40913-43-7Relevant academic research and scientific papers
Synthesis of Carbazoles and Dihydrocarbazoles by a Divergent Cascade Reaction of Donor-Acceptor Cyclopropanes
Faltracco, Matteo,Damian, Matteo,Ruijter, Eelco
supporting information, p. 7592 - 7596 (2021/10/12)
An alkylation/olefination cascade of indolecarboxaldehydes and phosphonate-functionalized donor-acceptor cyclopropanes affords functionalized dihydrocarbazoles and cyclohepta[cd]indoles in formal (3 + 3) and (4 + 3) cycloadditions. A minor modification to the reaction conditions also allows access to the fully aromatic heterocyclic scaffolds by thermal loss of an electron-rich aryl moiety.
HETEROCYCLIC COMPOUNDS AS PAD INHIBITORS
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Paragraph 000313, (2019/04/16)
Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis.
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
BENZOIMIDAZOLE DERIVATIVES AS PAD4 INHIBITORS
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Page/Page column 72, (2016/12/07)
Compounds of formula (I): wherein X, Y, R1 and R3-R11 are as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
Gold(I)-catalyzed rearrangement of alkynylaziridine indoles for the synthesis of spiro-tetrahydro-β-carbolines
Yang, Yan-Fang,Li, Lian-Hua,He, Yu-Tao,Luo, Jian-Yi,Liang, Yong-Min
supporting information, p. 702 - 707 (2014/02/14)
Functionalized spiro-tetrahydro-β-carbolines were formed by an efficient gold(I)-catalyzed rearrangement reaction of alkynylaziridine indoles. The reaction involved a Friedel-Crafts type intramolecular reaction of alkynylaziridine indoles, following by hydroamination of aminoallene intermediate.
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.
BENZENESULFONAMIDE COMPOUNDS AS EDG-1 ANTAGONISTS USEFUL IN THE TREATMENT OF CANCER
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Page/Page column 37-38, (2008/12/05)
This invention relates to novel compounds of formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess Edg-1 antagonistic activity and are accordingly useful in the treatment and/or prophylaxis of canc
Lithiation of Heterocycles Directed by α-Amino Alkoxides
Comins, Daniel L.,Killpack, Michael O.
, p. 104 - 109 (2007/10/02)
The addition of heterocyclic aromatic aldehydes to certain lithium dialkylamides gave α-amino alkoxides that were ring-lithiated with butyllithium.Alkylation and hydrolysis provided ring-substituted heterocyclic aromatic aldehydes via a one-pot reaction.The metalation of α-amino alkoxides derived from thiophenecarboxaldehydes, furaldehydes, N-methylpyrrolecarboxaldehydes, and indolecarboxaldehydes was examined.The regioselectivity of the lithiation, was dependent on the heterocycle, the amine component of the α-amino alkoxide, and the metalation conditions.A novel N-methyl metalation of α-amino alkoxides derived from N-methylpyrrole-2-carboxaldehyde and N-methylindole-2-carboxaldehyde was achieved when N,N,N'-trimethylethylenediamine was used as the amine component for in situ formation of the α-amino alkoxides.The novel directed N-methyl lithiations are attributed to an intramolecular TMEDA-like assisted metalation.
