- Pd(II)-Catalyzed asymmetric oxidative annulation of N-alkoxyheteroaryl amides and 1,3-dienes
-
The first Pd(II)-catalyzed asymmetric oxidative annulation of N-alkoxyaryl amides and 1,3-dienes is reported, which features particular applicability for quick assembly of different types of chiral heterocycles with high yields and enantioselectivities. A novel chiral pyridine-oxazoline bearing a methoxyl group at the C-5 position and a gem-dimethyl group on the oxazoline moiety was found to be crucial for conversion.
- Zhang, Tao,Shen, Hong-Cheng,Xu, Jia-Cheng,Fan, Tao,Han, Zhi-Yong,Gong, Liu-Zhu
-
supporting information
p. 2048 - 2051
(2019/03/29)
-
- Novel indole derivative and medicine containing the same (by machine translation)
-
[A] formation of Amyloid fibrils can be compounds, including therapeutic or prophylactic agent for neurodegenerative disease Amyloid fibrils formation inhibitor compound and of. (I) or its pharmaceutically acceptable compound represented by the formula [a] or a salt or solvate thereof includes the, Amyloid fibrils formation inhibitor. [R1 And R2 Each independently is H, an alkyl group, a cyano group or the like; R3 And R4 Each independently is H, or an alkyl group; R3 And R4 The, joint may form a ring; Ar1 And Ar2 The substituted or unsubstituted heteroaryl group are independently substituted/unsubstituted aryl groups /; X and Y are each independently a single bond, - (=O) - C etc., Z is O or CH2 ; N is an integer of 1 - 3][Drawing] no (by machine translation)
- -
-
Paragraph 0122; 0123
(2018/06/30)
-
- Me2AlCl-mediated carboxylation, ethoxycarbonylation, and carbamoylation of indoles
-
Various 1-methyl-, 1-triisopropylsilyl-, and 1-benzylindoles are carboxylated under CO2 pressure (3.0 MPa) with the aid of 1.0 molar equiv of Me2AlCl to give 1-substituted indole-3-carboxylic acids in good to excellent yields. Mechanistic studies suggest that the intermediate, an indol-3-ylaluminum ate complex, was reversibly formed by electrophilic addition of Me2AlCl to the substrate followed by deprotonation of the resulting adduct. This method is successfully extended to alkoxycarbonylation with ethyl chloroformate and carbamoylation with naphthalen-1-yl isocyanate, which afford ethyl indole-3-carboxylates and N-naphthalen-1-ylindole-3-carboxamides, respectively.
- Nemoto, Koji,Tanaka, Shinya,Konno, Megumi,Onozawa, Satoru,Chiba, Masafumi,Tanaka, Yuuki,Sasaki, Yosuke,Okubo, Ryo,Hattori, Tetsutaro
-
p. 734 - 745
(2016/01/15)
-
- Synthesis and biological evaluation of novel indole derivatives containing sulfonamide scaffold as potential tubulin inhibitor
-
Microtubule-targeted drugs play a critical role in various types of cancer therapy worldwide. In our study, a series of novel indole derivatives containing a sulfonamide scaffold were designed, synthesized and biologically evaluated as potential tubulin p
- Man, Ruo-Jun,Tang, Dan-Jie,Lu, Xiao-Yuan,Duan, Yong-Tao,Tao, Xiang-Xiang,Yang, Meng-Ru,Wang, Le-Le,Wang, Bao-Zhong,Xu, Chen,Zhu, Hai-Liang
-
p. 1759 - 1767
(2016/09/23)
-
- Hydroxamic acids block replication of hepatitis c virus
-
Intrigued by the role of protein acetylation in hepatitis C virus (HCV) replication, we tested known histone deacetylase (HDAC) inhibitors and a focused library of structurally simple hydroxamic acids for inhibition of a HCV subgenomic replicon. While known HDAC inhibitors with varied inhibitory profiles proved to be either relatively toxic or ineffective, structure-activity relationship (SAR) studies on cinnamic hydroxamic acid and benzo[b]thiophen-2-hydroxamic acid gave rise to compounds 22 and 53, which showed potent and selective anti-HCV activity and therefore are promising starting points for further structural optimization and mechanistic studies.
- Ai, Teng,Xu, Yanli,Qiu, Li,Geraghty, Robert J.,Chen, Liqiang
-
p. 785 - 800
(2015/01/30)
-
- Construction of indoloquinolinones via Pd(II)-catalyzed tandem CC/CN bond formation: Application to the total synthesis of isocryptolepine
-
Construction of indoloquinolinone skeleton via Pd-catalyzed tandem CC/CN bond formation has been achieved in moderate to good yields. The method was applied toward the total synthesis of the bioactive natural product isocryptolepine in good overall yields.
- Chen, Xuebing,Sun, Peng,Xu, Jinyi,Wu, Xiaoming,Kong, Lingyi,Yao, Hequan,Lin, Aijun
-
p. 7114 - 7117
(2015/01/08)
-
- Synthesis of 1-benzyl-3-[4-(aryl-1-piperazinyl) carbonyl]-1h-indoles. novel ligands with potential D4 dopaminergic activity
-
The synthesis of a series of functionalized 1-Benzyl-3-[4-Aryl-1- piperazingl]carbonyl-1H-Indoles 6(a-f), as a potential new class of bioactive ligands at D4 receptors is reported. The synthetic strategy took place through a five steps sequence
- Pessoa-Mahana, Hernan,Ignacio Cuevas,David Pessoa-Mahana,Araya-Maturana, Ramiro,Fajardo, Iriux Almodovar,Barria, Claudio Saitz
-
experimental part
p. 866 - 869
(2012/05/04)
-
- Effect of indole-3-acetic acid analogs on the differentiation of HL-60 cells
-
In continuing search for novel cell differentiation agents, a series of derivatives of indole-3-acetic acid and indole-3-carboxylic acid were prepared and tested against HL-60 cells for their differentiation and antiproliferation activities. Among them, N-ethyl-1-benzylindole-3-carboxamide (14) was the most potent, whereas N-methyl 1-benzylindole-3-acetamide (5) and N-methyl 1-benzylindole-3-carboxamide (13) synergistically potentiated with all-trans-retinoic acid to induce cell differentiation as well as antiproliferation. Our results indicate that these compounds are effective cell differentiation and antiproliferation agents in combination with retinoic acid.
- Lien, Jin-Cherng,Jiang, Yu-Dong,Chen, Chun-Jen,Kuo, Sheng-Chu,Huang, Li-Jiau
-
experimental part
p. 1160 - 1165
(2009/12/08)
-
- INDOL-3-YL-CARBONYL-SPIRO-PIPERIDINE DERIVATIVES AS V1A RECEPTOR ANTAGONISTS
-
The invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the spiro-piperidine head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, methods for preparing the compounds and pharmaceutical compositions, and their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders.
- -
-
Page/Page column 35
(2008/06/13)
-
- Indol-3-yl-carbonyl-piperidin-benzoimidazol derivatives
-
The present invention relates to Indol-3-yl-carbonyl-piperidin-benzoimidazol derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R7 are as defined herein. The invention
- -
-
Page/Page column 17
(2010/11/25)
-
- N-heteroaryl indole carboxamides and analogues thereof, for use as glucokinase activators in the treatment of diabetes
-
This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is benefical, such as diabetes. The compounds are of the general formula (I) wherein B is and A is heteroaryl as defined in the claims.
- -
-
Page/Page column 39; 41
(2010/02/11)
-
- VLA-4 INHIBITORS
-
The present invention relates to a compound represented by the following formula (I): (wherein, W represents WA-A1 -WB - (in which, WA is substituted or unsubstituted aryl, etc., A1 is -NR1-, single bond, -C(O)-, etc., and WB is substituted or unsubstituted arylene, etc.), R is single bond, -NH-, -OCH2-, alkenylene, etc., X is -C(O) -CH2-, etc., and M is, for example, the following formula: (in which, R11, R12 and R13 each independently represents hydrogen, hydroxyl, amino, halogen, etc., R14 is hydrogen or lower alkyl, Y represents -CH2-O-, etc., Z is substituted or unsubstituted arylene, etc., A2 is single bond, etc, and R10 is hydroxyl or lower alkoxy)), or salt thereof; and a medicament containing the same. This compound or salt thereof selectively inhibits binding of cell adhesion molecules to VAL-4 and exhibits high bioavailability so that it is useful as a preventive and/or remedy for inflammatory diseases, autoimmune diseases, metastasis, bronchial asthma, rhinostenosis, diabetes, and the like.
- -
-
-
- Syntheses and biological evaluation of indole-2 and 3-carboxamides: New selective cyclooxygenase-2 inhibitors
-
A series of indol-2 and 3-carboxamides were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2) and cyclooxygenase-1 (COX-1). Substitution on indol nitrogen with benzyl and p-fluorobenzyl group of indole-2 carboxamides 8, 10, 11 provides fairly active COX-2 enzyme inhibitors.
- Oelgen, Suereyya,Guener,Fabregat,Crespo,Nebioglu
-
p. 238 - 242
(2007/10/03)
-
- Chemoselective deprotection of benzyl esters in the presence of benzyl ethers, benzyloxymethyl ethers and N-benzyl groups by catalytic transfer hydrogenation
-
-COOBn, -PO(OH)OBn, -O-CBz and N-CBz groups are efficiently and chemoselectively deprotected in the presence of Bn and BOM ethers and N-Bn groups by hydrogenolysis under catalytic transfer hydrogenation using 10% palladium on carbon as the catalyst and cyclohexadiene as the hydrogen donor.
- Bajwa
-
p. 2299 - 2302
(2007/10/02)
-
- A New Synthesis of some Indolecarboxylic Acids
-
1-Substituted isatins are transformed into indole derivatives by means of ethyl chloroacetate.In fact, under the conditions of the Darzens reaction they give two glycidic ester isomers 4 and 5 which, by hydrolysis in alkaline medium, undergo a transposition to indole-2,3-dicarboxylic acids 2 together with minor amounts of indole-3-carboxylic acids 3.From isatin itself, 2,3-dicarboxyindole-1-acetic acid (6) was obtained.
- Baiocchi, Leandro,Giannangeli, Marilena
-
p. 1905 - 1909
(2007/10/02)
-
- Potential antitumor agents. XIII. Indole derivatives related to Lonidamine
-
The synthesis and the antitumor activities of 1-benzylindole-3-carboxylic acids are reported. Compound 16b, which bears at position 1 the same substituent as Lonidamine (1), proved to be the most active derivative.
- Andreani,Rambaldi,Bonazzi,Andreani,Bossa,Galatulas
-
p. 847 - 851
(2007/10/02)
-
