87694-53-9 (（S）-2,2' - 双[双（3,5 - 三氟甲基苯基）膦基] -4,4',6,6' - 四甲氧基联苯,N-Boc-N-methoxy-N-methyl-L-phenylalaninamide)

1117-97-1

_100%

反应条件：

1.1 Reagents: Diisopropylethylamine , 1-[Bis(dimethylamino)methylene]-1H-benzotriazolium hexafluorophosphate(1-) 3-oxi… Solvents: Dichloromethane ; 2 h, rt

参考文献：

Exploration of the carmaphycins as payloads in antibody drug conjugate anticancer agents

Almaliti, Jehad; et al, European Journal of Medicinal Chemistry, 2019, 161, 416-432

合成路线：1 步

1117-97-1

_100%

反应条件：

1.1 Reagents: Diisopropylethylamine , O-(Benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate Solvents: Dichloromethane ; rt

参考文献：

Assessment of the in vitro effect of antibodies induced by peptido-mimetics derived from the Plasmodium merozoite surface protein-2 in malaria caused by P. berghei and P. yoelii in BALB/c mice

Lesmes, Liliana Patricia; et al, Revista Colombiana de Ciencias Quimico-Farmaceuticas, 2010, 39(2), 188-210

合成路线：1 步

_100%

反应条件：

1.1 Reagents: 1-Hydroxybenzotriazole , 1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Dichloromethane ; 10 min, rt
1.2 Reagents: Triethylamine ; overnight, rt

参考文献：

Probing α-Amino Aldehydes as Weakly Acidic Pronucleophiles: Direct Access to Quaternary α-Amino Aldehydes by an Enantioselective Michael Addition Catalyzed by Bronsted Bases

Garcia-Urricelqui, Ane; et al, Chemistry - A European Journal, 2021, 27(7), 2483-2492

合成路线：1 步

_100%

反应条件：

1.1 Reagents: 1,1′-Carbonyldiimidazole Solvents: Dichloromethane ; rt; 1.25 h, rt
1.2 Solvents: Dichloromethane ; overnight, rt

参考文献：

Heterocyclic Cathinones as Inhibitors of Kynurenine Aminotransferase II-Design, Synthesis, and Evaluation

Maryska, Michal; et al, Pharmaceuticals, 2021, 14(12),

合成路线：1 步

35150-06-2

1117-97-1

_87%

反应条件：

1.1 Solvents: Dichloromethane ; 5 min, 23 °C
1.2 Reagents: N-(Dimethoxymethyl)-N-(1-methylethyl)-2-propanamine ; 23 °C → reflux; 4 h, reflux; reflux → 23 °C
1.3 3 min, 23 °C
1.4 Catalysts: Zirconium chloride (ZrCl4) Solvents: Acetonitrile ; 1 h, 23 °C

参考文献：

Efficient Transamidation of Primary Carboxamides by in Situ Activation with N,N-Dialkylformamide Dimethyl Acetals

Dineen, Thomas A.; et al, Journal of the American Chemical Society, 2006, 128(50), 16406-16409

合成路线：1 步

_86%

反应条件：

1.1 Reagents: Triethylamine Solvents: Methanol ; 16 h, rt
1.2 Reagents: Triethylamine , 1-Hydroxybenzotriazole , 1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Dichloromethane ; 10 min, rt
1.3 16 h, rt

参考文献：

Convenient Synthesis of Alternatively Bridged Tryptophan Ketopiperazines and Their Activities against Trypanosomatid Parasites

Cockram, Peter E.; et al, ChemMedChem, 2022, 17(4),

合成路线：1 步

51987-73-6

_85%

反应条件：

1.1 Reagents: Chloro(1-methylethyl)magnesium Solvents: Tetrahydrofuran ; 15 min, -40 °C; 3 h, -30 °C → 0 °C
1.2 Reagents: Ammonium chloride Solvents: Water

参考文献：

Synthesis and antiproteasomal activity of novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine

Jorda, Radek; et al, European Journal of Medicinal Chemistry, 2017, 135, 142-158

合成路线：1 步

163625-29-4

_77%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: Methanol , Water
1.2 Reagents: Ammonium hydroxide Solvents: Water
1.3 -
1.4 Reagents: Triethylamine

参考文献：

Gold(I)-Catalyzed Asymmetric Aldol Reaction of N-Methoxy-N-methyl-α-isocyanoacetamide (α-Isocyano Weinreb Amide). An Efficient Synthesis of Optically Active β-Hydroxy α-Amino Aldehydes and Ketones

Sawamura, Masaya; et al, Journal of Organic Chemistry, 1995, 60(6), 1727-32

合成路线：1 步

474890-08-9

_75%

反应条件：

1.1 Reagents: Triethylamine Catalysts: Methanesulfonic acid, 1,1,1-trifluoro-, samarium(3+) salt (3:1) Solvents: Tetrahydrofuran
1.2 Reagents: Hydrochloric acid Solvents: Water

参考文献：

A Convenient Method for the Conversion of N-Acyloxazolidinones to Hydroxamic Acids

Sibi, Mukund P.; et al, Organic Letters, 2002, 4(20), 3343-3346

合成路线：1 步

514214-66-5

_75%

反应条件：

1.1 Solvents: Tetrahydrofuran ; 5 min; 24 h, rt

参考文献：

An efficient conversion of carboxylic acids into Weinreb amides

Katritzky, Alan R.; et al, ARKIVOC (Gainesville, 2002, (11), 39-44

合成路线：1 步

133489-47-1

参考文献：

Novel bis-cyclic guanidines as potent membrane-active antibacterial agents with therapeutic potential

Teng, Peng; et al, Chemical Communications (Cambridge, 2017, 53(87), 11948-11951

合成路线：1 步

反应条件：

1.1 Solvents: Dichloromethane

参考文献：

Preparation of heterocyclic conformationally restricted HIV-1 protease inhibitors

, United Kingdom, , ,

合成路线：1 步

参考文献：

A facile approach to trans-4,5-pyrrolidine lactam and application in the synthesis of nemonapride and streptopyrrolidine

Huang, Wei; et al, Tetrahedron, 2011, 67(40), 7829-7837

合成路线：2 步

37073-15-7

反应条件：

1.1 Reagents: Triethylamine Solvents: Tetrahydrofuran ; rt; 6 - 12 h, reflux
2.1 Solvents: Tetrahydrofuran ; 5 min; 24 h, rt

参考文献：

An efficient conversion of carboxylic acids into Weinreb amides

Katritzky, Alan R.; et al, ARKIVOC (Gainesville, 2002, (11), 39-44

合成路线：2 步

163625-30-7

反应条件：

1.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethanol
2.1 Reagents: Hydrochloric acid Solvents: Methanol , Water
2.2 Reagents: Ammonium hydroxide Solvents: Water
2.3 -
2.4 Reagents: Triethylamine

参考文献：

Sawamura, Masaya; et al, Journal of Organic Chemistry, 1995, 60(6), 1727-32

合成路线：2 步

63-91-2

反应条件：

1.1 Reagents: Triethylamine Solvents: Methanol ; 16 h, rt
2.1 Reagents: Triethylamine , 1-Hydroxybenzotriazole , 1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Dichloromethane ; 10 min, rt
2.2 16 h, rt

参考文献：

Convenient Synthesis of Alternatively Bridged Tryptophan Ketopiperazines and Their Activities against Trypanosomatid Parasites

Cockram, Peter E.; et al, ChemMedChem, 2022, 17(4),

合成路线：2 步

7524-50-7

反应条件：

1.1 Reagents: Triethylamine Solvents: Tetrahydrofuran ; 0 °C; 20 h, 0 °C → rt
2.1 Reagents: Chloro(1-methylethyl)magnesium Solvents: Tetrahydrofuran ; 15 min, -40 °C; 3 h, -30 °C → 0 °C
2.2 Reagents: Ammonium chloride Solvents: Water

参考文献：

Synthesis and antiproteasomal activity of novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine

Jorda, Radek; et al, European Journal of Medicinal Chemistry, 2017, 135, 142-158

合成路线：3 步

163625-26-1

100-52-7

反应条件：

1.1 Catalysts: Gold(1+), bis[(isocyano-κC)cyclohexane]-, tetrafluoroborate(1-) (1:1) , (1R)-1,1′-Bis(diphenylphosphino)-2-[(1R)-1-[methyl[2-(4-morpholinyl)ethyl]amino]… Solvents: Dichloromethane
2.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethanol
3.1 Reagents: Hydrochloric acid Solvents: Methanol , Water
3.2 Reagents: Ammonium hydroxide Solvents: Water
3.3 -
3.4 Reagents: Triethylamine

参考文献：

Sawamura, Masaya; et al, Journal of Organic Chemistry, 1995, 60(6), 1727-32

合成路线：4 步

163625-27-2

反应条件：

1.1 Reagents: Triethylamine , Phosphorus oxychloride Solvents: Tetrahydrofuran
1.2 Reagents: Sodium bicarbonate Solvents: Dichloromethane , Water
2.1 Catalysts: Gold(1+), bis[(isocyano-κC)cyclohexane]-, tetrafluoroborate(1-) (1:1) , (1R)-1,1′-Bis(diphenylphosphino)-2-[(1R)-1-[methyl[2-(4-morpholinyl)ethyl]amino]… Solvents: Dichloromethane
3.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethanol
4.1 Reagents: Hydrochloric acid Solvents: Methanol , Water
4.2 Reagents: Ammonium hydroxide Solvents: Water
4.3 -
4.4 Reagents: Triethylamine

参考文献：

Sawamura, Masaya; et al, Journal of Organic Chemistry, 1995, 60(6), 1727-32

合成路线：5 步

120939-75-5

109-94-4