93-84-5 (5-硝基-2-苯咪唑酮,5-nitro-2,3-dihydro-1H-1,3-benzodiazol-2-one)

反应条件：

1.1 Reagents: Nitric acid Solvents: Water ; 1 h, 45 - 70 °C; 1 h, 60 - 70 °C

参考文献：

Method for synthesizing 5-nitro-benzimidazolone via secondary nitration

, China, , ,

合成路线：1 步

95-54-5

_99%

反应条件：

1.1 Solvents: Chlorobenzene ; 5 h, 110 °C; 110 °C → 85 °C
1.2 Solvents: Chlorobenzene ; pH 6
1.3 Reagents: Nitric acid Solvents: Water ; 55 °C; 3 h, 55 °C

参考文献：

Production of 5-nitrobenzimidazolone by one-pot method

, China, , ,

合成路线：1 步

_95%

反应条件：

1.1 Solvents: 1,2-Dichlorobenzene ; 4 h, rt → 160 °C

参考文献：

Process for preparation of pigment intermediate 5-aminobenzimidazolone

, China, , ,

合成路线：1 步

32315-10-9

_95%

反应条件：

1.1 Reagents: Triethylamine Solvents: Tetrahydrofuran

参考文献：

Preparation of 1,3-dihydrobenzimidazol-2-ones

, German Democratic Republic, , ,

合成路线：1 步

75-44-5

_95%

参考文献：

Preparation of benzimidazolones

, Germany, , ,

合成路线：1 步

630-08-0

97-02-9

_92%

反应条件：

1.1 Reagents: Triethylamine Catalysts: Selenium Solvents: Toluene

参考文献：

Selenium-catalyzed carbonylation of o-nitroaniline and its derivatives

Xue, Yan; Lu, Shiwei, Huaxue Tongbao, 2002, 65(3), 187-190

合成路线：1 步

630-08-0

97-02-9

_91%

反应条件：

1.1 Catalysts: Triethylamine , Selenium Solvents: Toluene ; 4 h, 3.0 MPa, 150 °C

参考文献：

Synthesis of benzimidazolones

, China, , ,

合成路线：1 步

_90%

反应条件：

1.1 Catalysts: Chlorosulfonic acid , Boric acid (H3BO3) ; 2 h, 120 °C; 120 °C → rt
1.2 Solvents: Water ; rt

参考文献：

Sulfated polyborate-catalyzed efficient and expeditious synthesis of (un)symmetrical ureas and benzimidazolones

Rekunge, Deelip S.; Khatri, Chetan K.; Chaturbhuj, Ganesh U., Tetrahedron Letters, 2017, 58(45), 4304-4307

合成路线：1 步

124-38-9

_88%

反应条件：

1.1 Reagents: Sodium hydrosulfide Solvents: N-Methyl-2-pyrrolidone ; 24 h, 3 MPa, 90 °C

参考文献：

Method for synthesizing benzothiazolone and 1,3-disubstituted urea derivatives using CO2 activation

, China, , ,

合成路线：1 步

_88%

反应条件：

1.1 Solvents: Dimethylformamide ; 0 °C; 4 h, rt
1.2 Reagents: Water

参考文献：

Bromodomain inhibitors for treating disease

, World Intellectual Property Organization, , ,

合成路线：1 步

_87%

反应条件：

1.1 Catalysts: Acetic acid Solvents: Tetrahydrofuran , Water ; 4.5 h, 100 - 120 °C; 0.5 h, 135 °C

参考文献：

Preparation of 2(3H)-benzimidazolone and its derivative under aqueous condition as a potential agent for antidiabetic compounds

Abbas, Muhammad Azhar; Hameed, Shahid; Kressler, Joerg, Asian Journal of Chemistry, 2013, 25(1), 509-511

合成路线：1 步

1202680-24-7

_86%

反应条件：

1.1 Solvents: Toluene ; 18 h, reflux

参考文献：

Facile Synthesis of Benzo[d]azol-2(3H)-ones Using 2-Phenoxycarbonyl-4,5-dichloropyridazin-3(2H)-one as Green CO Source

Ryu, Ki Eun; Kim, Bo Ram; Sung, Gi Hyeon; Yoon, Hyo Jae; Yoon, Yong-Jin, Synlett, 2015, 26(14), 1985-1990

合成路线：1 步

_85%

反应条件：

1.1 Solvents: Dimethylformamide ; 6 h, rt

参考文献：

Oxidative Cyclization-Induced Activation of a Phosphoinositide 3-Kinase Inhibitor for Enhanced Selectivity of Cancer Chemotherapeutics

Zhu, Haizhou; Mishra, Rosalin; Yuan, Long; Abdul Salam, Safnas F.; Liu, Jing; et al, ChemMedChem, 2019, 14(22), 1933-1939

合成路线：1 步

_82%

反应条件：

1.1 Solvents: Tetrahydrofuran ; cooled; overnight, rt
1.2 Reagents: Hydrochloric acid Solvents: Water

参考文献：

Design and synthesis of novel benzimidazole derivatives as anti-tuberculosis agents

Zhang, Hui-ying; Wang, Bin; Sheng, Li; Li, Dan; Zhang, Dong-feng; et al, Yaoxue Xuebao, 2014, 49(5), 644-651

合成路线：1 步

541-41-3

_78%

反应条件：

1.1 Solvents: Pyridine ; 5 min, 0 °C; 24 h, 70 °C

参考文献：

Synthesis of various benzimidazolone derivatives

Ouzidan, Younes; Rodi, Youssef Kandri; Chakroune, Said; Chahdi, Fouad Ouazzani; Essassi, El Mokhtar, Journal Marocain de Chimie Heterocyclique, 2022, 21(2), 29-35

合成路线：1 步

_78%

反应条件：

1.1 Solvents: Urea, compd. with zinc chloride (ZnCl2) (1:?) ; 4 h, 100 °C

参考文献：

ZnCl2/Urea Eutectic Solvent as Stable Carbonylation Source for Benign Synthesis of 2-Benzimidazolones and 2-Imidazolones: An Effective Strategy for Preventing NH3 Gas Evolution

Aghapoor, Kioumars ; Mohsenzadeh, Farshid; Darabi, Hossein Reza; Sayahi, Hani; Jalali, Mohammad Reza, ChemistrySelect, 2019, 4(37), 11093-11097

合成路线：1 步

1192307-15-5

_78%

反应条件：

1.1 Reagents: Sodium hydroxide , Ammonia Catalysts: L-Proline , Cuprous iodide Solvents: Dimethyl sulfoxide , Water ; rt; 3 - 7 h, rt
1.2 Reagents: Acetic acid ; rt; 3 - 12 h, 130 °C; cooled

参考文献：

Assembly of substituted 1H-benzimidazoles and 1,3-dihydrobenzimidazol-2-ones via CuI/L-proline catalyzed coupling of aqueous ammonia with 2-iodoacetanilides and 2-iodophenylcarbamates

Diao, Xiaoqiong; Wang, Yuji; Jiang, Yongwen; Ma, Dawei, Journal of Organic Chemistry, 2009, 74(20), 7974-7977

合成路线：1 步

616-79-5

_75%

反应条件：

1.1 Reagents: Dimethylformamide , Ammonium chloride , Sodium azide Solvents: Dimethylformamide ; 0 °C
1.2 Reagents: Phosphorus oxychloride ; 0 °C; 0 °C → rt; 8 h, rt
1.3 Reagents: Sodium hydroxide Solvents: Water ; neutralized

参考文献：

A novel method for the synthesis of 2(3H)-benzimidazolones, 2(3H)-benzoxazolone, and 2(3H)-benzothiazolone via in situ generated ortho-substituted benzoic acid azides. Application of ammonium azide and Vilsmeier complex for acid azide generation

Sridhar, Radhakrishnan; Perumal, Paramasivan T., Synthetic Communications, 2004, 34(4), 735-742

合成路线：1 步

_74%