Production Method 1

24424-99-5

4887-88-1

942590-05-8

Reaction Conditions

1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)pyridine Solvents: Dichloromethane ;  0.5 h, rt

Reference

Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation

Yang, Chengbin ; Xu, Chenyue; Li, Zhipeng; Chen, Yi; Wu, Tianze; et al, European Journal of Medicinal Chemistry, 2021, 223,

Production Method 2

24424-99-5

4887-88-1

942590-05-8

Reaction Conditions

1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)pyridine Solvents: Tetrahydrofuran ;  overnight, rt

Reference

Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors

Mortensen, Deborah S.; Perrin-Ninkovic, Sophie M.; Harris, Roy; Lee, Branden G. S.; Shevlin, Graziella; et al, Bioorganic & Medicinal Chemistry Letters, 2011, 21(22), 6793-6799

Production Method 3

24424-99-5

4887-88-1

942590-05-8

Reaction Conditions

1.1 Reagents: Triethylamine Solvents: Dichloromethane ;  0 °C; overnight, rt

Reference

Azabenzimidazoles as fatty acid synthase inhibitors and their preparation and use for the treatment of cancer

, World Intellectual Property Organization, , ,

Production Method 4

942590-05-8

Reaction Conditions

Reference

Preparation of 3-phenylhydantoins as cannabinoid receptor inhibitors

, World Intellectual Property Organization, , ,

Production Method 5

24424-99-5

1810037-62-7

942590-05-8

1006899-77-9

Reaction Conditions

1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)pyridine Solvents: Tetrahydrofuran ;  overnight, rt

Reference

Preparation of 3-substituted indole derivatives for the treatment of HIV, depression and obesity

, World Intellectual Property Organization, , ,

Production Method 6

24424-99-5

4887-88-1

942590-05-8

1006899-77-9

Reaction Conditions

1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)pyridine Solvents: Tetrahydrofuran ;  overnight, rt

Reference

Preparation of 4-oxoquinolizines as antimicrobials

, World Intellectual Property Organization, , ,

Production Method 7

24424-99-5

4887-88-1

942590-05-8

Reaction Conditions

1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)pyridine Solvents: Tetrahydrofuran ;  4 h, rt

Reference

Deazapurines, thienopyrimidines and furopyrimidines as phosphoinositide 3-kinase inhibitors with a zinc binding moiety and their preparation and use in the treatment of diseases

, United States, , ,

Production Method 8

24424-99-5

4887-88-1

942590-05-8

Reaction Conditions

1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)pyridine Solvents: Tetrahydrofuran ;  4 h, rt

Reference

Treatment of cancers having k-ras mutations using PI3 kinase and HDAC inhibitors and preparation of bifunctional thienopyrimidine compounds that inhibit both enzymes

, World Intellectual Property Organization, , ,

Production Method 9

24424-99-5

4887-88-1

942590-05-8

Reaction Conditions

1.1 Reagents: Triethylamine Solvents: Tetrahydrofuran ;  18 h, 25 °C

Reference

Heteroaryl compounds, compositions thereof, preparation and methods of treatment therewith

, World Intellectual Property Organization, , ,

Production Method 10

24424-99-5

4887-88-1

942590-05-8

Reaction Conditions

1.1 Catalysts: 4-(Dimethylamino)pyridine Solvents: Tetrahydrofuran ;  16 h, reflux

Reference

Pyrimidine derivatives that are useful in the treatment of diseases mediated by mTOR and/or PI3K enzyme and their preparation

, World Intellectual Property Organization, , ,

Production Method 11

24424-99-5

4887-88-1

942590-05-8

Reaction Conditions

1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)pyridine Solvents: Dichloromethane ;  20 h, rt

Reference

Preparation of substituted (cyclohexylcarbonylamino)thiophenecarboxylic acids as antiviral agents for the treatment of hepatitis C infection

, World Intellectual Property Organization, , ,

Production Method 12

24424-99-5

4887-88-1

942590-05-8

1006899-77-9

Reaction Conditions

1.1 Reagents: Triethylamine ,  4-(Dimethylamino)pyridine Solvents: Tetrahydrofuran ;  overnight, rt

Reference

"All-Aqueous" Tandem Boc-Deprotection and Alkylation of N-Boc-benzimidazole Derivatives under Visible Light with Alkyl Aryl Diazoacetates: Application to Site-Selective Insertion of Carbenes into the N-H Bond of Purines

Rath, Suchismita; Mohanty, Biswajit; Sen, Subhabrata, Journal of Organic Chemistry, 2023, 88(2), 1036-1048

Production Method 13

24424-99-5

4887-88-1

942590-05-8

1006899-77-9

Reaction Conditions

1.1 Reagents: 4-(Dimethylamino)pyridine Solvents: Dichloromethane

Reference

Aminomethylation of Aryl Bromides by Nickel-Catalyzed Electrochemical Redox Neutral Cross Coupling

Ma, Yueyue; Hong, Jufei; Yao, Xiantong; Liu, Chengyu; Zhang, Ling; et al, Organic Letters, 2021, 23(24), 9387-9392

Production Method 14

24424-99-5

4887-88-1

942590-05-8

1006899-77-9

Reaction Conditions

1.1 Reagents: Triethylamine Solvents: Dichloromethane ;  2 min, rt
1.2 0 °C; 4 h, rt

Reference

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

Hay, Duncan; Fedorov, Oleg; Filippakopoulos, Panagis; Martin, Sarah; Philpott, Martin; et al, MedChemComm, 2013, 4(1), 140-144

tert-Butyl 5-Bromo-1H-benzoDimidazole-1-carboxylate Raw materials

• Di-tert-butyl dicarbonate
• 5-Bromo-1H-benzimidazole
• 5-Bromo-2,3-dihydro-1H-benzimidazole

tert-Butyl 5-Bromo-1H-benzoDimidazole-1-carboxylate Preparation Products

• Tert-Butyl 6-bromo-1H-benzo[d]imidazole-1-carboxylate (1006899-77-9)
• tert-Butyl 5-Bromo-1H-benzoDimidazole-1-carboxylate (942590-05-8)

• 1. An approach for correlating the structural and electrical properties of Zr4+-modified SrBi4Ti4O15/SBT ceramic
  Priyambada Nayak,Tanmaya Badapanda,Anil Kumar Singh,Simanchalo Panigrahi RSC Adv., 2017,7, 16319-16331
• 2. An aptasensor for the detection of ampicillin in milk using a personal glucose meter
  Xixi Li,Nanwei Zhu,Ruohan Li,Qinpu Zhang Anal. Methods, 2020,12, 3376-3381
• 3. An integrated microfluidic 3D tumor system for parallel and high-throughput chemotherapy evaluation?
  Dan Liu,Rui Hu,Zhongchao Huang,Meilin Sun,Kai Han Analyst, 2020,145, 6447-6455
• 4. An integrated digital microfluidic chip for multiplexed proteomic sample preparation and analysis by MALDI-MS?
  Hyejin Moon,Aaron R. Wheeler,Robin L. Garrell,Chang-Jin “CJ” Kim Lab Chip, 2006,6, 1213-1219
• 5. An aptasensor for detection of potassium ions based on RecJf exonuclease mediated signal amplification
  Bidou Wang,Xifeng Chen Analyst, 2014,139, 5695-5699

• 863877-81-0(tert-Butyl 5-methyl-1H-benzo[d]imidazole-1-carboxylate)
• 705262-62-0(tert-Butyl 5-iodo-1H-benzo[d]imidazole-1-carboxylate)
• 297756-31-1(tert-Butyl 5-amino-1H-benzimidazole-1-carboxylate)
• 127119-07-7(tert-Butyl 1H-Benzodimidazole-1-carboxylate)
• 72473-85-9(1H-Benzimidazole-1-carboxylicacid, ethyl ester)
• 725237-71-8(tert-Butyl 5-(hydroxymethyl)-1H-benzo[d]imidazole-1-carboxylate)
• 105652-39-9(3,9-diethyltridecan-6-yl Benzimidazole-1-carboxylate)
• 1037207-08-1(tert-Butyl 5-(bromomethyl)-1H-benzo[d]imidazole-1-carboxylate)
• 139525-24-9(1H-Benzimidazole-1-carboxylic acid, 4-methyl-, 1,1-dimethylethyl ester)
• 1006899-77-9(Tert-Butyl 6-bromo-1H-benzo[d]imidazole-1-carboxylate)