872492-58-5Relevant academic research and scientific papers
Accessing Unsymmetrically Linked Heterocycles through Stereoselective Palladium-Catalyzed Domino Cyclization
Arora, Ramon,Lautens, Mark,Rodríguez, José F.,Whyte, Andrew
supporting information, (2021/12/09)
A palladium-catalyzed strategy is presented to synthesize unsymmetrically linked heterocycles within stereoselective tetrasubstituted olefins. This reaction is proposed to occur via a vinyl-PdII intermediate capable of initiating the cyclizatio
Cycloisomerization of Carbamoyl Chlorides in Hexafluoroisopropanol: Stereoselective Synthesis of Chlorinated Methylene Oxindoles and Quinolinones
Bajohr, Jonathan,Lautens, Mark,Mirabi, Bijan,Rodríguez, José F.,Whyte, Andrew,Zhang, Anji
supporting information, p. 18478 - 18483 (2021/07/19)
Hexafluoroisopropanol (HFIP) was employed as an additive for the generation of 3-(chloromethylene)oxindoles via the chloroacylation of alkyne-tethered carbamoyl chlorides. This reaction avoids the use of a metal catalyst and accesses products in high yields and stereoselectivities. Additionally, this reaction is scalable and proved amenable to a series of product derivatizations, including the synthesis of nintedanib. The reactivity of alkene-tethered carbamoyl chlorides with hexafluoroisopropanol (HFIP) was harnessed towards the synthesis of 2-quinolinones.
ACLY INHIBITORS AND USES THEREOF
-
Paragraph 00743, (2020/06/01)
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.
Gold(I)-Catalyzed Cascade Cyclization of Anilines with Diynes: Controllable Formation of Eight-Membered Ring-Fused Indoles and Propellane-Type Indolines
Yamaguchi, Ayuta,Inuki, Shinsuke,Tokimizu, Yusuke,Oishi, Shinya,Ohno, Hiroaki
, p. 2543 - 2559 (2020/03/13)
Heterocycle-fused indoles or indolines are distributed widely in a variety of natural products, bioactive agents, and pharmaceuticals. Herein, we describe the development of gold-catalyzed cascade reactions of anilines with diynes to form eight-membered r
Cp?Rh(iii) catalyzed: Ortho -halogenation of N -nitrosoanilines by solvent-controlled regioselective C-H functionalization
Peng, Qiujun,Hu, Jian,Huo, Jiyou,Yuan, Hongshun,Xu, Lanting,Pan, Xianhua
, p. 4471 - 4481 (2018/06/29)
We present a novel, efficient, and regioselective method for the rhodium-catalyzed direct C-H ortho-halogenation of anilines that involves a removable N-nitroso directing group. This method featured mild reaction conditions, wide substrate scope, good functional group tolerance and satisfactory yields. To maintain the high ortho-regioselectivity and conversion, increasing the steric hindrance of the solvent was critical. Preliminary mechanistic studies suggest that C-H activation may be involved in the rate-determining step.
A catalyst-free and additive-free method for the synthesis of benzothiazolethiones from: O -iodoanilines, DMSO and potassium sulfide
Zhu, Xiaoming,Li, Wenguang,Luo, Xiai,Deng, Guobo,Liang, Yun,Liu, Jianbing
supporting information, p. 1970 - 1974 (2018/05/23)
Under catalyst-free and additive-free conditions, a novel, convenient, eco-friendly method for the synthesis of benzothiazolethiones has been developed. The three-component reaction of o-iodoanilines and K2S with DMSO proceeded smoothly and the corresponding benzothiazolethiones were obtained with good isolated yields. Meanwhile, this method could be used for the synthesis of thioureas from primary diamines. Furthermore, mechanism research showed that DMSO not only functioned as a carbon source, but also as a mild oxidant in this reaction.
Copper-Catalyzed Three-Component Synthesis of Benzothiazolethiones from o-Iodoanilines, Isocyanide, and Potassium Sulfide
Dang, Pan,Zeng, Weilan,Liang, Yun
supporting information, p. 34 - 37 (2015/07/28)
An efficient copper catalyzed strategy for the synthesis of a variety of benzothiazolethione derivatives has been developed. In the presence of CuCl, the three-component reaction of o-iodoanilines and K2S with p-toluenesulfonylmethyl isocyanide proceeded smoothly to obtain the corresponding benzothiazolethiones in good to excellent isolated yields. Notably, isocyanide functioned as a carbon source and K2S functioned as a sulfur source in this reaction.
A CuAAC/Ullmann C-C coupling tandem reaction: Copper-catalyzed reactions of organic azides with N -(2-Iodoaryl)propiolamides or 2-iodo- N -(prop-2-ynyl)benzenamines
Cai, Qian,Yan, Jiajie,Ding, Ke
supporting information; experimental part, p. 3332 - 3335 (2012/08/28)
A novel copper-catalyzed tandem reaction was developed by utilizing two famous copper-catalyzed reactions, CuAAC and Ullmann coupling. The trapping of the C-Cu intermediate produced in CuAAC led to further formation of an aryl C-C bond through intramolecu
DIPEPTIDE ANALOGS AS COAGULATION FACTOR INHIBITORS
-
Page/Page column 169, (2009/01/23)
Disclosed are novel dipeptide analogs compounds of Formula (I), (II) or (III) or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, which are inhibitors of factor XIa and/or plasma kallikrein, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of thrombotic diseases.
A valuable synthesis of pyrrolo[1,2-a]quinoxalines, indolo[1,2-a] quinoxalines and their aza-analogues by palladium-catalyzed intramolecular carbon-nitrogen bond formation
Abbiati, Giorgio,Beccalli, Egle M.,Broggini, Gianluigi,Paladino, Giuseppe,Rossi, Elisabetta
, p. 2881 - 2886 (2007/10/03)
A novel and efficient method for the construction of pyrrolo[1,2-a] quinoxalines, indolo[1,2-a]quinoxalines and their aza-analogues is described. The reaction involves a Pd-catalyzed intramolecular cyclization as the key step and provides the desired prod
