- Practical and Modular Construction of C(sp3)-Rich Alkyl Boron Compounds
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Alkyl boronic acids and esters play an important role in the synthesis of C(sp3)-rich medicines, agrochemicals, and material chemistry. This work describes a new type of transition-metal-free mediated transformation to enable the construction of C(sp3)-rich and sterically hindered alkyl boron reagents in a practical and modular manner. The broad generality and functional group tolerance of this method is extensively examined through a variety of substrates, including synthesis and late-stage functionalization of scaffolds relevant to medicinal chemistry. The strategic significance of this approach, with alkyl boronic acids as linchpins, is demonstrated through various downstream functionalizations of the alkyl boron compounds. This two-step concurrent cross-coupling approach, resembling formal and flexible alkyl-alkyl couplings, provides a general entry to synthetically challenging high Fsp3-containing drug-like scaffolds.
- Yang, Yangyang,Tsien, Jet,Ben David, Ayala,Hughes, Jonathan M. E.,Merchant, Rohan R.,Qin, Tian
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supporting information
p. 471 - 480
(2021/01/13)
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- Transition metal- And light-free radical borylation of alkyl bromides and iodides using silane
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We report operationally simple and neutral conditions for borylation of alkyl bromides and iodides to alkyl boronic esters under transition metal- and light-free conditions. A series of substrates with a wide range of functional groups were effectively transformed into the borylation products in moderate to good yields. Mechanistic studies, including radical clock experiments and DFT calculations, gave detailed insight into the radical borylation process.
- Mo, Fanyang,Sun, Beiqi,Zheng, Sihan
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supporting information
p. 5674 - 5677
(2021/06/16)
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- SUBSTITUTED BENZOIC ACIDS, INHIBITORS OF PHOSPHOLIPASES A2
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The compounds of formula I are potent inhibitors of phospholipases A 2 (PLA 2 's) and are therefore useful in the treatment of diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia, and trauma induced inflammation, such as spinal cord injury.
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