Production Method 1

915697-62-0

88321-09-9

Reaction Conditions

1.1 Reagents: Potassium hydroxide Solvents: Water ;  2 h, 0 °C

Reference

Stereoselective synthesis of the epoxysuccinyl peptide E-64c

Lygo, Barry; et al, Synlett, 2006, (13), 2063-2066

Production Method 2

84851-37-6

89886-73-7

88321-09-9

Reaction Conditions

1.1 Reagents: Dicyclohexylcarbodiimide ,  1-Hydroxybenzotriazole Solvents: Ethyl acetate ;  3 h, 0 °C; 12 h, rt

Reference

Design, synthesis, and screen of cathepsin K inhibitors

Yu, Ying-Ying; et al, Chinese Chemical Letters, 2013, 24(8), 715-718

Production Method 3

89886-73-7

88321-09-9

Reaction Conditions

1.1 Reagents: Dicyclohexylcarbodiimide Solvents: Ethyl acetate
2.1 Solvents: Ethyl acetate

Reference

An efficient synthetic method for ethyl (+)-(2S,3S)-3-[(S)-3-methyl-1-(3-methylbutylcarbamoyl)butylcarbamoyl]-2-oxiranecarboxylate (EST), a new inhibitor of cysteine proteinases

Tamai, Masaharu; et al, Chemical & Pharmaceutical Bulletin, 1987, 35(3), 1098-104

Production Method 4

75657-73-7

88321-09-9

Reaction Conditions

1.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Methanol ,  Ethyl acetate
2.1 Reagents: 4-Methylmorpholine ,  1-Hydroxybenzotriazole ,  1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Chloroform
2.2 Solvents: Ethyl acetate ,  Water

Reference

A new synthesis of peptidyl epoxysuccinates for probing cysteine protease-inhibitor P3/S3 binding interactions

Roush, William R.; et al, Synthesis, 1999, 1500, 1500-1504

Production Method 5

84863-67-2

88321-09-9

Reaction Conditions

1.1 Reagents: Hydrochloric acid Solvents: Ethyl acetate
2.1 Solvents: Ethyl acetate

Reference

An efficient synthetic method for ethyl (+)-(2S,3S)-3-[(S)-3-methyl-1-(3-methylbutylcarbamoyl)butylcarbamoyl]-2-oxiranecarboxylate (EST), a new inhibitor of cysteine proteinases

Tamai, Masaharu; et al, Chemical & Pharmaceutical Bulletin, 1987, 35(3), 1098-104

Production Method 6

915697-61-9

88321-09-9

Reaction Conditions

1.1 Reagents: 1-Hydroxybenzotriazole ,  1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Dichloromethane ,  4-Methylmorpholine
2.1 Reagents: m-Chloroperbenzoic acid Solvents: Chloroform ;  50 °C
3.1 Reagents: Potassium hydroxide Solvents: Water ;  2 h, 0 °C

Reference

Stereoselective synthesis of the epoxysuccinyl peptide E-64c

Lygo, Barry; et al, Synlett, 2006, (13), 2063-2066

Production Method 7

174759-66-1

88321-09-9

Reaction Conditions

1.1 Reagents: 4-Methylmorpholine ,  1-Hydroxybenzotriazole ,  1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Chloroform
1.2 Solvents: Ethyl acetate ,  Water

Reference

A new synthesis of peptidyl epoxysuccinates for probing cysteine protease-inhibitor P3/S3 binding interactions

Roush, William R.; et al, Synthesis, 1999, 1500, 1500-1504

Production Method 8

84851-37-6

100464-19-5

88321-09-9

Reaction Conditions

1.1 Solvents: Ethyl acetate

Reference

An efficient synthetic method for ethyl (+)-(2S,3S)-3-[(S)-3-methyl-1-(3-methylbutylcarbamoyl)butylcarbamoyl]-2-oxiranecarboxylate (EST), a new inhibitor of cysteine proteinases

Tamai, Masaharu; et al, Chemical & Pharmaceutical Bulletin, 1987, 35(3), 1098-104

Production Method 9

848778-06-3

88321-09-9

Reaction Conditions

1.1 Reagents: Lithium ethoxide Solvents: Ethanol ;  10 min, rt
1.2 Reagents: 4-(Dimethylamino)pyridine ,  1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Dimethylformamide ;  4 h, rt

Reference

Stereoselective synthesis of E-64 and related cysteine proteases inhibitors from 2,3-epoxyamides

Sarabia, Francisco; et al, Bioorganic & Medicinal Chemistry, 2005, 13(5), 1691-1705

Production Method 10

73890-18-3

88321-09-9

Reaction Conditions

1.1 Reagents: Potassium hydroxide Solvents: Water ;  1 h, 4 °C → 6 °C; 4 h, rt
2.1 Reagents: Dicyclohexylcarbodiimide ,  1-Hydroxybenzotriazole Solvents: Ethyl acetate ;  3 h, 0 °C; 12 h, rt

Reference

Design, synthesis, and screen of cathepsin K inhibitors

Yu, Ying-Ying; et al, Chinese Chemical Letters, 2013, 24(8), 715-718

Production Method 11

84863-67-2

88321-09-9

Reaction Conditions

1.1 Reagents: Hydrochloric acid Solvents: Ethyl acetate ;  2.5 h, rt
2.1 Reagents: Dicyclohexylcarbodiimide ,  1-Hydroxybenzotriazole Solvents: Ethyl acetate ;  3 h, 0 °C; 12 h, rt

Reference

Design, synthesis, and screen of cathepsin K inhibitors

Yu, Ying-Ying; et al, Chinese Chemical Letters, 2013, 24(8), 715-718

Production Method 12

848778-05-2

88321-09-9

Reaction Conditions

1.1 Reagents: 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone Solvents: Benzene ;  72 h, reflux
2.1 Reagents: Lithium ethoxide Solvents: Ethanol ;  10 min, rt
2.2 Reagents: 4-(Dimethylamino)pyridine ,  1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Dimethylformamide ;  4 h, rt

Reference

Stereoselective synthesis of E-64 and related cysteine proteases inhibitors from 2,3-epoxyamides

Sarabia, Francisco; et al, Bioorganic & Medicinal Chemistry, 2005, 13(5), 1691-1705

Production Method 13

915697-59-5

88321-09-9

Reaction Conditions

1.1 Reagents: m-Chloroperbenzoic acid Solvents: Chloroform ;  50 °C
2.1 Reagents: Potassium hydroxide Solvents: Water ;  2 h, 0 °C

Reference

Stereoselective synthesis of the epoxysuccinyl peptide E-64c

Lygo, Barry; et al, Synlett, 2006, (13), 2063-2066

Production Method 14

13139-15-6

88321-09-9

Reaction Conditions

1.1 Reagents: Dicyclohexylcarbodiimide ,  1-Hydroxybenzotriazole Solvents: Ethanol ;  1.5 h, 3 °C → 8 °C; 2.5 h, rt
2.1 Reagents: Hydrochloric acid Solvents: Ethyl acetate ;  2.5 h, rt
3.1 Reagents: Dicyclohexylcarbodiimide ,  1-Hydroxybenzotriazole Solvents: Ethyl acetate ;  3 h, 0 °C; 12 h, rt

Reference

Design, synthesis, and screen of cathepsin K inhibitors

Yu, Ying-Ying; et al, Chinese Chemical Letters, 2013, 24(8), 715-718

Production Method 15

17087-75-1

88321-09-9

Reaction Conditions

1.1 Reagents: Sulfuric acid ;  4.5 h, reflux
2.1 Reagents: Potassium hydroxide Solvents: Water ;  1 h, 4 °C → 6 °C; 4 h, rt
3.1 Reagents: Dicyclohexylcarbodiimide ,  1-Hydroxybenzotriazole Solvents: Ethyl acetate ;  3 h, 0 °C; 12 h, rt

Reference

Design, synthesis, and screen of cathepsin K inhibitors

Yu, Ying-Ying; et al, Chinese Chemical Letters, 2013, 24(8), 715-718

Production Method 16

1738-69-8

89886-73-7

88321-09-9

Reaction Conditions

1.1 Reagents: 4-Methylmorpholine ,  1-Hydroxybenzotriazole ,  1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Chloroform
1.2 Solvents: Ethyl acetate ,  Water
2.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Methanol ,  Ethyl acetate
3.1 Reagents: 4-Methylmorpholine ,  1-Hydroxybenzotriazole ,  1-Ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride Solvents: Chloroform
3.2 Solvents: Ethyl acetate ,  Water

Reference

A new synthesis of peptidyl epoxysuccinates for probing cysteine protease-inhibitor P3/S3 binding interactions

Roush, William R.; et al, Synthesis, 1999, 1500, 1500-1504

Aloxistatin Raw materials

• benzyl (2S)-2-amino-4-methylpentanoate
• 174759-66-1
• 2-Oxiranecarboxamide, 3-benzoyl-N-[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]-, (2S,3S)-
• BOC-S-N\'異己烷-亮氨酰胺
• S-2-Amino-4-methylpentanoic acid (3-methylbutyl)amide
• (2S,3S)-2,3-Oxiranedicarboxylic Acid Monoethyl Ester
• Boc-L-Leu-OH
• 2-Oxiranecarboxylic acid, 3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-, phenyl ester, (2S,3S)-
• (2S,3S)-3-(1H-Indol-1-ylcarbonyl)-N-[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]-2-oxiranecarboxamide
• (2S,3S)-3-[(2,3-Dihydro-1H-indol-1-yl)carbonyl]-N-[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]-2-oxiranecarboxamide
• Ethyl-(2S,3S)-(p-nitrophenyl)-oxirane-2,3-dicarboxylate
• 2,3-Oxiranedicarboxylicacid, (2S,3S)-
• L-Leucine, N-[[(2S,3S)-3-benzoyl-2-oxiranyl]carbonyl]-
• Oxiranecarboxylic acid, 3-[[[(1S)-3-methyl-1-[(phenylmethoxy)carbonyl]butyl]amino]carbonyl]-, ethyl ester, (2S,3S)- (9CI)
• 2,3-Oxiranedicarboxylicacid, 2,3-diethyl ester, (2S,3S)-

Aloxistatin Preparation Products

• Aloxistatin (88321-09-9)

• 1. Aggregated-fluorescent detection of PFAS with a simple chip
  Cheng Fang,Jinjian Wu,Zahra Sobhani,Md. Al Amin,Youhong Tang Anal. Methods, 2019,11, 163-170
• 2. An integrated cathode and solid electrolyte via in situ polymerization with significantly reduced interface resistance?
  Jialiang Yuan,Ran Dong,Yuan Li,Yang Liu,Zhuo Zheng,Yuxia Liu,Yan Sun,Benhe Zhong,Zhenguo Wu,Xiaodong Guo Chem. Commun., 2021,57, 13004-13007
• 3. An insight into the role of side chains in the microstructure and carrier mobility of high-performance conjugated polymers?
  Jianyao Huang,Dong Gao,Zhihui Chen,Weifeng Zhang Polym. Chem., 2021,12, 2471-2480
• 4. An Aptamer Bio-barCode (ABC) assay using SPR, RNase H, and probes with RNA and gold-nanorods for anti-cancer drug screening
  Chengbin Yang,Hing Lun Tsang,Pui Man Lau,Ken-Tye Yong,Ho Pui Ho,Siu Kai Kong Analyst, 2017,142, 3579-3587
• 5. An alumina stabilized graphene oxide wrapped SnO2 hollow sphere LIB anode with improved lithium storage?
  Xiang Liu,Qian Sun,A. B. Djuri?i?,Maohai Xie,Baohu Dai,Jinyao Tang,Charles Surya,Changzhong Liao,Kaimin Shih RSC Adv., 2015,5, 100783-100789

• Other Chemical additives Functional Additives

• 81719-38-2(Oxiranecarboxylic acid, 3-[[[(1S)-1-[[(7-aminoheptyl)amino]carbonyl]-3-methylbutyl]amino]carbonyl]-, (2S,3S)- (9CI))
• 79385-96-9(Destruxin E1 (9CI))
• 646533-01-9(2-Oxiranecarboxylic acid, 3-[[[(1S)-1-(aminocarbonyl)-3-methylbutyl]amino]carbonyl]-, (2S,3S)-)
• 76684-89-4(E 64c)
• 646533-02-0(2-Oxiranecarboxylic acid, 3-[[[(1S)-1-(aminocarbonyl)-3-methylbutyl]amino]carbonyl]-, (2R,3R)-)
• 76739-51-0(2-Oxiranecarboxylicacid,3-[[[(1S)-1-[[(4-aminobutyl)amino]carbonyl]-3-methylbutyl]amino]carbonyl]-,(2S,3S)-)
• 160825-48-9(Oxiranecarboxylic acid,3-[[[1-[[(5-hydroxypentyl)amino]carbonyl]-3-methylbutyl]amino]carbonyl]- (9CI))
• 134447-97-5(L-Proline,N-[[(2S,3S)-3-(ethoxycarbonyl)-2-oxiranyl]carbonyl]-L-isoleucyl-)
• 160825-49-0(L-Lysine,N6-[N-[(3-carboxyoxiranyl)carbonyl]-L-leucyl]- (9CI))
• 89819-78-3(2-Oxiranecarboxylic acid, 3-[[[1-[[(5-aminopentyl)amino]carbonyl]-3-methylbutyl]amino]carbonyl]-)