88495-63-0 (青蒿琥酯,Artesunate)

_89%

反应条件：

1.1 Reagents: Sodium bicarbonate Solvents: Acetone ; 24 h, rt
1.2 Reagents: Acetic acid Solvents: Water ; pH 3, rt
1.3 Solvents: Water ; 30 min, rt

参考文献：

Synthesis of artesunate from dihydroartemisinin with sodium bicarbonate as catalyst

Do, Huu Nghi; et al, Tap Chi Duoc Hoc, 2008, 48(4), 29-31

合成路线：1 步

_94%

反应条件：

1.1 Reagents: Triethylamine Solvents: Isopropyl acetate ; 30 min, 25 °C; 4 h, 25 °C
1.2 Reagents: Sulfuric acid Solvents: Water ; > 1 min, pH 5, 25 °C

参考文献：

A simplified and scalable synthesis of artesunate

Presser, Armin ; et al, Monatshefte fuer Chemie, 2017, 148(1), 63-68

合成路线：1 步

_92%

反应条件：

1.1 Solvents: Dichloromethane ; rt
1.2 Catalysts: 4-(Dimethylamino)pyridine ; 30 min, 0 - 5 °C; 5 °C → rt; 1 h, rt
1.3 Reagents: Hydrochloric acid Solvents: Water ; pH 3

参考文献：

Synthesis of dihydroartemisinin-isosorbitan mononitrate hybrid and its antitumor activities in vitro

Xie, Bin; et al, Hecheng Huaxue, 2011, 19(1), 62-65

合成路线：1 步

_28%

反应条件：

1.1 Reagents: Triethylamine Solvents: Dichloromethane ; rt
1.2 Reagents: Hydrochloric acid Solvents: Water

参考文献：

Continuous synthesis of artemisinin-derived medicines

Gilmore, Kerry; et al, Chemical Communications (Cambridge, 2014, 50(84), 12652-12655

合成路线：1 步

反应条件：

1.1 Reagents: Imidazole Solvents: Dichloromethane ; 2 h, rt
1.2 Reagents: Hydrochloric acid Solvents: Water ; pH 3, rt

参考文献：

Structural optimization and biological evaluation for novel artemisinin derivatives against liver and ovarian cancers

Zhou, Yu; et al, European Journal of Medicinal Chemistry, 2021, 211,

合成路线：1 步

_91%

反应条件：

1.1 Reagents: Sodium borohydride Solvents: Methanol ; 2 h, 0 - 5 °C
1.2 Reagents: Imidazole Solvents: Dichloromethane ; 2 h, rt

参考文献：

Reverse Chemical Proteomics Identifies an Unanticipated Human Target of the Antimalarial Artesunate

Gotsbacher, Michael P. ; et al, ACS Chemical Biology, 2019, 14(4), 636-643

合成路线：1 步

81496-81-3

110-15-6

_84%

反应条件：

1.1 Reagents: 1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Catalysts: 4-(Dimethylamino)pyridine Solvents: Dichloromethane ; 4 h, 0 °C

参考文献：

Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo

Wang, Liang-Liang; et al, European Journal of Medicinal Chemistry, 2019, 182,

合成路线：1 步

_73%

反应条件：

1.1 Reagents: Iron chloride (FeCl3) Solvents: Methanol ; 12 h, reflux; 24 h; overnight, cooled

参考文献：

Some transition metal complexes bearing artemisinin derivatives and (N-N-O) tridentate chromium (III) complexes ligated by 2-benzolmidazo-yl-6-acetyl-pyridines for catalytic behaviour towards ethylene

Obaleye, Joshua Ayoola; et al, Journal of Chemistry and Chemical Engineering, 2010, 4(12), 23-32

合成路线：1 步

98672-75-4

_60%

参考文献：

Studies on analogs of arteannuin. II. Synthesis of some carboxylic esters and carbonates of dihydroarteannuin by using 4-(N,N-dimethylamino)pyridine as an active acylation catalyst

Li, Ying; et al, Huaxue Xuebao, 1982, 40(6), 557-61

合成路线：1 步

110-15-6

_45%

反应条件：

1.1 Reagents: Trichloroacetonitrile , 1,8-Diazabicyclo[5.4.0]undec-7-ene Solvents: Dichloromethane
1.2 Solvents: Dichloromethane

参考文献：

C-10 ester and ether derivatives of dihydroartemisinin - 10-α artesunate, preparation of authentic 10-β artesunate, and of other ester and ether derivatives bearing potential aromatic intercalating groups at C-10

Haynes, Richard K.; et al, European Journal of Organic Chemistry, 2002, (1), 113-132

合成路线：2 步

反应条件：

1.1 Reagents: Sodium borohydride Solvents: Methanol ; 2 h, 0 °C
2.1 Reagents: Triethylamine Solvents: Dichloromethane ; 2 h, rt

参考文献：

Artemisinin-derived artemisitene blocks ROS-mediated NLRP3 inflammasome and alleviates ulcerative colitis

Hua, Lei; et al, International Immunopharmacology, 2022, 113,

合成路线：2 步

反应条件：

1.1 Reagents: Sodium borohydride Solvents: Methanol ; 30 min, 0 - 5 °C; 5 °C → rt; 30 min, rt
1.2 Reagents: Acetic acid Solvents: Methanol ; pH 5 - 6, rt
2.1 Reagents: Triethylamine Solvents: Isopropyl acetate ; 30 min, 25 °C; 4 h, 25 °C
2.2 Reagents: Sulfuric acid Solvents: Water ; > 1 min, pH 5, 25 °C

参考文献：

A simplified and scalable synthesis of artesunate

Presser, Armin ; et al, Monatshefte fuer Chemie, 2017, 148(1), 63-68

合成路线：2 步

反应条件：

1.1 Reagents: Sodium borohydride Solvents: Methanol ; 1 h, 0 - 5 °C
1.2 Reagents: Acetic acid ; pH 7
1.3 Solvents: Water ; cooled; 15 min, rt
2.1 Reagents: Triethylamine Solvents: Acetone ; 9 h, rt
2.2 Reagents: Hydrochloric acid Solvents: Water ; pH 3 - 4

参考文献：

Synthesis of water soluble chitosan-artemisinin conjugate

Xiao, Dan; et al, Asian Journal of Chemistry, 2013, 25(8), 4637-4639

合成路线：3 步

85031-59-0