79821-73-1 ((1-甲基-2-氧代-2-苯基-乙基)-氨基甲酸叔丁酯,(1-METHYL-2-OXO-2-PHENYL-ETHYL)-CARBAMIC ACID TERT-BUTYL ESTER)

_99%

反应条件：

1.1 Reagents: Oxygen Catalysts: 1-Methylimidazole , 4,4′-Dimethoxy-2,2′-bipyridine , 9-Azabicyclo[3.3.1]non-9-yloxy , Copper(I) triflate Solvents: Acetonitrile ; 1 min, 24 atm, 100 °C
1.2 Reagents: Ethyl acetate

参考文献：

PTFE-Membrane Flow Reactor for Aerobic Oxidation Reactions and Its Application to Alcohol Oxidation

Greene, Jodie F.; et al, Organic Process Research & Development, 2015, 19(7), 858-864

合成路线：1 步

_97%

反应条件：

1.1 Reagents: 1-Methylimidazole , Oxygen Catalysts: Cuprous iodide , 9-Azabicyclo[3.3.1]non-9-yloxy Solvents: N-Methyl-2-pyrrolidone ; 1 h, 60 °C

参考文献：

Process Development of CuI/ABNO/NMI-Catalyzed Aerobic Alcohol Oxidation

Steves, Janelle E.; et al, Organic Process Research & Development, 2015, 19(11), 1548-1553

合成路线：1 步

_95%

反应条件：

1.1 Reagents: Oxygen Catalysts: 1-Methylimidazole , 4,4′-Dimethoxy-2,2′-bipyridine , 9-Azabicyclo[3.3.1]non-9-yloxy , Copper(1+), tetrakis(acetonitrile)-, (T-4)-, 1,1,1-trifluoromethanesulfonate (1:… Solvents: Acetonitrile ; 0.75 h, rt
1.2 Reagents: Water

参考文献：

Copper(I)/ABNO-Catalyzed Aerobic Alcohol Oxidation: Alleviating Steric and Electronic Constraints of Cu/TEMPO Catalyst Systems

Steves, Janelle E.; et al, Journal of the American Chemical Society, 2013, 135(42), 15742-15745

合成路线：1 步

100-59-4

_97%

反应条件：

1.1 Reagents: Chloro(1-methylethyl)magnesium Solvents: Tetrahydrofuran ; rt → -15 °C
1.2 Solvents: Tetrahydrofuran ; -5 °C; 330 min, -5 °C → rt; 4 h, rt; rt → 0 °C
1.3 Reagents: Hydrochloric acid Solvents: Ethyl acetate , Water

参考文献：

Improved syntheses of α-BOC-aminoketones from α-BOC-amino-Weinreb amides using a pre-deprotonation protocol

Liu, Jinchu; et al, Tetrahedron Letters, 2002, 43(46), 8223-8226

合成路线：1 步

390747-62-3

_97%

反应条件：

1.1 Reagents: Dess-Martin periodinane Solvents: Dichloromethane , Water ; 20 min, rt

参考文献：

Copper(I)/ABNO-Catalyzed Aerobic Alcohol Oxidation: Alleviating Steric and Electronic Constraints of Cu/TEMPO Catalyst Systems

Steves, Janelle E.; et al, Journal of the American Chemical Society, 2013, 135(42), 15742-15745

合成路线：1 步

186431-89-0

_95%

反应条件：

1.1 Solvents: Tetrahydrofuran ; 0 °C; 2 h, 0 °C
1.2 Reagents: Ammonium chloride Solvents: Water

参考文献：

Enantioconvergent Cu-Catalyzed Radical C-N Coupling of Racemic Secondary Alkyl Halides to Access α-Chiral Primary Amines

Zhang, Yu-Feng; et al, Journal of the American Chemical Society, 2021, 143(37), 15413-15419

合成路线：1 步

_90%

反应条件：

1.1 Solvents: Tetrahydrofuran ; 0 °C; overnight, 0 °C
1.2 Reagents: Ammonium chloride Solvents: Water ; 0 °C; 10 min, 0 °C

参考文献：

Diastereoselective Synthesis of Nonplanar 3-Amino-1,2,4-oxadiazine Scaffold: Structure Revision of Alchornedine

Tang, Shuang-Qi; et al, Journal of Organic Chemistry, 2020, 85(23), 15347-15359

合成路线：1 步

_48%

反应条件：

1.1 rt

参考文献：

A convenient method for the synthesis of chiral N-protected 1,2-amino alcohols via the reduction of the aminoketones

Zhou, Zheng Hong; et al, Chinese Chemical Letters, 2003, 14(12), 1227-1229

合成路线：1 步

_48%

反应条件：

1.1 Solvents: Tetrahydrofuran ; 4 h, 0 °C
1.2 Reagents: Hydrochloric acid Solvents: Water ; 5 min

参考文献：

Synthesis of optically active N-protected α-amino ketones and α-amino alcohols

Zhou, Zheng Hong; et al, Heteroatom Chemistry, 2003, 14(7), 603-606

合成路线：1 步

2485788-75-6

_88%

反应条件：

1.1 Reagents: Trichloroisocyanuric acid , Sulfuric acid Solvents: Acetonitrile , Water ; 16 h, rt
1.2 Reagents: Triethylamine Solvents: Dichloromethane ; 0 °C → rt; 3 h, rt
1.3 Solvents: Water

参考文献：

Chiral Phosphoric Acid Catalyzed Enantioselective Synthesis of α-Tertiary Amino Ketones from Sulfonium Ylides

Guo, Wengang; et al, Journal of the American Chemical Society, 2020, 142(33), 14384-14390

合成路线：1 步

2142687-00-9

_82%

反应条件：

1.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethyl acetate ; 15 min, 25 °C

参考文献：

Enantioselective decarboxylative chlorination of β-ketocarboxylic acids

Shibatomi, Kazutaka; et al, Nature Communications, 2017, 8,

合成路线：1 步

1072435-12-1

_78%

反应条件：

1.1 Reagents: 1,3-Dibromo-5,5-dimethylhydantoin Solvents: Acetone , Water ; 10 min, 0 °C
1.2 Reagents: Sodium sulfite Solvents: Dichloromethane , Hexane , Water ; 0 °C

参考文献：

α-Amino cyclic dithioketal mediated asymmetric synthesis of (S)-(-)-α-(N-p-toluenesulfonyl)aminopropiophenone (N-tosyl cathinone)

Davis, Franklin A.; et al, ARKIVOC (Gainesville, 2008, (2), 190-203

合成路线：1 步

157394-63-3

_76%

反应条件：

1.1 Reagents: Pyridinium chlorochromate Solvents: Dichloromethane
1.2 Solvents: Diethyl ether

参考文献：

An efficient synthesis of both enantiomers of cathinone by regioselective reductive ring opening of substituted aziridines

Hwang, Gweon Il; et al, Tetrahedron, 1996, 52(37), 12111-12116

合成路线：1 步

_69%

反应条件：

1.1 Reagents: tert-Butylmagnesium chloride Solvents: Toluene , Tetrahydrofuran ; 0 °C; 15 min, 0 °C
1.2 Reagents: 2760961-11-1 Solvents: Diethyl ether ; 0 °C; 15 min, 0 °C; 1 h, 40 °C
1.3 Reagents: Hydrochloric acid Solvents: Water ; 0 °C

参考文献：

Direct Addition of Grignard Reagents to Aliphatic Carboxylic Acids Enabled by Bulky turbo-Organomagnesium Anilides

Colas, Kilian ; et al, Chemistry - A European Journal, 2022, 28(9),

合成路线：1 步

591-51-5

_50%

反应条件：

1.1 Solvents: Diethyl ether , Benzene
1.2 Reagents: Phosphoric acid Solvents: Water

参考文献：

Synthesis and structure elucidation of merucathinone and synthesis of cathinone. Constituents of Catha edulis Forsk

Wolf, Jean Pierre; et al, Helvetica Chimica Acta, 1986, 69(6), 1498-504

合成路线：1 步

72739-14-1

反应条件：

1.1 Reagents: Triethylamine Solvents: Dichloromethane ; 0 °C → rt; 3 h, rt
1.2 Solvents: Water

参考文献：

Chiral Phosphoric Acid Catalyzed Enantioselective Synthesis of α-Tertiary Amino Ketones from Sulfonium Ylides

Guo, Wengang; et al, Journal of the American Chemical Society, 2020, 142(33), 14384-14390

合成路线：2 步

2485766-32-1

104-94-9

反应条件：

1.1 Catalysts: (S)-3,3′-Bis(9-anthryl)-1,1′-binaphthalene-2,2′-diyl hydrogen phosphate Solvents: Toluene ; 72 h, -40 °C
1.2 Catalysts: Cupric acetate ; -40 °C → rt; 0.5 h, rt
2.1 Reagents: Trichloroisocyanuric acid , Sulfuric acid Solvents: Acetonitrile , Water ; 16 h, rt
2.2 Reagents: Triethylamine Solvents: Dichloromethane ; 0 °C → rt; 3 h, rt
2.3 Solvents: Water

参考文献：

Chiral Phosphoric Acid Catalyzed Enantioselective Synthesis of α-Tertiary Amino Ketones from Sulfonium Ylides

Guo, Wengang; et al, Journal of the American Chemical Society, 2020, 142(33), 14384-14390

合成路线：2 步

1072435-09-6

反应条件：

1.1 Reagents: Triethylamine Solvents: Carbon tetrachloride ; 5 min, 0 °C
1.2 0 °C; 0 °C → rt; 8 h, rt
1.3 Reagents: Water ; 0 °C
2.1 Reagents: 1,3-Dibromo-5,5-dimethylhydantoin Solvents: Acetone , Water ; 10 min, 0 °C
2.2 Reagents: Sodium sulfite Solvents: Dichloromethane , Hexane , Water ; 0 °C

参考文献：

α-Amino cyclic dithioketal mediated asymmetric synthesis of (S)-(-)-α-(N-p-toluenesulfonyl)aminopropiophenone (N-tosyl cathinone)

Davis, Franklin A.; et al, ARKIVOC (Gainesville, 2008, (2), 190-203

合成路线：2 步

108-86-1

反应条件：

1.1 Reagents: Chloro(1-methylethyl)magnesium Solvents: Tetrahydrofuran ; 0 °C → rt
2.1 Reagents: Chloro(1-methylethyl)magnesium Solvents: Tetrahydrofuran ; < -10 °C; -15 °C → 0 °C
2.2 Solvents: Tetrahydrofuran ; 0 °C → rt
2.3 Reagents: Hydrochloric acid Solvents: tert-Butyl methyl ether , Water ; 10 °C

参考文献：

Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases

Hemmerling, Martin ; et al, Journal of Medicinal Chemistry, 2017, 60(20), 8591-8605

合成路线：2 步

1117-97-1

反应条件：

1.1 Reagents: Dicyclohexylcarbodiimide Solvents: Chloroform
2.1 Solvents: Tetrahydrofuran ; 4 h, 0 °C
2.2 Reagents: Hydrochloric acid Solvents: Water ; 5 min

参考文献：

Synthesis of optically active N-protected α-amino ketones and α-amino alcohols

Zhou, Zheng Hong; et al, Heteroatom Chemistry, 2003, 14(7), 603-606

合成路线：2 步

反应条件：

1.1 Reagents: Hydrogen Catalysts: Palladium dihydroxide Solvents: Ethyl acetate
2.1 Reagents: Pyridinium chlorochromate Solvents: Dichloromethane
2.2 Solvents: Diethyl ether

参考文献：

An efficient synthesis of both enantiomers of cathinone by regioselective reductive ring opening of substituted aziridines

Hwang, Gweon Il; et al, Tetrahedron, 1996, 52(37), 12111-12116

合成路线：2 步

6638-79-5