CAS: 165534-43-0; Diethyl (4-Oxobenzo[d][1,2,3]Triazin-3(4H)-yl) Phosphate

该化合物其二氧磷磷基磷酸酯组在进一步功能化方面提供了多功能性,使其成为构建复杂的有机磷化合物的宝贵工具.该试剂与一系列溶剂和功能组的兼容性有助于其在合成化学工作流程中的广泛用途.

结构式图片

相似化合物

28230-32-2 125700-69-8 132533-58-5

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CAS号814-49-3 氯磷酸二乙酯 | CAS号28230-32-2 3-羟基-1,2,3-苯并三嗪... | CAS号762-04-9 亚磷酸二乙酯

合成工艺路线路线简述

  • 合成目标产物 Depbt 主要起始原料 Diethyl Chlorophosphate And 3-Hydroxy-1,2,3-Benzotriazin-4(3H)-One
  • (文献来源)合成步骤主要原料 Diethyl Chlorophosphate 和 3-Hydroxy-1,2,3-Benzotriazin-4(3H)-One
氯磷酸二乙酯,3-羟基-1,2,3-苯并三嗪-4(3H)-酮置于三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 3.0H,以82%的收率获得3-(二乙氧基邻酰氧基)-1,2,3-苯并三嗪-4-酮
参考文献:3-(二乙氧基磷酰氧基)-1,2,3-苯并三嗪-4(3H)-One(depbt):一种新型的偶联剂,具有出色的抗消旋性.
标题:3-(二乙氧基磷酰氧基)-1,2,3-苯并三嗪-4(3H)-One(depbt):一种新型的偶联剂,具有出色的抗消旋性.
摘要:[公式:参见文本]新型结晶磷酸盐试剂3-(二乙氧基磷酰氧基)-1,2,3-苯并三嗪-4(3H)-一(depbt)介导酰胺键的形成,并具有出色的抗外消旋性.进行了比较外消旋研究,事实证明depbt优于典型的phospho和铀偶联剂.Depbt易于制备,并且非常稳定,在室温下的保质期为数月.Depbt的优越性能使其成为偶联试剂库的有用且独特的补充.
Doi:10.1021/ol990573K

海关参考信息

专利信息


专利号:WO-2024181781-A1
优先权日:2023-02-27
标 题:Substrate for synthesis of biological polymers having anti-aggregation function and biological polymer synthesis method using same
发明人:JANG MYOUNG HOON; CHOI JAE SUN
权利人:SP2 TX INC
摘要:The present invention relates to a substrate for the synthesis of biological polymers having an anti-aggregation function, and a biological polymer synthesis method using the substrate. The substrate according to an aspect may have anti-aggregation functionality to enable high-yield and high-purity processes in the synthesis of biological polymers.

专利号:US-2013267680-A1
优先权日:2010-09-15
标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof
发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL
权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST
摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.

专利号:US-11066439-B2
优先权日:2016-12-10
标题 :Synthesis of liraglutide
发明人:GANGA RAMU VASANTHAKUMAR; PATIL NITIN; CHARYULU PALLE VENKATA RAGHAVENDRA; JASMINE CASTELINO ROOPA; MACHANI RAMBABU; SUVARNA DEEPA SHANKAR
权利人:BIOCON LTD
摘要:The present invention relates to the efficient solid-phase synthesis of liraglutide represented by Formula-I. The present invention relates to an efficient process for the preparation of liraglutide by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare backbone of liraglutide and upon completion of linear sequence, synthesis was extended from lysine side chain by adding γ-glutamic acid and palmitic acid, followed by removal of protective groups, cleavage of the peptide from solid support and purification of crude liraglutide obtained. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to suppress the aggregation of peptides and ensure reactions are going for completion, and thus avoid deletion sequences and improve the process yield.

专利号:US-2020247841-A1
优先权日:2017-09-27
标 题 :Synthesis of icatibant
发明人:RAMU VASANTHAKUMAR GANGA; PATIL NITIN SOPANRAO; PALLE VENTAKA RAGHAVENDRACHARYUL; Yogesha
权利人:BIOCON LTD
摘要:The present invention relates to the efficient solid-phase synthesis of Icatibant represented by Formula (I). The present invention relates to an efficient process for the preparation of Icatibant by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare Icatibant. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to ensure complete removal of piperidine and reactions are going for completion, and thus avoid addition/deletion sequences and also improve the process yield.

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:WO-2023039068-A1
优先权日:2021-09-08
标题:Compositions and methods for synthesis of peptide nucleic acid intermediates
发明人:COULL JAMES M; GILDEA BRIAN D
权利人:NEUBASE THERAPEUTICS INC
摘要:The present disclosure provides intermediates for the synthesis of peptide nucleic acid (PNA) backbones and monomers, such as cyclic intermediates, and methods of making the same.
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主要参考文献


1: Ye YH, Li H, Jiang X. DEPBT as an efficient coupling reagent for amide bond formation with remarkable resistance to racemization. Biopolymers. 2005;80(2-3):172-8. doi: 10.1002/bip.20201. 60(2):95-103. doi: 10.1034/j.1399-3011.2002.201000.x. 17(2-3):261-77. doi: 10.1016/0305-7372(90)90057-m. 1(1):91-3. doi: 10.1021/ol990573k. 60(3):229-45. doi: 10.1002/1097-0282(2001)60:3<229::AID-BIP10034>3.0.CO;2-P. 20(13):2601-2604. doi: 10.1039/d2ob00070a. Erratum in: Org Biomol Chem. 2022 Mar 30;20(13):2729. doi: 10.1039/d2ob90038f. 22(8):1729-35. doi: 10.1021/bc2002665. Epub 2011 Jul 29. 4(1):49-60. doi: 10.2174/1389557043487565. 65(1):55-64. doi: 10.1111/j.1399-3011.2004.00199.x. 14(9):1051-61. doi: 10.1002/psc.1041.
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合成参考文献


摘要:Li, Y.; Fang, X.; Wang, Y., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 68.
摘要:Li, Y.; Fang, X.; Wang, Y., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 7.
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