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71.
72.
Malay Patra Larissa S. Eichenberger Gregor Fischer Jason P. Holland 《Angewandte Chemie (International ed. in English)》2019,58(7):1928-1933
Monoclonal antibodies (mAbs), immunoglobulin fragments, and other proteins are important scaffolds in the development of radiopharmaceuticals for diagnostic immuno‐positron emission tomography (immuno‐PET) and targeted radioimmunotherapy (RIT). Conventional methods for radiolabelling proteins with metal ions such as 68Ga, 64Cu, 89Zr, and 90Y require multi‐step procedures involving pre‐purification, functionalisation with a chelate, and subsequent radiolabelling. Standard coupling chemistries are time‐consuming, difficult to automate, and involve synthesis, isolation, and storage of an intermediate, new molecular entity (the conjugated mAb) whose biochemical properties can differ from those of the parent protein. To circumvent these issues, we developed a photoradiochemical approach that uses fast, chemoselective, light‐induced protein modification under mild conditions with novel metal‐ion‐binding chelates derivatised with aryl azide (ArN3) groups. Experiments show that one‐pot photochemical conjugation and radiolabelling of formulated mAbs can be achieved in <20 min. 相似文献
73.
Olga Bakhanovich Dr. Petr Beier 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(4):773-782
Organic α-fluorinated azidoalkanes appeared in the literature for the first time half a century ago. However, for a long time they remained undeveloped and were regarded as chemical curiosities. Recent advances in the preparation of α-fluorinated azidoalkanes as well as studies on their stability and reactivity opened up their broader synthetic potential for the preparation of valuable fluorinated and non-fluorinated compounds. 相似文献
74.
Enantioselective Copper‐Catalyzed Azide–Alkyne Click Cycloaddition to Desymmetrization of Maleimide‐Based Bis(alkynes) 下载免费PDF全文
Tao Song Dr. Li Li Dr. Wei Zhou Dr. Zhan‐Jiang Zheng Dr. Yuan Deng Dr. Zheng Xu Prof. Dr. Li‐Wen Xu 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(2):554-558
A copper catalyst system derived from TaoPhos and CuF2 was used successfully for catalytic asymmetric Huisgen [3+2] cycloaddition of azides and alkynes to give optically pure products containing succinimide‐ and triazole‐substituted quaternary carbon stereogenic centers. The desired products were obtained in good yields (60–80 %) and 85:15 to >99:1 enantiomeric ratio (e.r.) in this click cycloaddition reaction. 相似文献
75.
Dirhodium(II) Carboxylate Catalyzed Formation of 1,2,3‐Trisubstituted Indoles from Styryl Azides 下载免费PDF全文
Crystalann Jones Quyen Nguyen Prof. Dr. Tom G. Driver 《Angewandte Chemie (International ed. in English)》2014,53(3):785-788
Dirhodium(II)‐carboxylate complexes were discovered to promote the selective migration of acyl groups in trisubstituted styryl azides to form 1,2,3‐trisubstituted indoles. The styryl azides are readily available in three steps from cyclobutanone and 2‐iodoaniline. 相似文献
76.
Domino Staudinger/aza‐Wittig/Mannich Reaction: An Approach to Diversity of Di‐ and Tetrahydropyrrole Scaffolds 下载免费PDF全文
Dr. Anna S. Pavlova Dr. Olga A. Ivanova Dr. Alexey O. Chagarovskiy Nikolay S. Stebunov Dr. Nikolay V. Orlov Dr. Alexey N. Shumsky Dr. Ekaterina M. Budynina Dr. Victor B. Rybakov Prof. Dr. Igor V. Trushkov 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(50):17967-17971
A highly efficient and selective domino reaction producing valuable di‐ and tetrahydropyrrole‐based skeletons from azidoethyl‐substituted CH‐acids and (thio)carbonyl compounds has been developed. By involving the additional functional groups in starting compounds into the domino reaction or postmodification of the primary reaction products, the simple construction of the pharmaceutically relevant three‐ and polycyclic azaheterocyclic scaffolds was demonstrated. 相似文献
77.
Tatsumi Ochiai Dr. Daniel Franz Dr. Elisabeth Irran Prof. Dr. Shigeyoshi Inoue 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(18):6704-6707
The novel amino(imino)stannylene 1 was prepared by conversion of HNIPr (NIPr=bis(2,6‐diisopropylphenyl)imidazolin‐2‐imino) with one equivalent of Lappert’s tin reagent (Sn[N(SiMe3)2]2). Treatment of 1 with DMAP (4‐dimethylaminopyridine) yields its Lewis acid–base adduct 2 . The reaction of 1 with one equivalent of trimethylsilyl azide results in replacement of the amino group at the tin center by an N3 substituent with concomitant elimination of N(SiMe3)3 to afford dimeric [N3SnNIPr]2 ( 3 ). Remarkably, the reaction of 1 with B(C6F5)3 produces the novel tin(II) monocation 4 +[MeB(C6F5)3]? comprising a four‐membered stannacycle through methyl‐abstraction from the trimethylsilyl group. 相似文献
78.
Ekaterina Chainikova Sergey Khursan Alfia Yusupova Alexander Lobov Marat Abdullin Rustam Safiullin 《Tetrahedron letters》2018,59(34):3267-3271
During the photooxidation of aromatic azides containing a secondary N–H bond at the para-position, a sequence of intramolecular transformations of nitroso oxides led to the formation of heterocyclic oximes along with the corresponding nitroso and nitro compounds. 相似文献
79.
We present here the first examples of Cu–azide compounds synthesized by using protonated diamine ions as cationic templates: (dmenH2)[Cu6(N3)14] and (trimenH2)[Cu6(N3)14] (dmenH22+: N,N′‐dimethylethylenediammonium; trimenH22+: N,N,N′‐trimethylethylenediammonium). Both compounds possess a similar, rarely observed anionic Cu–azide layer, which consists of [Cu6(N3)142?]n anionic chains linked by asymmetric end‐to‐end azido bridges. The chain, in turn, is made up of elongated Cu6 rings, with double and single end‐on azido linkages between the square‐planar Cu2+ sites within the ring and double end‐on azido bridges serially connecting the rings. The molecular geometry results in ferromagnetic interactions within the Cu–azide layer in both compounds. The interlayer separations are determined by the cations, with the shortest interlayer Cu???Cu separations being 8.016 Å for the dmenH22+ compound and 9.106 Å for the trimenH22+ compound. These different interlayer separations tune the magnetic properties of the two materials. The dmenH22+ compound displays long‐range antiferromagnetic ordering at lowtemperature and short‐range ferromagnetic interaction at high temperature, while only short‐range ferromagnetism was observed in the trimenH22+compound at 2–300 K. 相似文献
80.