187264-03-5Relevant articles and documents
Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators
Singla, Ramit,Gupta, Kunj Bihari,Upadhyay, Shishir,Dhiman, Monisha,Jaitak, Vikas
, p. 266 - 277 (2017/12/06)
Ground breaking clinical therapeutic advances in the treatment of breast cancer (BC) is the introduction of selective estrogen receptor modulators (SERMs). We have expeditiously designed and synthesized indole-xanthendione hybrids by coalescing the indole
Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-α)
Singla, Ramit,Gupta, Kunj Bihari,Upadhyay, Shishir,Dhiman, Monisha,Jaitak, Vikas
, p. 206 - 219 (2018/02/10)
In the course of efforts to develop novel selective estrogen receptor modulators (SERMs), indole-benzimidazole hybrids were designed and synthesised by fusing the indole nucleus with benzimidazole. All the compounds were first inspected for anti-prolifera
Identification of novel indole based heterocycles as selective estrogen receptor modulator
Singla, Ramit,Prakash, Kunal,Bihari Gupta, Kunj,Upadhyay, Shishir,Dhiman, Monisha,Jaitak, Vikas
, p. 72 - 88 (2018/05/09)
In the present study, we have designed and synthesized indole derivatives by coalescing the indole nucleus with chromene carbonitrile and dihydropyridine nucleus. Two compounds 5c and 6d were selected from series I and II after sequential combinatorial li
Cycloaddition of in Situ Formed Azaoxyallyl Cations with 2-Alkenylindoles: An Approach to Tetrahydro-β-carbolinones
Zhang, Kaifan,Xu, Xiaoying,Zheng, Jiuan,Yao, Hequan,Huang, Yue,Lin, Aijun
, p. 2596 - 2599 (2017/05/24)
A novel [3 + 3] cycloaddition between in situ formed azaoxyallyl cations and 2-alkenylindoles has been developed. This concise method allows the efficient construction of a series of tetrahydro-β-carbolinones in good yields under mild conditions. Gram-sca
Fluorination-Oxidation of 2-Hydroxymethylindole Using Selectfluor
Jiang, Xiaojian,Zhang, Feng,Yang, Junjie,Yu, Pei,Yi, Peng,Sun, Yewei,Wang, Yuqiang
supporting information, p. 853 - 858 (2017/03/11)
An unexpected fluorination-oxidation of 2-hydroxymethylindole using selectfluor under mild condi-tions without a catalyst is described. This new chemistry allows for efficient and rapid synthesis of various 3-fluoroindole-2-aldehydes and novel quaternary
Facile Synthesis of 3-Halobenzo-heterocyclic-2-carbonyl Compounds via in situ Halogenation-Oxidation
Jiang, Xiaojian,Yang, Junjie,Zhang, Feng,Yu, Pei,Yi, Peng,Sun, Yewei,Wang, Yuqiang
supporting information, p. 2678 - 2683 (2016/09/03)
A facile method to synthesize 3-halobenzo-heterocyclic-2-carbonyl compounds is described. Mechanistic studies suggested that a halo-cyclization process, which generated the unstable spiro-acetal transition state and readily convertible to the corresponding carbonyl compound might be involved. Diverse 3-halobenzo-heterocyclic-2-carbonyl compounds could be synthesized with up to 95 % yield in mild conditions with inexpensive starting materials. (Figure presented.).
Rh(II)-catalyzed intramolecular annulation of N-sulfonyl 1,2,3-triazoles with indole derivatives: A new method for synthesis pyranoindoles
Xie, Hui,Yang, Jian-Xin,Bora, Pranjal Protim,Kang, Qiang
supporting information, p. 3014 - 3021 (2016/05/19)
A direct and highly stereoselective approach for the synthesis of Z-alkenyl-pyranoindoles had been developed by utilizing Rh(II)-catalyzed intramolecular cyclization of N-sulfonyl-1,2,3-triazoles with indole derivatives. A variety of pyranoindoles were obtained in 44-93% yields. Moreover, a more convenient synthesis of pyranoindoles starting from terminal alkyne was realized via a Cu-Rh sequentially catalyzed one-pot cascade reaction.
Zinc-Catalyzed Alkyne Oxidation/C-H Functionalization: Highly Site-Selective Synthesis of Versatile Isoquinolones and β-Carbolines
Li, Long,Zhou, Bo,Wang, Yong-Heng,Shu, Chao,Pan, Yi-Fei,Lu, Xin,Ye, Long-Wu
supporting information, p. 8245 - 8249 (2015/07/07)
An efficient zinc(II)-catalyzed alkyne oxidation/C￡H functionalization sequence was developed, thus leading to highly site-selective synthesis of a variety of isoquinolones and β-carbolines. Importantly, in contrast to the well-established gold-catalyzed intermolecular alkyne oxidation, over-oxidation can be completely suppressed in this system and the reaction most likely proceeds by a Friedel-Crafts-type pathway. Mechanistic studies and theoretical calculations are described.
Studies toward the synthesis of (R)-(+)-harmicine
Mo, Fanyang,Li, Fei,Qiu, Di,Zhang, Yan,Wang, Jianbo
, p. 2297 - 2302,6 (2020/09/16)
The study toward the total synthesis of (R)-(+)-harmicine is reported in this paper. The enantioselective synthesis of pyrrolidinone, the main backbone of of (R)-(+)-harmicine, has been completed by the methodology based on photo-induced Wolff rearrangement of α-diazo-β-carbonyl compounds. Copyright
Synthesis of carbazoles by gold(I)-catalyzed carbocyclization of 2-(enynyl)indoles
Praveen, Chandrasekaran,Perumal, Paramasivan Thirumalai
, p. 521 - 524 (2011/04/17)
A new synthetic protocol for carbazoles through gold(I)-catalyzed intramolecular hydroarylation of (Z)-2-(enynyl)indoles was achieved in good yields. The requisite (Z)-2-(enynyl)indoles were synthesized stereoselectively by trimethylgallium-promoted, Z-selective Wittig olefination of N-alkylindole-2-carboxaldehydes with propargyl ylides. Substrates possessing both alkyl as well as aromatic groups are well tolerated under these reaction conditions. Georg Thieme Verlag Stuttgart.
