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We report diverse C-N cross-coupling reactions of aryl thianthrenium salts that are formed site-selectively by direct C-H functionalization. The scope of N-nucleophiles ranges from primary and secondary alkyl and aryl amines to various N-containing heterocycles, and the overall transformation is applicable to late-stage functionalization of complex, drug-like small molecules.
This article was published in the following journal.
Name: Journal of the American Chemical Society
Incorporation of the CF3 group into arenes has found increasing importance in drug discovery. Here we report the first photoredox-catalyzed cross-coupling of aryl thianthrenium salts with a copper-bas...
The combination of commonly used FeCl3/SIPr with Ti(OEt)4/PhOM enabled a highly general iron-based catalyst system which could efficiently catalyze the biaryl coupling reaction between various electro...
We have reported a new late-stage functionalization of small peptides and cyclopeptides using readily prepared iodotyrosine or iodophenylalanine containing peptides and performing Negishi cross-coupli...
A transition-metal-free direct trifluoromethylthiolation of the -carbon of lithium aryl boronates with trifluoromethanesulfenate under mild conditions was described. In addition, late-stage site-selec...
Site-selective late-stage functionalizations of a pyrano[3,2-a]carbazole core related to the murrayamine natural products is reported. Specifically, selective C3 and C6 bromination has been achieved a...
The purpose of the Optimize RV Follow-Up study is to determine the long-term effect of selective site pacing. Selective site pacing refers to which area of the right ventricle the lead is ...
The purpose of the Optimize RV study is to determine the long-term effect of selective site pacing. Selective site pacing refers to which area of the right ventricle the lead is placed. T...
This study will evaluate the effect of the timing of treatment completion in two-staged selective laser trabeculoplasty therapy on intraocular pressure lowering effect.
This study evaluates four different doses of ACIT-1 for safety and for the ability to raise effective anti-cancer immune responses in patients with pancreatic and other late stage cancers....
RATIONALE: Gathering information over time about patients' sense of being a burden on their caregiver, and caregivers' sense of burden on themselves, may help doctors learn more about the ...
A pathologic change in leukemia in which leukemic cells permeate various organs at any stage of the disease. All types of leukemia show various degrees of infiltration, depending upon the type of leukemia. The degree of infiltration may vary from site to site. The liver and spleen are common sites of infiltration, the greatest appearing in myelocytic leukemia, but infiltration is seen also in the granulocytic and lymphocytic types. The kidney is also a common site and of the gastrointestinal system, the stomach and ileum are commonly involved. In lymphocytic leukemia the skin is often infiltrated. The central nervous system too is a common site.
Organic chemicals where aryl or alkyl groups are joined by two nitrogen atoms through a double bond (R-N=N-R'; R and R' may be either aryl or alkyl). They may be used as DYES.
The stage in the first meiotic prophase, following ZYGOTENE STAGE, when CROSSING OVER between homologous CHROMOSOMES begins.
The process of TOOTH formation. It is divided into several stages including: the dental lamina stage, the bud stage, the cap stage, and the bell stage. Odontogenesis includes the production of tooth enamel (AMELOGENESIS), dentin (DENTINOGENESIS), and dental cementum (CEMENTOGENESIS).
A 105-kDa serum glycoprotein with significant homology to the other late complement components, C7-C9. It is a polypeptide chain cross-linked by 32 disulfide bonds. C6 is the next complement component to bind to the membrane-bound COMPLEMENT C5B in the assembly of MEMBRANE ATTACK COMPLEX. It is encoded by gene C6.
Clinical Approvals Clinical Trials Drug Approvals Drug Delivery Drug Discovery Generics Drugs Prescription Drugs In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are dis...