120161-06-0Relevant academic research and scientific papers
Benzimidazole derivative and preparation method and application thereof
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Paragraph 0049; 0050; 0051, (2019/01/08)
The invention discloses a benzimidazole derivative and a preparation method and the application thereof. The prepared benzimidazole derivative is capable of effectively reducing the relapse arte afterabstaining from morphine addiction, has a remarkable ef
CuI-catalyzed amination of arylhalides with guanidines or amidines: A facile synthesis of 1-H-2-substituted benzimidazoles
Deng, Xiaohu,McAllister, Heather,Mani, Neelakandha S.
supporting information; experimental part, p. 5742 - 5745 (2009/12/06)
(Figure Presented) CuI/L5 (N,N′-dimethylethylenediamine) proves to be an efficient catalyst system for the amination of arylhalides with guanidines. The same catalyst system is then successfully applied to the one-step synthesis of 1-H-2-aminobenzimidazol
Synthesis of 1(11)H-2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole starting from benzimidazole-2-sulfonic acid. Intramolecular cyclization of 2-(δ-chlorobutylamino)benzimidazole
Anisimova,Kuz'Menko,Kuz'Menko,Morkovnik
, p. 2315 - 2322 (2008/09/18)
The intramolecular cyclization of 2-(δ-chlorobutylamino)benzimidazole (3c) follows the unusual pathway involving the predominant attack on the exocyclic amino group rather than on the much more nucleophilic endocyclic nitrogen atom. This reaction affords 2-pyrrolidinobenzimidazole and 1(11)H-2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole as the major product and the by-product, respectively. The cyclization can be directed exclusively toward the annulation of the diazepine ring only after the acetylation of the amino group of compound 3c. According to the quantum chemical calculations, the unusual regioselectivity of the cyclization of chloramine 3c is associated primarily with a substantially less steric strain and the higher entropy of pyrrolidine transition states compared to diazepine transition states.
Chloroformamidinium salts: Efficient reagents for preparation of 2-aminobenzoimidazole, 2-aminobenzoxazole, and 2-aminobenzothiazole derivatives
El-Faham, Ayman,Chebbo, Mohamed,Abdul-Ghani, Mohamed,Younes, Ghassan
, p. 599 - 606 (2007/10/03)
A Reaction involving chloroformamidinium salts (TCFH 1a, BTCFH 1b, DmCFH 1c, DmPCFH 1d, BPCFH 1e) and 2-aminophenol 9a, benzene-1,2-diamine 9b, and 2-aminothiophenol 9c afforded 2-aminobenzoxazole 13, 2-aminobenzoimidazole 14, and 2-aminobenzothiazole 15 derivatives, respectively as major products, due to the in situ heterocyclization with dimethylamine acting as the better leaving group. Attempts for preparation of 13-15 from the reaction of N,N-dimethyl carbomyl chloride 16 with 2-aminophenol 9a, benzene-1,2-diamine 9b, and 2-aminothiophenol 9c were unsuccessful, and gave the unexpected products benzoxazol-2-ol 18a, benzoimidazol-2-one 18b, and S-(2-amino-phenyl) N,N-dimethylthiocarbamate 19 respectively. On the other hand reaction of chloroformamidinium salts 1a-e with 3-benzyl-2-hydrazinoquinoxaline 3 and 1-hydrazinophthalazine hydrochloride 4 in the presence of triethylamine as a base, afforded the [1,2,4]triazolo derivatives 6 and 7 respectively in good yield and purity. These triazole derivatives were formed due to the strong tendency towards heterocyclization and substitution of dimethylamine group as a better leaving group.
Amide substituted imidazoquinolines
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, (2008/06/13)
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain amide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
Amide substituted imidazoquinolines
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, (2008/06/13)
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain amide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
Benzimidazoles/Imidazoles Linked to a Fibrinogen Receptor Antagonist Template Having Vitronectin Receptor Antagonist Activity
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, (2008/06/13)
Vitronectin receptor antagonists having the formula: STR1 which are useful for the treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporsis.
