三甲基硅烷基)乙氧羰氧基]苯并三氮唑(teoc-Obt)和1-[2-(三甲基硅烷基)乙氧羰氧基]吡咯烷-2,5-二酮(teoc-Osu)的高产率合成.这两种化合物均为晶体化合物,在schotten-Baumann条件下与氨基酸反应,可高产率地反应生成teoc-氨基酸.报告了九种新的teoc-氨基酸衍生物的合成.在合成teoc-苯丙氨酸过程中,分析了结晶为环己胺盐前后的产物,结果显示,当使用teoc-Obt作为酰化试剂时,产生了约5%的相应二肽,即teoc-苯丙氨酸-苯丙氨酸-Oh.相比之下,当使用teoc-Osu作为酰化试剂合成所研究的teoc-氨基酸衍生物时,未检测到二肽.使用teoc-Osu将有助于teoc基团在肽合成中的应用.
DOI:10.1055/s-1987-27939
海关参考信息
- 2912110000-甲醛
2912120000-乙醛
2915110000-甲酸
2924199090-其他无环酰胺 - 💡 提示:海关信息按照顺序优先匹配,如需确认的海关信息,请参考相关资料。
- 详情请参考:📖 海关编码查询和海关进出口税则
专利信息
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-2023391818-A1
优先权日:2020-11-05
标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人:NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.
专利号:US-8487094-B2
优先权日:2008-07-25
标题 :Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
发明人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA
权利人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA; BOEHRINGER INGELHEIM INT
摘要:Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).
专利号:US-8487108-B2
优先权日:2005-11-14
标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors
发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T
权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC
摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:WO-2023214577-A1
优先权日:2022-05-02
标 题 :Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人:KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO; NOMURA KENICHI
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:The present invention addresses the problem of a desired elongation reaction not progressing as a result of a 6-membered cyclic amidine skeleton structure and a diketopiperazine formed when removing an N-terminated protective group during peptide synthesis. The inventors have discovered that it is possible to solve said problem during peptide production by treating a peptide protected by an N-terminated amino group in a protective group having an Fmoc skeleton by using a base which has a pKa of 23 or higher in an acetonitrile of a conjugate acid in a specific solvent, and next, performing peptide chain elongation.