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C16H20N2O5, triclinic, P1‾ $P\overline{1}$ (no. 2), a = 7.9179(7) Å, b = 10.1982(9) Å, c = 10.4144(8) Å, α = 76.184(7)°, β = 87.090 (7)°, γ = 73.500(8)°, V = 782.86(12) Å3, Z = 2, R gt(F) = 0.0458, wR ref(F 2) = 0.1333, T = 93 K.

Despite the attractive properties of tetrafluorosulfanyl (SF4) compounds in drug discovery, medicinal research on SF4 molecules is hindered by the scarcity of suitable synthetic methodologies. Drawing inspiration from the well‐established Sonogashira cross‐coupling of terminal alkynes under Pd‐catalysis, it is envisioned that SF4‐alkynes can serve as effective coupling partners. To overcome the challenges associated with the electron‐deficient nature of SF4‐alkynes and the lability of the SF4 unit under transition‐metal catalysis, an aryl radical mediated Csp–Csp3 cross‐coupling reaction is successfully developed under Cu catalysis. This methodology facilitates the coupling of SF4‐alkynes with alkyl iodides, leading to the immediate synthesis of SF4‐attached drug‐like molecules. These findings highlight the potential impact of SF4‐containing molecules in the drug industry, paving the way for further research in this emerging field. [ABSTRACT FROM AUTHOR]

C16H20N2O5, triclinic, P 1 ‾ (no. 2), a = 7.9179(7) Å, b = 10.1982(9) Å, c = 10.4144(8) Å, α = 76.184(7)°, β = 87.090 (7)°, γ = 73.500(8)°, V = 782.86(12) Å3, Z = 2, Rgt(F) = 0.0458, wRref(F2) = 0.1333, T = 93 K. [ABSTRACT FROM AUTHOR]

C16H20N2O5, triclinic, P 1 ‾ (no. 2), a = 7.9179(7) Å, b = 10.1982(9) Å, c = 10.4144(8) Å, α = 76.184(7)°, β = 87.090 (7)°, γ = 73.500(8)°, V = 782.86(12) Å3, Z = 2, Rgt(F) = 0.0458, wRref(F2) = 0.1333, T = 93 K. [ABSTRACT FROM AUTHOR]

A multifaceted approach comprising MCR (multicomponent reaction), amination and stereoselective reduction reactions was used to synthesize new pyrrolidine-based iminosugars. The key step of this strategy involves the contruction of a highly functionalised pyrroldine ring skeleton through MCR approach. Subsequently, amination and reduction reactions to the ring skeleton provide a quick access to new pyrrolidine-based imino sugars. The iminosugars were then tested against alpha glucosidase activity in which one compound (4-((4-methoxyphenyl)amino)pyrrolidin-3-ol), was found to be the most potent at low dosage. [ABSTRACT FROM AUTHOR]

We present a viable approach for the cross-dehydrogenative coupling of Het-SF 4 -alkynes with tetrahydroisoquinolines under oxidative conditions, using TBHP and copper catalysts. These newly developed conditions boast enhanced yields and a more extensive range of substrates, demonstrating tolerance to various functional groups and addressing the limitations of earlier reports. Consequently, this method should increase opportunities for the exploration of SF 4 -containing compounds and their potential applications in drug discovery, materials science, and as alternatives to PFAS.

Despite the attractive properties of tetrafluorosulfanyl (SF 4 ) compounds in drug discovery, medicinal research on SF 4 molecules is hindered by the scarcity of suitable synthetic methodologies. Drawing inspiration from the well-established Sonogashira cross-coupling of terminal alkynes under Pd-catalysis, it is envisioned that SF 4 -alkynes can serve as effective coupling partners. To overcome the challenges associated with the electron-deficient nature of SF 4 -alkynes and the lability of the SF 4 unit under transition-metal catalysis, an aryl radical mediated C sp -C sp 3 cross-coupling reaction is successfully developed under Cu catalysis. This methodology facilitates the coupling of SF 4 -alkynes with alkyl iodides, leading to the immediate synthesis of SF 4 -attached drug-like molecules. These findings highlight the potential impact of SF 4 -containing molecules in the drug industry, paving the way for further research in this emerging field., (© 2023 The Authors. Advanced Science published by Wiley-VCH GmbH.)

The asymmetric unit of the title compound, C 9 H 15 NO 4 , consists of a functionalized pyrrolidine ring having an envelope conformation, synthesized as an ethyl ester. The mol-ecule has three chiral centres and crystallized as a racemic mixture. In the crystal, mol-ecules are linked by pairwise O-H⋯O bonds, generating dimers with twofold rotational symmetry., (© Abdul id et al. 2023.)