934664-41-2 (1-BOC-3-亚甲基氮杂环丁烷,tert-butyl 3-methylideneazetidine-1-carboxylate)

_100%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether ; 1 h, rt
1.2 Solvents: Diethyl ether ; 2 h, 35 °C

参考文献：

Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

Rice, Kenneth D.; Aay, Naing; Anand, Neel K.; Blazey, Charles M.; Bowles, Owen J.; et al, ACS Medicinal Chemistry Letters, 2012, 3(5), 416-421

合成路线：1 步

_100%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether ; 1 h, rt
1.2 Solvents: Diethyl ether ; 2 h, 35 °C

参考文献：

Preparation of N-acylazetidine MEK inhibitors and 4-aryl-2-aminopyrimidine or 4-aryl-2-aminoalkylpyrimidine JAK-2 inhibitors and their combinations useful for treating neoplasm

, World Intellectual Property Organization, , ,

合成路线：1 步

_100%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether ; 1 h, rt
1.2 Solvents: Diethyl ether ; 2 h, 35 °C; 35 °C → rt

参考文献：

Preparation of azetidines as MEK kinase inhibitors for the treatment of proliferative diseases, especially cancer

, World Intellectual Property Organization, , ,

合成路线：1 步

_99%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether ; 1 h, rt
1.2 2 h, 35 °C; 35 °C → rt

参考文献：

Pleuromutilin derivative and application as antibacterial agents

, China, , ,

合成路线：1 步

2065-66-9

_96%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Tetrahydrofuran ; 30 min, 0 °C
1.2 Solvents: Tetrahydrofuran ; < 10 °C; 2 h, rt

参考文献：

Synthesis of sp3-Enriched β-Fluoro Sulfonyl Chlorides

Gurbanov, Rustam; Sokolov, Andriy; Golovach, Sergey; Melnykov, Kostiantyn; Dobrydnev, Alexey V. ; et al, Synthesis, 2021, 53(10), 1771-1784

合成路线：1 步

_86%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether ; 0.5 h, 0 °C; 0 °C → rt; 1 h, rt
1.2 cooled; heated
1.3 Reagents: Ammonium chloride Solvents: Water

参考文献：

Spiroheterocyclic compounds as mGlu5 antagonists and their preparation and use for the treatment of diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

2065-66-9

_82%

反应条件：

1.1 Reagents: Butyllithium Solvents: Diethyl ether , Tetrahydrofuran ; 0 °C; 1 h, 0 °C
1.2 Solvents: Diethyl ether ; 1 - 6 h, 0 °C
1.3 Reagents: Ammonium chloride Solvents: Water ; 0 °C → rt

参考文献：

Site-Specific Alkene Hydromethylation via Protonolysis of Titanacyclobutanes

Law, James A.; Bartfield, Noah M.; Frederich, James H., Angewandte Chemie, 2021, 60(26), 14360-14364

合成路线：1 步

_81%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Tetrahydrofuran ; 1 h, rt
1.2 Solvents: Tetrahydrofuran ; rt; 2 h, 35 °C

参考文献：

Preparation of azaindazole compounds as inhibitors of T790M containing EGFR mutants

, World Intellectual Property Organization, , ,

合成路线：1 步

_80%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether , Tetrahydrofuran ; rt; 30 min, rt
1.2 Solvents: Diethyl ether ; rt; 16 h, rt
1.3 Reagents: Water ; rt

参考文献：

Branch-Selective Addition of Unactivated Olefins into Imines and Aldehydes

Matos, Jeishla L. M.; Vasquez-Cespedes, Suhelen; Gu, Jieyu; Oguma, Takuya; Shenvi, Ryan A., Journal of the American Chemical Society, 2018, 140(49), 16976-16981

合成路线：1 步

_80%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether , Tetrahydrofuran ; rt; 30 min, rt
1.2 Solvents: Diethyl ether ; rt; 16 h, rt
1.3 Reagents: Water ; rt

参考文献：

Branch-selective addition of unactivated olefins into imines and aldehydes

Matos, Jeishla L. M.; Vasquez-Cespedes, Suhelen; Gu, Jieyu; Oguma, Takuya; Shenvi, Ryan A., ChemRxiv, 2018, 1, 1-7

合成路线：1 步

_80%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Tetrahydrofuran ; 4 h, 70 °C; 70 °C → 50 °C
1.2 Solvents: Tetrahydrofuran ; 15 h, 70 °C

参考文献：

Selective octahydrocyclopenta[c]pyrroles as negative modulators of NR2B and their preparation

, World Intellectual Property Organization, , ,

合成路线：1 步

_79%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether ; 0 °C; 0 °C → rt; 1.5 h, rt
1.2 Solvents: Diethyl ether ; 2 h, rt → reflux; reflux → rt

参考文献：

Preparation of triazolopyridine derivatives for use as PIM kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

1449-46-3

_70%

反应条件：

1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran , Hexane ; 30 min, 0 °C; 18 h, reflux

参考文献：

Oxidative Cascade Reaction of N-Aryl-3-alkylideneazetidines and Carboxylic Acids: Access to Fused Pyridines

Cai, Wangshui; Wang, Shuang; Jalani, Hitesh B. ; Wu, Junxian; Lu, Hongjian ; et al, Organic Letters, 2018, 20(13), 3833-3837

合成路线：1 步

2065-66-9

_69%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether ; 1 h, reflux
1.2 30 min, rt
1.3 Reagents: Water

参考文献：

Preparation of spiroisoxazoline compounds having a potentiating effect on the activity of ethionamide and their use for treating mycobacterial infections such as tuberculosis and leprosy

, France, , ,

合成路线：1 步

_65%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Diethyl ether

参考文献：

Hydrophilic azaspiroalkenes as robust bioorthogonal reporters

An, Peng; Wu, Hsuan-Yi; Lewandowski, Tracey M.; Lin, Qing, Chemical Communications (Cambridge, 2018, 54(99), 14005-14008

合成路线：1 步

_63%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Tetrahydrofuran ; 2 h, rt
1.2 0 °C
1.3 Reagents: Ammonium chloride Solvents: Water

参考文献：

Asymmetric Catalytic Ring-Expansion of 3-Methyleneazetidines with α-Diazo Pyrazoamides towards Proline-Derivatives

Wang, Kaixuan ; Yang, Longqing; Li, Yi; Li, Hongye; Liu, Zhili; et al, Angewandte Chemie, 2023, 62(32),

合成路线：1 步

_61%