18990-98-2Relevant articles and documents
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Nikishin,G.I.,Vorob'ev,V.D.
, (1962)
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2,6-Bis(trifluoromethyl)phenylboronic Esters as Protective Groups for Diols: A Protection/Deprotection Protocol for Use under Mild Conditions
Shimada, Naoyuki,Urata, Sari,Fukuhara, Kenji,Tsuneda, Takao,Makino, Kazuishi
, p. 6064 - 6068 (2018/09/27)
The application of 2,6-bis(trifluoromethyl)phenyl boronic acid (o-FXylB(OH)2; o-FXyl = 2,6-(CF3)2C6H3) as a recoverable and reusable protective agent for diols is described. The resulting cyclic boronic esters are water- and air-stable and tolerant to various organic transformations. Moreover, they can be deprotected under mild conditions. This methodology was applied to the synthesis of a highly conjugated enetriyne natural product with anti-angiogenic activities.
Maximizing the potency of siRNA lipid nanoparticles for hepatic gene silencing in vivo
Jayaraman, Muthusamy,Ansell, Steven M.,Mui, Barbara L.,Tam, Ying K.,Chen, Jianxin,Du, Xinyao,Butler, David,Eltepu, Laxman,Matsuda, Shigeo,Narayanannair, Jayaprakash K.,Rajeev, Kallanthottathil G.,Hafez, Ismail M.,Akinc, Akin,Maier, Martin A.,Tracy, Mark A.,Cullis, Pieter R.,Madden, Thomas D.,Manoharan, Muthiah,Hope, Michael J.
supporting information; experimental part, p. 8529 - 8533 (2012/10/18)
Special (lipid) delivery: The role of the ionizable lipid pKa in the in?vivo delivery of siRNA by lipid nanoparticles has been studied with a large number of head group modifications to the lipids. A tight correlation between the lipid pKa?value and silencing of the mouse FVII gene (FVII ED50) was found, with an optimal pKa range of 6.2-6.5 (see graph). The most potent cationic lipid from this study has ED50 levels around 0.005?mg?kg?1 in mice and less than 0.03?mg?kg?1 in non-human primates.