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Showing 1–9 of 9 results
Advanced filters: Author: Rohan R. Merchant Clear advanced filters

  • Bicyclo[1.1.1]pentane (BCP) is a valuable three-dimensional bioisostere of benzene. This Perspective highlights emerging, propellane-free strategies to access multisubstituted and bridge-functionalized BCP derivatives, assesses their scope and limitations, and outlines remaining challenges.

    • Chang Liu
    • Wenyuan Li
    • Tian Qin
    ReviewsOpen Access
    Nature Communications
    Volume: 17, P: 1-11

  • The pentafluorosulfanyl group has been long considered a potential (bio)isostere for tert-butyl and trifluoromethyl groups, yet limitations in methodologies have constrained access to it. Here, the authors report a general pentafluorosulfanylation platform that employs bench-stable solid reagents to generate SF5 radicals via a decarboxylation and β-scission sequence.

    • Renzhe Li
    • Chang Liu
    • Tian Qin
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-8

  • The bicyclo[1.1.1]pentane (BCP) motif has drawn increasing attention recently in drug discovery. Now, a programmable bis-functionalization strategy has been developed to modularly access bridge-substituted BCP scaffolds, based on the inherent chemoselectivity of BCP bis-boronates (3° > 2°). This strategy should enable further structure–activity relationship studies of BCP-containing drug candidates and open the door to unexplored chemical space.

    • Yangyang Yang
    • Jet Tsien
    • Tian Qin
    Research
    Nature Chemistry
    Volume: 16, P: 285-293

  • Direct and stereospecific C(sp3)–C(sp2) cross-coupling reactions are highly desirable for the construction of complex molecular scaffolds. Now, using stable and easily accessible alkyl sulfinates as coupling reagents, a modular and programmable sulfurane-mediated coupling method has been developed for the installation of various hindered alkyl bioisosteres, such as trifluoromethyl cyclopropyl, to (hetero)aromatics.

    • Min Zhou
    • Jet Tsien
    • Tian Qin
    Research
    Nature Chemistry
    Volume: 15, P: 550-559

  • Bicyclic hydrocarbons, and bicyclo[1.1.1]pentanes in particular, are playing an emerging role as saturated bioisosteres in pharmaceutical, agrochemical and materials intramolecular coupling approach has been developed for the modular construction of underexplored multisubstituted strained bicyclic hydrocarbons, ranging from [1.1.1] to [3.2.1] scaffolds.

    • Yangyang Yang
    • Jet Tsien
    • Tian Qin
    Research
    Nature Chemistry
    Volume: 13, P: 950-955

  • Starting with alkyl carboxylic acids, a simple olefin synthesis using any substitution pattern or geometry, based on amide-bond synthesis with nickel- or iron-based catalysis, is described.

    • Jacob T. Edwards
    • Rohan R. Merchant
    • Phil S. Baran
    Research
    Nature
    Volume: 545, P: 213-218

  • The FANTOM4 study identified transcriptional start sites active during proliferation arrest and differentiation of the human monocytic cell line THP-1. Systematic knockdown of 52 transcription factors provide support for their model in which a complex transcriptional network regulates the differentiation process.

    • Harukazu Suzuki
    • Alistair R R Forrest
    • Yoshihide Hayashizaki
    Research
    Nature Genetics
    Volume: 41, P: 553-562

  • In this Review, synthetic approaches to polycyclic scaffolds, which can act as saturated, three-dimensional bioisosteric replacements of ortho-substituted, meta-substituted and multi-substituted benzenes, are discussed. Their application in medicinal chemistry is also summarized.

    • Jet Tsien
    • Chao Hu
    • Tian Qin
    Reviews
    Nature Reviews Chemistry
    Volume: 8, P: 605-627