92855-65-7 (7-苄氧吲哚-3-甲醛,7-(benzyloxy)-1H-indole-3-carbaldehyde)

_100%

反应条件：

1.1 Reagents: Phosphorus oxychloride ; 15 min, < -5 °C; 1 h, -10 - 0 °C
1.2 Solvents: Dimethylformamide ; < 0 °C; 0 °C → rt; 1 h, rt; rt → 0 °C
1.3 Reagents: Sodium hydroxide Solvents: Water ; 20 min, 0 - 5 °C; 30 min, reflux; reflux → 10 °C; 20 min, 10 °C

参考文献：

Preparation of indolylethylaminopropanediol aryl ethers as β3 adrenergic agonists

, World Intellectual Property Organization, , ,

合成路线：1 步

_100%

反应条件：

参考文献：

Preparation and use of 3-substituted oxoindole as β3 agonists

, World Intellectual Property Organization, , ,

合成路线：1 步

_99%

反应条件：

1.1 Reagents: Phosphorus oxychloride Solvents: Dimethylformamide
1.2 Solvents: Water

参考文献：

A scalable synthesis of (R)-3-(2-aminopropyl)-7-benzyloxyindole via resolution

Fujii, Akihito; Fujima, Yoshito; Harada, Hiroshi; Ikunaka, Masaya; Inoue, Toru; et al, Tetrahedron: Asymmetry, 2001, 12(23), 3235-3240

合成路线：1 步

_98%

反应条件：

1.1 Reagents: Phosphorus oxychloride Solvents: Dimethylformamide ; 2 h, 0 °C → rt

参考文献：

Structure-activity relationship study of novel necroptosis inhibitors

Teng, Xin; Degterev, Alexei; Jagtap, Prakash; Xing, Xuechao; Choi, Sungwoon; et al, Bioorganic & Medicinal Chemistry Letters, 2005, 15(22), 5039-5044

合成路线：1 步

_96%

反应条件：

1.1 Reagents: Phosphorus oxychloride ; 10 - 20 °C; 45 min, 35 °C; 35 °C → rt
1.2 Reagents: Sodium hydroxide Solvents: Water ; 1 min, pH 13, reflux

参考文献：

Indole derivatives as cholinesterase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

_96%

反应条件：

1.1 Reagents: Phosphorus oxychloride ; 10 - 20 °C
1.2 Solvents: Dimethylformamide ; 20 - 30 °C; 45 min, 35 °C; 35 °C → rt
1.3 Reagents: Sodium hydroxide Solvents: Water ; pH 13, cooled; 1 min, heated

参考文献：

Carbamate Derivatives of Indolines as Cholinesterase Inhibitors and Antioxidants for the Treatment of Alzheimer's Disease

Yanovsky, Inessa; Finkin-Groner, Efrat; Zaikin, Andrey; Lerman, Lena; Shalom, Hila; et al, Journal of Medicinal Chemistry, 2012, 55(23), 10700-10715

合成路线：1 步

_86%

反应条件：

1.1 Reagents: Phosphorus oxychloride Solvents: 1,2-Dichloroethane ; 25 - 30 °C; 22 h, 30 °C → 88 °C; 88 °C → rt

参考文献：

Process for preparation of 3-cyanoindole derivatives

, China, , ,

合成路线：1 步

100-61-8

_65%

反应条件：

1.1 Reagents: Pivalic acid , tert-Butyl peroxybenzoate Catalysts: Tetrabutylammonium iodide Solvents: Dimethyl sulfoxide ; 8 h, 80 °C
1.2 Reagents: Sodium bicarbonate Solvents: Water

参考文献：

nBu4NI-catalyzed C3-formylation of indoles with N-methylaniline

Li, Lan-Tao; Huang, Juan; Li, Hong-Ying; Wen, Li-Juan; Wang, Peng; et al, Chemical Communications (Cambridge, 2012, 48(42), 5187-5189

合成路线：1 步

反应条件：

1.1 Reagents: Sodium hydroxide , Phosphorus oxychloride Solvents: Dimethylformamide

参考文献：

Synthesis of indolyl-3-acetonitrile derivatives and their inhibitory effects on nitric oxide and PGE2 productions in LPS-induced RAW 264.7 cells

Kwon, Tae Hoon; Yoon, Ik Hwan; Shin, Ji-Sun; Lee, Young Hun; Kwon, Bong Jin; et al, Bioorganic & Medicinal Chemistry Letters, 2013, 23(9), 2571-2574

合成路线：1 步

反应条件：

1.1 Reagents: Phosphorus oxychloride Solvents: Dimethylformamide ; 3 min, 0 °C
1.2 Solvents: Dimethylformamide ; 0 °C; 0 °C → rt; 4.5 h, rt; rt → 0 °C
1.3 Reagents: Potassium hydroxide Solvents: Water ; 0 °C; 0 °C → reflux; 5 min, reflux

参考文献：

Total Synthesis of (+)-Haplophytine

Ueda, Hirofumi; Satoh, Hitoshi; Matsumoto, Koji; Sugimoto, Kenji; Fukuyama, Tohru; et al, Angewandte Chemie, 2009, 48(41), 7600-7603

合成路线：1 步

参考文献：

Preparation of 3,7-disubstituted indoles and their optically active compounds as intermediates for β3 adrenergic agonists

, Japan, , ,

合成路线：1 步