[Research progress on artemisinin and its derivatives in treatment of orthopedics-related diseases].

As research into the mechanisms of orthopedic diseases continues to deepen, the shortcomings of traditional single-target the-rapies are becoming increasingly apparent. Consequently, the search for multi-target drugs has become the mainstream research direction for orthopedics-related diseases. Artemisinin, a sesquiterpene lactone compound extracted from Artemisia annua, has led to the gradual synthesis of various derivatives such as dihydroartemisinin, artesunate, artemether, and arteether.

Site-selective -difluoroallylation of unprotected peptides with 3,3-difluoroallyl sulfonium salts.

Bench-stable 3,3-difluoroallyl sulfonium salts (DFASs), featuring tunable activity and their editable C-β and -difluoroallyl group, proved to be versatile fluoroalkylating reagents for site-selective -difluoroallylation of cysteine residues in unprotected peptides. The reaction proceeds with high efficiency under mild conditions (ambient temperature and aqueous and weak basic conditions). Various protected/unprotected peptides, especially bioactive peptides, are site-selectively -difluoroallylated.

Copper Difluorocarbene Enables Catalytic Difluoromethylation.

Despite the synthetic versatility of difluorocarbene, its high reactivity severely regulates widespread applications of difluorocarbene in organic synthesis. Here, we report a copper difluorocarbene-involved catalytic coupling, representing a new mode of the difluoromethylation reaction. This method allows difluoromethylation of a wide range of readily available allyl/propargyl electrophiles with NaBHCN and low-cost difluorocarbene precursor BrCFCOK, featuring high cost-efficiency, high stereo- and regioselectivities, and high functional group tolerance, even with complex drug-like molecules.

Historic dog Furs Unravel the Origin and Artificial Selection of Modern Nordic Lapphund and Elkhound dog Breeds.

The origins and extreme morphological evolution of the modern dog breeds are poorly studied because the founder populations are extinct. Here, we analyse eight 100 to 200 years old dog fur samples obtained from traditional North Swedish clothing, to explore the origin and artificial selection of the modern Nordic Lapphund and Elkhound dog breeds. Population genomic analysis confirmed the Lapphund and Elkhound breeds to originate from the local dog population, and showed a distinct decrease in genetic diversity in agreement with intense breeding.

Late-stage -difluoroallylation of phenol in bioactive molecules and peptides with 3,3-difluoroallyl sulfonium salts.

An efficient method for the late-stage selective -fluoroalkylation of tyrosine residues with a stable yet highly reactive fluoroalkylating reagent, 3,3-difluoroallyl sulfonium salts (DFASs), has been developed. The reaction proceeds in a mild basic aqueous buffer (pH = 11.6) with high efficiency, high biocompatibility, and excellent regio- and chemoselectivity.

Synthesis of α-Trifluoromethyl Alkynes through Fluoroalkynylation of -Difluoroalkenes.

A trifluoromethylalkynylation reaction of -difluoroalkenes with alkynyl sulfoxide by photoredox radical addition with good functional group tolerance in moderate to high yields, is developed for the synthesis of α-trifluoromethyl alkyne. This reaction features simple operation and inexpensive raw materials and provides an expeditious route to synthesize biologically relevant fluorine-containing alkynyl compounds with diverse structural skeletons.

3,3-Difluoroallyl Sulfonium Salts: Practical and Bench-Stable Reagents for Highly Regioselective gem-Difluoroallylations.

The site-selective introduction of the difluoromethylene group into organic molecules has important applications in producing pharmaceuticals and agrochemicals. However, the general and efficient methods that can construct both C(sp )-CF R and C(sp )-CF R bonds remain challenging. Here, we disclose a new type of practical and bench-stable difluoroalkylating reagent 3,3-difluoroallyl sulfonium salt (DFAS) that can be practically prepared from inexpensive and bulk chemical feedstock 3,3,3-trifluoropropene.