- α-Oxocarboxylic Acids as Three-Carbon Insertion Units for Palladium-Catalyzed Decarboxylative Cascade Synthesis of Diverse Fused Heteropolycycles
-
A novel palladium-catalyzed decarboxylative cascade cyclization for the assembly of diverse fused heteropolycycles by employing α-oxocarboxylic acids as three-carbon insertion units is reported. This protocol enables the synthesis of isoquinolinedione- and indolo[2,1-a]isoquinolinone-fused benzocycloheptanones in moderate to good yields by the use of different aryl iodides, including alkene-tethered 2-iodobenzamides and 2-(2-iodophenyl)-1H-indoles. Notably, the approach achieves simultaneous construction of both six- and seven-membered rings via sequential intramolecular carbopalladation, C-H activation, and decarboxylation.
- Zhou, Liwei,Qiao, Shujia,Zhou, Fengru,Xuchen, Xinyu,Deng, Guobo,Yang, Yuan,Liang, Yun
-
supporting information
p. 2878 - 2883
(2021/05/05)
-
- Atmosphere-Controlled Palladium-Catalyzed Divergent Decarboxylative Cyclization of 2-Iodobiphenyls and α-Oxocarboxylic Acids
-
A novel palladium-catalyzed divergent decarboxylative cyclization of 2-iodobiphenyls and α-oxocarboxylic acids utilizing the atmosphere as a controlled switch is reported. Under the protection of a nitrogen atmosphere, tribenzotropones are synthesized by a [4 + 3] decarboxylative cyclization. Employing a palladium/O2 system enables a [4 + 2] decarboxylative cyclization to assemble triphenylenes. Notably, preliminary mechanistic studies indicate that the formation of triphenylenes involves a double decarboxylation.
- Zhou, Liwei,Sun, Mingjie,Zhou, Fengru,Deng, Guobo,Yang, Yuan,Liang, Yun
-
supporting information
p. 7150 - 7155
(2021/09/18)
-
- QUINOXALINE DERIVATIVES
-
The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
- -
-
Page/Page column 79; 80
(2021/07/24)
-
- The intramolecular reaction of acetophenoneN-tosylhydrazone and vinyl: Br?nsted acid-promoted cationic cyclization toward polysubstituted indenes
-
In the presence of TsNHNH2, a Br?nsted acid-promoted intramolecular cyclization ofo-(1-arylvinyl) acetophenone derivatives was developed, leading to polysubstituted indenes with complexity and diversity in moderate to excellent yields. In sharp contrast with either the radical or carbene involved cyclization of aldehydicN-tosylhydrazone with vinyl, a cationic cyclization pathway was involved, whereN-tosylhydrazone served as an electrophile and alkylation reagent during this transformation.
- Wang, Zhixin,Li, Yang,Chen, Fan,Qian, Peng-Cheng,Cheng, Jiang
-
p. 1810 - 1813
(2021/02/27)
-
- Divergent Access to Benzocycles through Copper-Catalyzed Borylative Cyclizations
-
A copper-catalyzed chemodivergent approach to five- and six-membered benzocycles from dienyl arenes tethered with a ketone has been developed. Through proper choice of coordinating ligands and catalytic conditions, copper-catalyzed borylative cyclization of a single dienyl arene can be diverted to two different pathways, leading to indanols and dihydronaphthalenols with high stereoselectivity. The chiral bidentate bisphosphine ligand (S,S)-Ph-BPE was optimal for asymmetric copper-allyl addition to a tethered ketone via a boat-like transition state, whereas NHC ligands led to boro-allyl addition producing indanols with high diastereoselectivity. (Figure presented.).
- Yoon, Wan Seok,Han, Jung Tae,Yun, Jaesook
-
supporting information
p. 4953 - 4959
(2021/09/14)
-
- Asymmetric Synthesis and Application of Chiral Spirosilabiindanes
-
Reported here is the development of a class of chiral spirosilabiindane scaffolds by Rh-catalyzed asymmetric double hydrosilation, for the first time. Enantiopure SPSiOL (spirosilabiindane diol), a new type of chiral building block for the preparation of various chiral ligands and catalysts, was readily prepared on greater than 10 gram scale using this protocol. The potential of this new spirosilabiindane scaffold in asymmetric catalysis was preliminarily demonstrated by development of the corresponding monodentate phosphoramidite ligands (SPSiPhos), which were used in both a Rh-catalyzed hydrogenation and a Pd-catalyzed intramolecular carboamination.
- Chang, Xin,Chen, Hong-Chao,Li, Chuan-Ying,Ma, Pei-Long,Wang, Peng
-
supporting information
p. 8937 - 8940
(2020/04/30)
-
- Organic compound having tetrahedron-like configuration
-
The present invention relates to an organic compound having a tetrahedron-like configuration, wherein the organic compound has a structure represented by the following general formula (I) defined in the specification, A1-A4 are respectively and independently an unsaturated five-membered ring or an unsaturated six-membered ring, B is a direct bond , -C, -O-, -N-, -S-, or -C=C-, m is 0 or 1, Ris hydrogen, fluorine, substituted or unsubstituted C1-C12 alkyl, or substituted or unsubstituted C6-C12 aryl, and n is an integer of 0-2. The organic compound of the present invention has excellentphotoelectric property.
- -
-
Paragraph 0250; 0252; 0253
(2018/07/07)
-
- Organic compound with tetrahedral-like geometry
-
An organic compound with a tetrahedral-like geometry is disclosed. The organic compound has a structure represented by formula (I): wherein A1 to A4 each independently represent a 5-membered or 6-membered unsaturated ring; B1 represents direct bonding, —C—, —O—, —N—, —S— or —C═C—; m is 0 or 1; each of Ra's is independently hydrogen, fluorine, oxygen, substituted or unsubstituted C1-C12 alkyl or substituted or unsubstituted C6-C12 aryl; and n is an integer of 0 to 2.
- -
-
Page/Page column 62; 63
(2018/03/25)
-
- PdII-Catalyzed Oxidative Tandem aza-Wacker/Heck Cyclization for the Construction of Fused 5,6-Bicyclic N,O-Heterocycles
-
A PdII-catalyzed oxidative tandem cyclization was developed for the construction of fused 5,6-bicyclic N, O-heterocycles. This reaction was enabled by the combined use of a 3-methylpyridine ligand and pentafluorobenzoic acid additive. A range of heterocyclic products with different substituents could be prepared in moderate to good yields via this methodology. Several transformations, including a scaled-up preparation of product 2 a, were also carried out showing the good applicability of our methodology.
- Ye, Chenghao,Kou, Xuezhen,Xia, Jingzhao,Yang, Guoqiang,Kong, Li,Wei, Quhao,Zhang, Wanbin
-
supporting information
p. 1897 - 1901
(2018/07/31)
-
- Preparation of isoindolinones via a palladium-catalyzed diamination
-
A Pd(II)-catalyzed cyclization using oxidative olefin diamination was developed for the preparation of isoindolinones from ortho-olefinic N-methoxybenzamides. Using the optimized reaction conditions, the desired products were obtained in up to 90% yield using NFSI as the oxidant. This reaction provides an efficient and direct access to isoindolinones with amine functionality, an important drug skeleton.
- Li, Yu,Kou, Xuezhen,Ye, Chenghao,Zhang, Xinghua,Yang, Guoqiang,Zhang, Wanbin
-
supporting information
p. 285 - 288
(2017/01/03)
-
- Palladium-Catalyzed Aerobic Aminooxygenation of Alkenes for Preparation of Isoindolinones
-
A palladium-catalyzed intramolecular isoindolinone-forming aminooxygenation of alkenes with 1 atm of oxygen as oxidant is reported. A variety of functionalized alkenes and carboxylic acids can be used, and high yields were observed. Preliminary mechanistic studies revealed that the aminooxygenation products were formed through the oxidation of a C-PdII species using a strong oxidant, peroxide, which is generated in situ from a Pd(OAc)2/bpy/O2/HOAc catalytic system.
- Kou, Xuezhen,Li, Yu,Wu, Liang,Zhang, Xinghua,Yang, Guoqiang,Zhang, Wanbin
-
supporting information
p. 5566 - 5569
(2015/12/01)
-
- HETEROCYCLIC DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
-
Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, C═CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.
- -
-
Page/Page column 76
(2011/12/14)
-
- HETEROCYCLIC DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
-
Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1-substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N-CR5R6, C=CR5 or CR13-CR5R6, Y is a bond or -C(O)-, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.
- -
-
Page/Page column 132
(2010/09/17)
-
- Atroposelective radical aryl migration reactions from sulfur to carbon
-
The paper describes stereoselective radical aryl migration reactions from sulfur in sulfonates to aryl radicals for the synthesis of axially chiral biaryls. A chirality center in secondary benzylic sulfonates is used to diastereoselectively (atroposelectively) install a stereogenic axis via a 1,5 aryl migration reaction. Atroposelectivity has not been investigated in stereoselective radical chemistry before. Good yields (53-82%) but low selectivities (up to 2 to 1) were obtained.
- Schulte, Birte,Fr?hlich, Roland,Studer, Armido
-
experimental part
p. 11852 - 11859
(2009/04/07)
-