The present invention relates to a sodium salt represented by average formula (I):
(wherein, m
1
, n
1
, m
2
and n
2
respectively and independently represent a positive number of
0
0r
2
or less, provided that m
1
+n
1
=2, m
2
+n
2
=2, 0
本发明涉及一种由平均式(I)表示的钠盐:(其中,m1、n1、m2和n2分别独立地表示00r2或更小的正数,前提是m1+n1=2,m2+n2=2,0
PROCESS FOR PRODUCTION OF LIPID A ANALOGUE
申请人:Eisai R&D Management Co., Ltd.
公开号:EP1939209A1
公开(公告)日:2008-07-02
Discloses is a process for producing α-D-glucopyranose, 3-O-decyl-2-deoxy-6-O-[2-deoxy-3-O-[(3R)-3-methoxydecyl]-6-O-methyl-2-[(11Z)-1-oxo-11-octadecenyl]amino]-4-O-phosphono-β-D-glucopyranosyl]-2-[(1,3-dioxotetradecyl)amino]- or 1-(dihydrogen phosphate) tetrasodium salt which is useful as an active ingredient of a pharmaceutical or an intermediate for the synthesis thereof, which is environment-friendly and excellent in safety, operationality and reproducibility. A process for producing a compound represented by the formula (I) comprising the steps of reacting a compound represented by the formula (VIII) with a palladium catalyst in the presence of a nucleopholic agent and treating the product with a sodium source.
本发明公开了一种制备α-D-葡萄糖吡喃糖,3-O-癸基-2-脱氧-6-O-[2-脱氧-3-O-[(3R)-3-甲氧基癸基]-6-O-甲基-2-[(11Z)-1-氧代-11-十八碳烯基]氨基]-4-O-膦酸-β-D-葡萄糖吡喃糖-2-[(1,3-二氧代-四十碳基)氨基]-或1-(二氢磷酸)四钠盐的方法,该方法可用作制药活性成分或其合成中间体,具有环保、安全、易操作和重复性优异的特点。一种制备式(I)化合物的方法,包括以下步骤:在核苷酸试剂的存在下,用钯催化剂反应式(VIII)化合物,并用钠源处理产物。
SODIUM SALT OF DISACCHARIDE COMPOUND, METHOD FOR PRODUCING THE SAME, AND USE OF THE SAME
申请人:Eisai R&D Management Co., Ltd.
公开号:EP2096116A1
公开(公告)日:2009-09-02
Abstract: Disclosed are a sodium salt represented by the average formula (I) below, and a method for producing such a sodium salt. (In the formula, m1, n1 m2 and n2 independently represent 0 or a positive number not greater than 2, while satisfying m1 + n1 = 2, m2 + n2 = 2, 0 < m1 + m2 < 4 and 0 < n1 + n2 < 4) Also disclosed is a decomposition suppression method which makes a sodium salt represented by average formula (I) coexist with a sodium salt represented by the general formula (IV) below. This method enables improvement of long-term stability of a sodium salt represented by general formula (IV).
摘要:本发明公开了一种由以下平均式(I)表示的钠盐,以及生产这种钠盐的方法。(式中,m1、n1 m2 和 n2 分别代表 0 或不大于 2 的正数,同时满足 m1 + n1 = 2,m2 + n2 = 2,0 < m1 + m2 < 4 和 0 < n1 + n2 < 4)还公开了一种分解抑制方法,该方法可使由平均式(I)表示的钠盐与由以下通式(IV)表示的钠盐共存。该方法可提高通式(IV)所代表的钠盐的长期稳定性。
Method for producing polyether carbonate polyols
申请人:Covestro Deutschland AG
公开号:US10040901B2
公开(公告)日:2018-08-07
The invention relates to a method for producing polyether carbonate polyols by binding alkylene oxides and carbon dioxide to one or more H-functional starter substance/s in the presence of a double metal cyanide (DMC) catalyst, characterized in that (y) one or more H-functional starter substance/s and DMC catalyst are continuously metered into the reactor during the binding process, and the free alkylene oxide concentration in the reaction mixture amounts to 1.5 to 5.0 wt %, and the obtained reaction mixture is continuously discharged from the reactor.
本发明涉及一种在双金属氰化物(DMC)催化剂存在下,通过将氧化亚烷和二氧化碳与一种或多种 H-官能起始物质结合而生产聚醚碳酸酯多元醇的方法,其特征在于:(y) 在结合过程中,将一种或多种 H-官能起始物质和 DMC 催化剂连续计量到反应器中,反应混合物中的游离氧化亚烷浓度为 1.5 至 5.0 wt %,得到的反应混合物连续从反应器中排出。
Engineering Orthogonal Polypeptide GalNAc-Transferase and UDP-Sugar Pairs
作者:Junwon Choi、Lauren J. S. Wagner、Suzanne B. P. E. Timmermans、Stacy A. Malaker、Benjamin Schumann、Melissa A. Gray、Marjoke F. Debets、Megumi Takashima、Jase Gehring、Carolyn R. Bertozzi
DOI:10.1021/jacs.9b04695
日期:2019.8.28
O-Linked alpha-N-acetylgalactosamine (O-GalNAc) glycans constitute a major part of the human glycome. They are difficult to study because of the complex interplay of 20 distinct glycosyltransferase isoenzymes that initiate this form of glycosylation, the polypeptide N-acetylgalactosaminyltransferases (GalNAc-Ts). Despite proven disease relevance, correlating the activity of individual GalNAc-Ts with biological function remains challenging due to a lack of tools to probe their substrate specificity in a complex biological environment. Here, we develop a "bump-hole" chemical reporter system for studying GalNAc-T activity in vitro. Individual GalNAc-Ts were rationally engineered to contain an enlarged active site (hole) and probed with a newly synthesized collection of 20 (bumped) uridine diphosphate N-acetylgalactosamine (UDP-GalNAc) analogs to identify enzyme-substrate pairs that retain peptide specificities but are otherwise completely orthogonal to native enzyme-substrate pairs. The approach was applicable to multiple GalNAc-T isoenzymes, including GalNAc-T1 and -T2 that prefer nonglycosylated peptide substrates and GalNAcT-10 that prefers a preglycosylated peptide substrate. A detailed investigation of enzyme kinetics and specificities revealed the robustness of the approach to faithfully report on GalNAc-T activity and paves the way for studying substrate specificities in living systems.
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