甲硅烷基烯醇醚5和β-内酰胺9(R = Me 3 Si)偶联得到酮13a-d。化合物13a,13c和13d转化为三环内酰胺16-20、23-25。(光学纯的甲硅烷基烯醇醚5的化学酶法合成可得到同手性内酰胺23-25。)此外,酮氮杂环丁酮13被保护为1,3-恶唑烷30。使用Bouffard方法进行所需的立体化学反应,得到醇32。形成相应的碳酸硝基苄酯,脱保护和氧化提供了酮35a和35b,其随后分别转化为三苯甲基41a和41b。
甲硅烷基烯醇醚5和β-内酰胺9(R = Me 3 Si)偶联得到酮13a-d。化合物13a,13c和13d转化为三环内酰胺16-20、23-25。(光学纯的甲硅烷基烯醇醚5的化学酶法合成可得到同手性内酰胺23-25。)此外,酮氮杂环丁酮13被保护为1,3-恶唑烷30。使用Bouffard方法进行所需的立体化学反应,得到醇32。形成相应的碳酸硝基苄酯,脱保护和氧化提供了酮35a和35b,其随后分别转化为三苯甲基41a和41b。
[EN] NUCLEIC ACID CHEMICAL MODIFICATIONS<br/>[FR] MODIFICATIONS CHIMIQUES D'ACIDE NUCLÉIQUE
申请人:ALNYLAM PHARMACEUTICALS INC
公开号:WO2010101951A1
公开(公告)日:2010-09-10
he present invention provides nucleosides of formula (1) and oligonucleotides comprising at least on nucleoside of formula (2): Another aspect of the invention relates to a method of inhibiting the expression of a gene in cell, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
Regioselective Amination or Alkoxylation of Halogenated Amino-, Thio- or Alkoxypyridines via Pyridyne Intermediates
作者:Paul Knochel、Benjamin Heinz、Dimitrije Djukanovic、Fiona Siemens、Mohamed Idriess、Benjamin Martin
DOI:10.1055/s-0037-1610786
日期:2022.11
bearing an R-substituent in position 2 (R = OEt, NEt2, N-piperidyl, or SEt) or in position 5 (R = OMe, OEt, SEt, NMe2, NEt2, or aryl) with KHMDS and an amine at 25 °C for 12 hours in THF provided regioselectively 3- and 4-aminated pyridines in 56–90% yields. The reaction of 3-bromo-2-diethylaminopyridine with various alcohols in the presence of t-BuOK/18-crown-6 in THF at 80 °C for 20–60 hours gave various
3-(5-HYDROXY-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF
申请人:Novartis AG
公开号:US20200017461A1
公开(公告)日:2020-01-16
The present disclosure provides a compound of Formula (I′):
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R
x
, X
1
, X
2
, and R
1
are as defined herein, and methods of making and using same.
CYCLOALKYL CONTAINING THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS
申请人:LEHMANN-LINTZ Thorsten
公开号:US20110217311A1
公开(公告)日:2011-09-08
The present invention relates to novel thienopyrimidine compounds of general formula
pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2
a
or Mnk2
b
) and/or variants thereof.
Synergistic effects of Ni and acid sites for hydrogenation and C–O bond cleavage of substituted phenols
作者:Wenji Song、Yuanshuai Liu、Eszter Baráth、Chen Zhao、Johannes A. Lercher
DOI:10.1039/c4gc01798f
日期:——
catalysts containing Ni and/or HZSM-5 in the aqueous phase. The aromatic ring of phenol is hydrogenated in the first step, and the C–O bond of the resulting cyclohexanol is dehydrated in sequence. The initial turnover frequency (TOF) of phenol hydrodeoxygenation increases in parallel with the acid site concentration irrespective of the concentration of the accessible surface Ni atoms. For catechol and