CAS: 134098-70-7; Fmoc-D-Asp-Otbu

该化合物是一种受保护的氨酸酸,作为浸硫化物合成中常用的浸硫酸,是一种受保护的形式.Fmoc(9-氟二氧基碳基)组群是氨基功能的保护群体,允许peptide组装期间有选择的反应.tet-butyl 酯(OTBU)保护碳箱酸组,加强有机溶剂中化合物的稳定性和溶解性.这种化合物表面上一般是白色到白的,在二氯甲烷和二甲基芳基胺等普通有机溶剂中溶解,在标准实验室条件下稳定,但应储存在一个冷干燥的地方防止降解.Fmoc-D-ASP-OTBU(OTBU)广泛用于固态浸硫化物合成,因为它与各种混合试剂的兼容性及其促进形成浸泡物联结的能力.这种化合物在表面上是白色至白色的,在二氯甲烷和二苯基化剂应用中可以进行高效的合成.

结构式图片

相似化合物

77004-75-2 4125-93-3 34582-32-6

上下游产品

L-Aspartic acid 9-fluorenylmethyl N-succinimidyl carbonate isobutene (S)-2-(9H-fluoren-9-ylmethoxycarbonylamino)succinic acid 4-benzyl ester 1-tert-butyl esterα-fluorenylmethoxycarbonyl-L-aspartic acid α-tert-butyl-β-pentafluorophenyl esterNα-fluorenylmethoxycarbonyl-L-aspartic acid α-tert-butyl-β-pentafluorophenyl ester N-α-9-fluorenylmethoxycarbonyl-aspartic acid methyl-6-O-carboxy-(N-(9-fluorenylmethoxycarbonyl)-L-aspartic-acid α-tert-butyl ester)-2,3,4-tri-O-benzyl-α-D-manno-pyranoside methyl-6-O-carboxy-(N-(9-fluorenylmethoxycarbonyl)-L-aspartic-acid α-tert-butyl ester)-2,3,4-tri-O-4-methoxybenzyl-α-D-manno-pyranoside

合成工艺路线路线简述

    9-芴甲基-N-琥珀酰亚胺基碳酸酯,(R)-Di-Tert-Butyl 2-Aminosuccinate置于copper(Ll) Sulfate Pentahydrate,Sodium Hydroxide,Edetate Disodium,Sodium Carbonate体系中,用 水,乙酸乙酯 用作溶剂,化学反应 3.0H,以72.3%的收率获得fmoc-D-天冬氨酸 1-叔丁酯
    参考文献:一种n-9-芴甲氧羰基-D-天门冬氨酸-4-叔丁酯
    标题:一种n-9-芴甲氧羰基-D-天门冬氨酸-4-叔丁酯
    摘要:本发明公开了一种n‑9‑芴甲氧羰基‑d‑天门冬氨酸‑4‑叔丁酯的制备方法,(A)向反应容器中加入醋酸叔丁酯,滴加催化剂,加入d‑天门冬氨酸,于20‑50oc反应,浓缩处理,得d‑天冬门氨酸二叔丁酯;(B)将d‑天门冬氨酸二叔丁酯加入到硫酸铜溶液中,调节ph值至4‑8,得到d‑天冬门氨酸二叔丁酯铜盐水溶液;(C)向d‑天冬门氨酸二叔丁酯铜盐水溶液中依次加入有机溶剂和乙二胺四乙酸二钠,搅拌均匀,再向溶液体系中加入芴甲氧羰酰琥珀酰亚胺,调节ph值至3‑5,静置分层,萃取,干燥有机层,过滤,有机层加入石油醚,搅拌结晶,得到n‑9‑芴甲氧羰基‑d‑天门冬氨酸‑4‑叔丁酯.本发明的制备方法在生产过程中避免消旋,提高产品的光学纯度.

    海关参考信息

    专利信息


    专利号:US-5218089-A
    优先权日:1988-12-23
    标 题 :Retro-inverso analogues of thymopentin and the method for their synthesis
    发明人:MARIOTTI SABINA; SISTO ALESSANDRO; NENCIONI LUCIANO; VILLA LUIGI; VERDINI ANTONIO S
    权利人:SCLAVO SPA
    摘要:New analogues of thymopentin (TP5) and of its tetrapeptide fragment (TP51-4) containing two non-contiguous retro-inverted bonds in the peptide chain are described which are of the general formula (I) (I) where R is hydrogen or an acyl radical, and R1 is an -OR2 group or an group where R2 is a hydrogen atom or a hydrocarbon radical, and R3 is a hydrogen atom or a hydroxyl group, and the corresponding pharmaceutically acceptable salts of acid or basic addition, possess immunomodulating activity.

    专利号:US-8338565-B2
    优先权日:2008-08-20
    标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha
    发明人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P
    权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP
    摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.

    专利号:US-9795613-B2
    优先权日:2014-12-10
    标题 :GLP-1 receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK
    权利人:CELGENE INT II SÀRL
    摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

    专利号:US-9598430-B2
    优先权日:2013-06-11
    标 题 :GLP-1 receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL
    权利人:RECEPTOS INC; CELGENE INT II SÀRL
    摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

    专利号:EP-0375058-B1
    优先权日:1988-12-23
    标 题 :New retro-inverso analogues of trymopentin, the method for their synthesis and their use in the preparation of pharmaceutical compositions
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    ✅ COA系统入驻 | 共享模式

    主要参考文献

    [参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.

    合成参考文献


    摘要:Yamada, H., Science of Synthesis, (2007) 30, 74.
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