- Synthesis process of ezutromid
-
The invention discloses a synthesis process of ezutromid, and relates to the field of drug synthesis. 4-mercaptophenol and an ethyl halide are taken as raw materials, a compound 2 is prepared, then acompound 3 is prepared through nitration, a compound 4 o
- -
-
Paragraph 0034; 0035; 0042; 0043; 0048; 0049
(2019/11/20)
-
- Selective Late-Stage Oxygenation of Sulfides with Ground-State Oxygen by Uranyl Photocatalysis
-
Oxygenation is a fundamental transformation in synthesis. Herein, we describe the selective late-stage oxygenation of sulfur-containing complex molecules with ground-state oxygen under ambient conditions. The high oxidation potential of the active uranyl cation (UO22+) enabled the efficient synthesis of sulfones. The ligand-to-metal charge transfer process (LMCT) from O 2p to U 5f within the O=U=O group, which generates a UV center and an oxygen radical, is assumed to be affected by the solvent and additives, and can be tuned to promote selective sulfoxidation. This tunable strategy enabled the batch synthesis of 32 pharmaceuticals and analogues by late-stage oxygenation in an atom- and step-efficient manner.
- Li, Yiming,Rizvi, S. Aal-e-Ali,Hu, Deqing,Sun, Danwen,Gao, Anhui,Zhou, Yubo,Li, Jia,Jiang, Xuefeng
-
supporting information
p. 13499 - 13506
(2019/08/21)
-
- The influence of electronic perturbations on the Sulfur-Fluorine Gauche Effect Dedicated to Prof. Dr. Antonio Togni on the occasion of his 60th birthday.
-
Herein, a solution phase NMR conformer population analysis is employed to probe the effect of remote electronic perturbations on the conformational equilibria of a series of para-substituted β-fluorosulfides (1), sulfoxides (2) and sulfone derivatives (3). Conformations that allow for stabilizing stereoelectronic (σC-H → σ?C-F) and electrostatic (Fδ-...Sδ+) interactions predominate: this is consistent with the Sulfur-Fluorine Gauche Effect. The molar fractions (χ) of the two possible gauche conformers correlate linearly with the electron-withdrawing aptitude of the para-substituent, rendering the system ideally suited for a Hammett-type analysis. Despite the clear influence that the remote para-substituents have on conformer population, this is superseded by the oxidation state on sulfur (II, IV, VI), where an increased preference for the gauche conformer follows the trend: sulfide sulfone sulfoxide. It is envisaged that this proof of concept in controlling conformer population, either by proximal (oxidation state) or remote tuning (para-substituent), will find application in molecular design.
- Thiehoff, Christian,Schifferer, Lukas,Daniliuc, Constantin G.,Santschi, Nico,Gilmour, Ryan
-
supporting information
p. 121 - 126
(2016/01/25)
-
- 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
-
The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
- -
-
Page/Page column 94
(2015/11/10)
-
- Chemoselectivity as a delineator of cuprate structure in Catalytic 1,4-Addition of Diorganozinc reagents to michael acceptors
-
Reaction of the cyclic thioacetal (RS)2CHCHO [R = 1/2x-(CH 2)3] with HCCCOMe, followed by treatment with TsCl/DABCO (Ts = tosyl, DABCO= 1,4-diazabicyclo[2.2.2]octane) affords the mono-protected 1,4-benzoquinone dithioaceta
- Welker, Matthias,Woodward, Simon,Veiros, Luis F.,Calhorda, Maria Jose
-
experimental part
p. 5620 - 5629
(2010/07/16)
-
- The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators
-
The optimization of a series of benzimidazole glucokinase activators is described. We identified a novel and potent achiral benzimidazole derivative as an allosteric GK activator. This activator was designed and synthesized via removal of the chiral center of the lead compound, 6-(N-acylpyrrolidin-2-yl)benzimidazole. The activator exhibited good PK profiles in rats and dogs, and significant hypoglycemic efficacy at 1 mg/kg po dosing in a rat OGTT model. The binding site and binding mode of the benzimidazole class of GKA with GK protein was confirmed by X-ray crystallographic analysis.
- Takahashi, Keiji,Hashimoto, Noriaki,Nakama, Chisato,Kamata, Kenji,Sasaki, Kaori,Yoshimoto, Riki,Ohyama, Sumika,Hosaka, Hideka,Maruki, Hiroko,Nagata, Yasufumi,Eiki, Jun-ichi,Nishimura, Teruyuki
-
experimental part
p. 7042 - 7051
(2010/01/06)
-
- Mercapto phenolic and alkylthio phenolic antioxidants
-
2-Mercapto phenol and/or 4-mercapto phenol are reacted with a compound selected from olefins, alcohols, and organic halides for example, styrene and isobutylene, to form (hydrocarbyl) thio phenolic antioxidants such as 2,6-di-tert. butyl-4-(tert.butylthio) phenol and 2,6-di(α-phenylethyl)-4-(α-phenylethylthio)phenol.
- -
-
-