76-05-1 (三氟乙酸,Trifluoroacetic acid)

78123-71-4

参考文献：

Improved procedure for the synthesis of DAMGO

Reddy, P. Anantha; Lewin, Anita H.; Carroll, F. Ivy, Synthetic Communications, 2007, 37(14), 2345-2348

合成路线：1 步

1057333-03-5

63386-61-8

反应条件：

1.1 Solvents: Dichloromethane ; 1 h, rt

参考文献：

Sulfonylated piperidine and piperazine derivatives as 11-βHSD1 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Catalysts: Trifluoroacetic acid

参考文献：

Enzyme substrates. VII. Synthesis of 4-methyl-7-coumarylamides of amino acids

Tetere, Z.; Strakova, I.; Zicane, D.; Ravina, I.; Rijkure, I.; et al, Latvijas PSR Zinatnu Akademijas Vestis, 1987, (6), 728-30

合成路线：1 步

77471-41-1

参考文献：

(Peptidylamino)coremarins

, Japan, , ,

合成路线：1 步

53109-32-3

参考文献：

Method for the preparation of all stereoisomers of cyclo(histidylproline)

, China, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Sodium bicarbonate , Sodium carbonate , Sodium chloride Catalysts: Papain Solvents: Water

参考文献：

A new simple route to the synthesis of protease substrates in ice

Ulmann, Dirk; Bordusa, Frank; Salchert, Katrin; Jakubke, Hans-Dieter, Tetrahedron: Asymmetry, 1996, 7(7), 2047-2054

合成路线：1 步

866547-56-0

206350-77-8

反应条件：

1.1 Reagents: Triisopropylsilane Solvents: Ethanol ; 5 h, rt

参考文献：

Soluble, stable insulin-containing formulations

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Dichloromethane ; 1 h, rt

参考文献：

Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility

Jia, Lanqi; Simpson, Robert D.; Yuan, Jing; Xu, Zhenrong; Zhao, Wei; et al, ACS Medicinal Chemistry Letters, 2011, 2(10), 747-751

合成路线：1 步

反应条件：

1.1 Solvents: Dichloromethane ; 30 min, rt

参考文献：

Preparation of piperidine derivatives as renin inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Dichloromethane ; 30 min, rt

参考文献：

Piperidine derivatives as aspartic protease inhibitors and their preparation, pharmaceutical compositions and use in the treatment of aspartic protease mediated diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Dichloromethane ; rt

参考文献：

Preparation of aminophenylpiperidinecarboxylate derivatives and analogs as renin inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Trifluoroacetic acid Solvents: Dichloromethane ; rt
1.2 -

参考文献：

Piperidines and morpholines as renin inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases associated with renin activity

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Dichloromethane ; rt

参考文献：

Diaminopropanol derivatives as renin inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

_64%

反应条件：

1.1 Catalysts: Zinc triflate Solvents: Acetonitrile ; 24 h, reflux
1.2 Reagents: Sodium carbonate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,2-Dimethoxyethane , Water ; 24 h, reflux
1.3 Reagents: Dibromotriphenylphosphorane , Diisopropylethylamine Solvents: Dichloromethane ; 18 h, rt
1.4 Reagents: Sodium hydride Solvents: Dimethylformamide ; 1 h, 40 °C
1.5 Catalysts: Tetrabutylammonium iodide ; 20 h, 45 °C
1.6 Solvents: Dichloromethane ; rt

参考文献：

Original loading and Suzuki conditions for the solid-phase synthesis of biphenyltetrazoles. Application to the first solid-phase synthesis of irbesartan

Cousaert, Nicolas; Willand, Nicolas; Gesquiere, Jean-Claude; Tartar, Andre; Deprez, Benoit; et al, Tetrahedron Letters, 2008, 49(17), 2743-2747

合成路线：1 步

1957235-57-2

1957235-66-3

反应条件：

1.1 Solvents: Dichloromethane ; 2 h, rt

参考文献：

Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91

Hanafi, Maha ; Chen, Xinde; Neamati, Nouri, Journal of Medicinal Chemistry, 2021, 64(3), 1626-1648

合成路线：1 步

1957235-57-2

1957235-66-3

反应条件：

1.1 Solvents: Dichloromethane ; 1 h, rt

参考文献：

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Zhou, Bing ; Hu, Jiantao; Xu, Fuming; Chen, Zhuo; Bai, Longchuan; et al, Journal of Medicinal Chemistry, 2018, 61(2), 462-481

合成路线：1 步

_91%

反应条件：

1.1 Solvents: Dichloromethane ; 3 h, 0 °C → rt

参考文献：

Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors

Lei, Meng; et al, Bioorganic & Medicinal Chemistry, 2019, 27(18), 4151-4162

合成路线：2 步

反应条件：

参考文献：

Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors

Lei, Meng; et al, Bioorganic & Medicinal Chemistry, 2019, 27(18), 4151-4162

合成路线：3 步

5874-73-7