922500-95-6 (3-硝基亚甲基-氧杂环丁烷,3-(Nitromethylene)oxetane)

_85%

反应条件：

1.1 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; 4 h, 60 °C
1.2 Reagents: Ammonium chloride Solvents: Water

参考文献：

Preparation of indolin-1-one derivatives as Cbl-b inhibitors for treatment of cancer

, World Intellectual Property Organization, , ,

合成路线：1 步

_83%

反应条件：

1.1 Reagents: Triethylamine Solvents: Dichloromethane
1.2 Reagents: Triethylamine , Methanesulfonyl chloride

参考文献：

3-Oxetanone

Banerjee, Abhisek, e-EROS Encyclopedia of Reagents for Organic Synthesis, 2014, 1, 1-6

合成路线：1 步

_83%

反应条件：

1.1 Catalysts: Triethylamine
1.2 Reagents: Triethylamine , Methanesulfonyl chloride

参考文献：

Oxetanes in Drug Discovery: Structural and Synthetic Insights

Wuitschik, Georg; Carreira, Erick M.; Wagner, Bjorn; Fischer, Holger; Parrilla, Isabelle; et al, Journal of Medicinal Chemistry, 2010, 53(8), 3227-3246

合成路线：1 步

_81%

反应条件：

1.1 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane

参考文献：

Oxetanes in Drug Discovery

Wuitschik, Georg, 2008, , ,

合成路线：1 步

_81%

反应条件：

1.1 Catalysts: Triethylamine Solvents: Nitromethane ; 20 min, rt
1.2 Reagents: Triethylamine Solvents: Dichloromethane ; -78 °C
1.3 Reagents: Methanesulfonyl chloride ; 10 min, -78 °C; 20 min, -78 °C

参考文献：

Oxetanes as promising modules in drug discovery

Wuitschik, Georg; Rogers-Evans, Mark; Mueller, Klaus; Fischer, Holger; Wagner, Bjoern; et al, Angewandte Chemie, 2006, 45(46), 7736-7739

合成路线：1 步

_78%

反应条件：

1.1 Reagents: (Diethylamino)sulfur trifluoride Solvents: Dichloromethane ; 0 °C; 1 h, 0 °C
1.2 Reagents: Potassium bicarbonate Solvents: Water

参考文献：

Method for synthesis of conjugated nitrovinyl-substituted derivatives adopting diethylaminosulfur trifluoride (DAST) reagent as elimination agent

, China, , ,

合成路线：1 步

_77%

反应条件：

1.1 Reagents: (Diethylamino)sulfur trifluoride Solvents: Dichloromethane ; 1 h, 0 °C
1.2 Reagents: Potassium bicarbonate Solvents: Water

参考文献：

(Hetero)arylamino-cyclohexyl-sulfonyl derivatives as CCR6 inhibitors and their preparation

, World Intellectual Property Organization, , ,

合成路线：1 步

_70%

反应条件：

1.1 Reagents: Triethylamine ; 30 min, rt
1.2 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane

参考文献：

Process Development of the BACE Inhibitors BI 1147560 BS and BI 1181181 MZ

Li, Guisheng; Tan, Zhulin; Xu, Yibo; Sidhu, Kanwar P. S.; Qu, Bo ; et al, Organic Process Research & Development, 2022, 26(12), 3345-3372

合成路线：1 步

_64%

反应条件：

1.1 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; 3 h, -78 °C; 2 h, -78 °C; -78 °C → rt; 12 h, rt
1.2 Reagents: Water ; cooled

参考文献：

Preparation of 3-(aminomethyl)oxetane and its organic acid salts

, China, , ,

合成路线：1 步

_58%

反应条件：

1.1 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; 0 °C → -78 °C; 1 h, -78 °C

参考文献：

Dibenzothiazepinone derivatives as hepatitis B core protein allosteric modulators and their preparation

, World Intellectual Property Organization, , ,

合成路线：1 步

_50%

反应条件：

1.1 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; 30 min, -78 °C; 1 h, -78 °C

参考文献：

Preparation of indolylalkylamide derivatives for use as positive allosteric modulators of nicotinic acetylcholine receptor

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Triethylamine ; 30 min, rt
1.2 Solvents: Dichloromethane ; rt → -78 °C
1.3 Reagents: Triethylamine , Methanesulfonyl chloride ; 10 min, -78 °C; 40 min, -78 °C; -78 °C → rt

参考文献：

Broad spectrum anti-cancer compounds for treatment of cancer

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Triethylamine ; 0 °C; 1 h, rt
1.2 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; -78 °C; 1.5 h, -78 °C

参考文献：

Development of oxetane modified building blocks for peptide synthesis

Roesner, Stefan; Beadle, Jonathan D.; Tam, Leo K. B.; Wilkening, Ina; Clarkson, Guy J.; et al, Organic & Biomolecular Chemistry, 2020, 18(28), 5400-5405

合成路线：1 步

反应条件：

1.1 Reagents: Triethylamine ; 1 h, rt
1.2 Solvents: Dichloromethane ; rt → -78 °C
1.3 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; -78 °C; 1.5 h, -78 °C

参考文献：

Enzymatically-stable oxetane-based dipeptide hydrogels

McDougall, Laura; Draper, Emily R.; Beadle, Jonathan D.; Shipman, Michael; Raubo, Piotr; et al, Chemical Communications (Cambridge, 2018, 54(14), 1793-1796

合成路线：1 步

53753-37-0

反应条件：

1.1 Reagents: Sodium hydride Solvents: Tetrahydrofuran ; rt

参考文献：

Synthesis of 6-Azaspiro[4.3]alkanes: Innovative Scaffolds for Drug Discovery

Chalyk, Bohdan A.; Isakov, Andrei A.; Butko, Maryna V.; Hrebeniuk, Kateryna V.; Savych, Olena V.; et al, European Journal of Organic Chemistry, 2017, 2017(31), 4530-4542

合成路线：1 步

反应条件：

1.1 Reagents: Triethylamine ; 1 h, rt
1.2 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; -78 °C; 1.5 h, -78 °C

参考文献：

Solid-phase synthesis of oxetane modified peptides

Beadle, Jonathan D.; Knuhtsen, Astrid; Hoose, Alex; Raubo, Piotr; Jamieson, Andrew G. ; et al, Organic Letters, 2017, 19(12), 3303-3306

合成路线：1 步

反应条件：

1.1 Reagents: Triethylamine ; 60 min, rt
1.2 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; -78 °C; 90 min, -78 °C

参考文献：

Synthesis of Oxetane- and Azetidine-Containing Spirocycles Related to the 2,5-Diketopiperazine Framework

Beadle, Jonathan D.; Powell, Nicola H.; Raubo, Piotr; Clarkson, Guy J.; Shipman, Michael, Synlett, 2016, 27(1), 169-172

合成路线：1 步

反应条件：

1.1 Reagents: Triethylamine ; 30 min, rt
1.2 Reagents: Triethylamine , Methanesulfonyl chloride Solvents: Dichloromethane ; 10 min, -78 °C; 40 min, -78 °C

参考文献：

Synthesis and structure of oxetane containing tripeptide motifs

Powell, Nicola H.; Clarkson, Guy J.; Notman, Rebecca; Raubo, Piotr; Martin, Nathaniel G.; et al, Chemical Communications (Cambridge, 2014, 50(63), 8797-8800

合成路线：1 步