The alkynylation is performed by treating a halopyridine 4 with an alkyne 13 ##STR46## wherein W and n are as above in an acid acceptor, e.g., a di- or trialkylamine, such as, diethylamine, dipropylamine, trimethylamine, triethylamine, or tripropylamine, in the presence of bis(triphen...
Trimethylgallium catalyzes the addition of 1-lithio-1-alkyne to oxiranes, affording 3-alkyn-1-ols in good to excellent yields. A mechanism including activation of the oxiranes by the coordination to trimethylgallium is proposed (Table 47).453,454 Similarly, regio- and stereoselective ring-openin...
By 1994, Cheresh and coworkers found that αvβ3-integrin plays a major role in angiogenesis, i.e., the sprouting of new vessels from existing ones (to be distinguished from de-novo formation of vasculature, called vasculogenesis) [16]. This process is not only of fundamental importance fo...
wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate...
The target SWCNTs hybrid material was prepared by the reaction of azido substituted SWCNTs with 1,6-diethynylpyrene containing double terminal alkyne groups via the azide-alkyne Huisgen cycloaddition (Click) reaction. The structure of the 1,6-diethynylpyrene compound was determined by different ...
This anti-human PD-L1 adnectin was then modified with DBCO-PEG4- Maleimide to introduce a strained alkyne bond. This was followed by copper-free click reaction with a 18F-labeled precursor to generate [18F]F-BMS-986192. This construct was studied in a mouse xenograft model with moderate, ...