Herein, we report the first synthesis of difluoromethanesulfinate esters via the direct difluoromethanesulfinylation of alcohols with HCF2SO2Na/Ph2P(O)Cl. Primary, secondary, and tertiary alcohols ...were converted to the corresponding difluoromethanesulfinate esters in good to excellent yields under mild conditions. The late-stage functionalization of complexed biologically active natural products was also demonstrated. The method was extended to the trifluoromethanesulfinylation of alcohols using CF3SO2Na in the presence of a catalytic amount of Me3SiCl to provide trifluoromethanesulfinate esters.
Schistosomiasis is a neglected parasitic disease of major public health concern as it affects over 250 million people in developing countries. Currently there is no licensed vaccine available against ...schistosomiasis. The Schistosoma mansoni calpain protein, Sm-p80, is a leading vaccine candidate now ready to move to clinical trials. In order to better assess Sm-p80 vaccine immunogenicity; here we used a systems biology approach employing RNA-sequencing to identify gene signatures and epistatic interactions following Sm-p80 vaccination in mouse and baboon models that may predict vaccine efficacy. Recombinant Sm-p80 + CpG-oligodeoxynucleotide (ODN) vaccine formulation induced both cellular and humoral immunity genes with a predominant TH1 response as well as TH2 and TH17 gene signatures. Early gene responses and gene-network interactions in mice immunized with rSm-p80 + ODN appear to be initiated through TLR4 signaling. CSF genes, S100A alarmin genes and TNFRSF genes appear to be a signature of vaccine immunogenicity/efficacy as identified by their participation in gene network interactions in both mice and baboons. These gene families may provide a basis for predicting desirable outcomes for vaccines against schistosomiasis leading to a better understanding of the immune system response to vaccination.
Celotno besedilo
Dostopno za:
DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, SIK, UILJ, UKNU, UL, UM, UPUK
A novel HF2CSO2Na/Ph2PCl/Me3SiCl system is disclosed for the late-stage direct difluoromethylthiolation of Csp2 and Csp3 nucleophiles. Difluoromethylthiolation of phenols and naphthols proceeded ...nicely under this system to regioselectively provide corresponding SCF2H compounds in good yields. Other substrates such as indoles, pyrroles, pyrazoles, enamines, ketones, and β-keto esters were also transformed to corresponding SCF2H products in good yields. The late-stage direct difluoromethylthiolation of a number of natural products and pharmaceutically attractive molecules was also achieved.
Difluoromethanesulfonyl hypervalent iodonium ylides 2 were developed as electrophilic difluoromethylthiolation reagents for a wide range of nucleophiles. Enamines, indoles, β-keto esters, silyl enol ...ethers and pyrroles were effectively reacted with 2 affording desired difluoromethylthio (SCF2H)-substituted compounds in good to high yields under copper catalysis. The reaction of allyl alcohols with 2 under the same conditions provided difluoromethylsulfinyl (S(O)CF2H) products in good yields. The difluoromethylthiolation of enamines is particularly effective with wide generality, thus the enamine method was nicely extended to the synthesis of a series of difluoromethythiolated cyclic and acyclic β-keto esters, 1,3-diketones, pyrazole and pyrimidine derivatives by a consecutive, two-step one-pot reaction using 2.
Reported herein is a new approach for the asymmetric installation of a (tetrazolyl)methyl group via Si/F activation using organocatalytic kinetic resolution of racemic MBH-fluorides.
A novel HF
CSO
Na/Ph
PCl/Me
SiCl system is disclosed for the late-stage direct difluoromethylthiolation of C
and C
nucleophiles. Difluoromethylthiolation of phenols and naphthols proceeded nicely ...under this system to regioselectively provide corresponding SCF
H compounds in good yields. Other substrates such as indoles, pyrroles, pyrazoles, enamines, ketones, and β-keto esters were also transformed to corresponding SCF
H products in good yields. The late-stage direct difluoromethylthiolation of a number of natural products and pharmaceutically attractive molecules was also achieved.
The first electrophilic diastereoselective direct introduction of the difluoromethylthio group is described. We used a chiral auxiliary-based approach to illustrate the versatility of our recently ...developed difluoromethanesulfonyl hypervalent iodonium ylide reagents for the difluoromethylthiolation of indanone-based β-keto esters. Chiral SCF₂H-featuring compounds were obtained in up to 93% ee value.
Reported herein is a new approach for the asymmetric installation of a (tetrazolyl)methyl group
via
Si/F activation using organocatalytic kinetic resolution of racemic MBH-fluorides.
A new approach ...for the asymmetric installation of a (tetrazolyl)methyl group
via
Si/F activation using organocatalytic kinetic resolution of racemic MBH-fluorides.
This study focuses on critical analysis of the rights of an accused person during trial in Somalia. The rights of accused person in Somalia have become a contentious and serious issue owing to the ...on-going civil war in Somalia which has now lasted for two decades. The doctrinal research methodoly was used to collect and analyse the data used in the study. The relevant secondary data were collected through documetary review where relevant data was collected from different books, national and international legal statutues and scholarly publications of scholars in relation to the rights of an accused person during trial in Somalia. The study employed a systematic procedure to analyse documentary evidence and answer specific research questions in the study through repeated review, examination and interpretation of the data in order to gain meaning and empirical knowledge of the construct being studied. The study analysed the rights of an accused person under the various national laws of Somalia, the various forms of violation of the rights of an accused person in Somalia and the causes of the violation of the rights of an accused person in Somalia. The main findings of the study revealed that the various and sufficient rights of an accused person during train in Somalia, as provided by the Provisional Constitution of Somalia, 2012, and the Criminal Code Act of Somalia, 1963, include: right to liberty and security, right to be informed promptly of the offence charged, right to fair and speedy trial, right to humane treatment, the right to be presumed innocent until proven guilty, right to a fair hearing, right to defend himself or herself, right to counsel, right to be informed of the nature offense an accused person has committed, the right to an interpreter, the right to be present at the trial, right to be brought promptly before a capable court, the right to habeas corpus, the right to apply for bail, the right not to be compelled to testify against himself or herself, right to examine evidence or witnesses and the right to appeal. However, these rights are neither being promoted nor protected in Somalia; instead they are being violated in various ways which they encompass: violation of arrest procedures and unfair and cruel treatment of accused person, arbitrary arrest, denial of fair public trial, violation of trial procedures, unlawful treatment and detention of political prisoners and accused persons being caused by structural and legal ambiguity, the continuous practise of legal pluralism, the existence of broken chain in the justice system, high level of corruption and mismanagement, military interference. The study recommended that the Federal Government of Somalia through its three organs should enact new law, promote fair and procedural arrest of accused train and sensitise the people about their rights as an accused and should initiate good policies and project that can foster the promotion and protection of human rights in the sphere of accused person’s protection during and after trial in Somalia.
This study focuses on the European Union (EU)-Somalia cooperation: areas, achievements, challenges and opportunities. The main aim of the stud is to provide a comprehensive assessment of the areas, ...achievements, challenges, and opportunities of the European Union-Somalia cooperation. The study employed qualitative research approach to gain clear understanding on the areas, achievements, challenges, and opportunities of the cooperation between European Union and Somalia. The researcher used an extensive documentary review tool to gather existing knowledge and insights on the European Union-Somalia cooperation. The researcher reviewed academic articles, reports, policy documents, and other relevant sources to understand the areas, achievements, challenges, and opportunities of the cooperation between European Union and Somalia. The findings of the study on areas of cooperation between European Union and Somalia which they entail: governance and institutional development, security and counterterrorism, development assistance, humanitarian aid, trade and investment, migration and displacement and regional integration; the achievements of cooperation between the European Union (EU) and Somalia entail: security and stability, humanitarian assistance, governance and state building, development resilience, political dialogue and reconciliation; the challenges hindering the effectiveness of the cooperation between the European Union (EU) and Somalia encompass: security concerns, weak institutional capacity, political fragmentation, limited infrastructure and logistical challenges, corruption and lack of transparency and humanitarian crises and natural disasters; the opportunities of the cooperation between the European Union (EU) and Somalia entail: economic development and trade, capacity building and knowledge transfer, infrastructure development, humanitarian aid and resilience-building, peacebuilding and conflict resolution and educational skills development. The study recommended that there should be more strengthening of political dialogue, increasing financial support, enhancing capacity building, fostering economic development, strengthening security cooperation and promoting inclusive governance to promote effectiveness of the cooperation between the European Union (EU) and Somalia.
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