Using a proazaphosphatranecatalyst, P(RNCH2CH2)3N (R=Me, i-Pr), allylaromatics and allylphenyl sulfide were selectively isomerized to the corresponding vinyl isomers in yields up to >99% in CH3CN at 40 °C. Efficient transformation of allylphenylsulfone at ambient temperature afforded an isomerization/dimerization product in >95% yield. Conjugation of bis-allylmethylene double bond-containing compounds
P(MeNCH<sub>2</sub>CH<sub>2</sub>)<sub>3</sub>N: An Efficient Catalyst for the Desilylation of <i>tert</i>-Butyldimethylsilyl Ethers
作者:Zhengkun Yu、John G. Verkade
DOI:10.1021/jo991591i
日期:2000.4.1
in 68-94% yield in the presence of 0.2-0.4 equiv of P(MeNCH2CH2)3N. Using P(i-PrNCH2-CH2)3N as the catalyst, 85-97% yields of desilylated alcohols were obtained from TBDMS ethers of 1-octanol, 2-phenoxyethanol, and racemic alpha-phenyl ethanol. These are the first examples of desilylations of silyl ethers catalyzed by nonionic bases. Both catalysts were much less effective for the desilylation of t
Compositions and methods for silencing apolipoprotein B
申请人:Heyes James
公开号:US08865675B2
公开(公告)日:2014-10-21
The present invention provides compositions and methods for the delivery of interfering RNAs such as siRNAs that silence APOB expression in cells such as liver cells. In particular, the nucleic acid-lipid particles provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells such as liver cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of APOB at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.