DayangChem exported this product to many countries and regions at best price. If you are looking for the material's manufacturer or supplier in China, DayangChem is your best choice. Pls contact with us freely for getting detailed product spe
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inquiry(alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-L-phenylalanine CAS No.:868540-16-3 Name: (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-L-phenyla
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inquiry(alphaS)-alpha-[(4-Morpholinylacetyl)aMino]benzenebutanoyl-L-leucyl-L-phenylalanine CAS:868540-16-3 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of c
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inquiryHello, dear friend! I'm Hansen and Allen from China. Welcome to my lookchem mall! The following is a brief introduction of our company's products and services. If you are interested in our products, please contact us by emai
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inquiryAppearance:white or light yellow crystalline powder Storage:Store in a cool,dry place and keep away from direct strong light Package:As customer request Application:Carfilzomib intermediate 2 Transportation:By Sea/Air/Courier Po
Cas:868540-16-3
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inquiryProName: (alphaS)-alpha-[(4-Morpholinylacetyl)a... CasNo: 868540-16-3 Molecular Formula: C31H42N4O6 Appearance: detailed see specifications Application: An important raw material and intermed... DeliveryTime: prompt PackAge: according to the
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inquiryProduct name: Carfilzomib Intermediates I CAS No.:868540-16-3 Molecule Formula:C31H42N4O6 Molecule Weight:566.68 Purity: 99% Package: 25kg/drum Description:White crystalline powder Manufacture Standards:Enterprise Standard TESTIN
Cas:868540-16-3
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inquiryProduct Details Grade: pharmaceutical grade Purity:99%+ ProductionCapacity: 1000 Kilogram/Month Scope of use: For scientific research only(The product must be used legally) Our Advantage 1. Best quality with competitive price. 2. Quick shipping,
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inquiry(S)-benzyl 2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido) pentanamido)-3-phenylpropanoate
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
With methanol; hydrogen; palladium 10% on activated carbon In ethyl acetate under 760.051 Torr; for 2h; | |
With palladium on activated charcoal; ammonium formate In methanol at 25 - 30℃; for 2h; Solvent; Reagent/catalyst; | 77 g |
With 5 mol% Pd/C; hydrogen In methanol for 0.5h; |
N-tert-butoxycarbonyl-L-leucine
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine; (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate / N,N-dimethyl-formamide / 0 °C / Inert atmosphere 2.1: trifluoroacetic acid / dichloromethane / 2 h / 0 - 20 °C 2.2: 0 - 20 °C / Inert atmosphere 3.1: trifluoroacetic acid / dichloromethane / 1 h / 20 °C 3.2: 0 - 20 °C / Inert atmosphere 4.1: potassium iodide / tetrahydrofuran / Inert atmosphere 5.1: lithium hydroxide / methanol; water / 12 h / 0 - 5 °C View Scheme | |
Multi-step reaction with 6 steps 1: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 2: hydrogenchloride / isopropyl alcohol / 2 h / 25 - 30 °C 3: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 4: hydrogenchloride / ethyl acetate / 2 h / 25 - 30 °C 5: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 6: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 2 - 30 °C 2.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 2.2: 2 - 30 °C 3.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 3.2: 2 - 30 °C 4.1: ammonium formate; palladium on activated charcoal / methanol / 2 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 2 - 30 °C 2.1: dichloromethane / 2 h / 0 - 30 °C 3.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / acetonitrile / 0 - 30 °C / Inert atmosphere 4.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 4.2: 2 - 30 °C 5.1: ammonium formate; palladium on activated charcoal / methanol / 2 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 6 steps 1: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 2: dichloromethane / 1 h / 20 °C 3: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 4: dichloromethane / 1 h / 20 °C 5: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 6: 5 mol% Pd/C; hydrogen / methanol / 0.5 h View Scheme |
methyl (2S)-2-amino-3-phenylpropanoate
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine; (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate / N,N-dimethyl-formamide / 0 °C / Inert atmosphere 2.1: trifluoroacetic acid / dichloromethane / 2 h / 0 - 20 °C 2.2: 0 - 20 °C / Inert atmosphere 3.1: trifluoroacetic acid / dichloromethane / 1 h / 20 °C 3.2: 0 - 20 °C / Inert atmosphere 4.1: potassium iodide / tetrahydrofuran / Inert atmosphere 5.1: lithium hydroxide / methanol; water / 12 h / 0 - 5 °C View Scheme | |
Multi-step reaction with 6 steps 1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 2: dichloromethane / 3 h / 0 - 20 °C 3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 4: dichloromethane / 3 h / 0 - 20 °C 5: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 6: lithium hydroxide monohydrate / methanol / 3 h / 0 - 20 °C View Scheme |
(N-(tert-butoxycarbonyl)-L-leucinyl)-L-phenylalanine methyl ester
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: trifluoroacetic acid / dichloromethane / 2 h / 0 - 20 °C 1.2: 0 - 20 °C / Inert atmosphere 2.1: trifluoroacetic acid / dichloromethane / 1 h / 20 °C 2.2: 0 - 20 °C / Inert atmosphere 3.1: potassium iodide / tetrahydrofuran / Inert atmosphere 4.1: lithium hydroxide / methanol; water / 12 h / 0 - 5 °C View Scheme | |
Multi-step reaction with 5 steps 1: hydrogenchloride / isopropyl alcohol / 2 h / 25 - 30 °C 2: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 3: hydrogenchloride / ethyl acetate / 2 h / 25 - 30 °C 4: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 5: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 5 steps 1: dichloromethane / 3 h / 0 - 20 °C 2: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 3: dichloromethane / 3 h / 0 - 20 °C 4: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 5: lithium hydroxide monohydrate / methanol / 3 h / 0 - 20 °C View Scheme |
(S)-methyl 2-((S)-2-tert.butoxycarbonyIamino-4-phenylbutanamido-4-methylpentanamido)-3-phenylpropanoate
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: trifluoroacetic acid / dichloromethane / 1 h / 20 °C 1.2: 0 - 20 °C / Inert atmosphere 2.1: potassium iodide / tetrahydrofuran / Inert atmosphere 3.1: lithium hydroxide / methanol; water / 12 h / 0 - 5 °C View Scheme | |
Multi-step reaction with 3 steps 1: hydrogenchloride / ethyl acetate / 2 h / 25 - 30 °C 2: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 3: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 3 steps 1: dichloromethane / 3 h / 0 - 20 °C 2: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 3: lithium hydroxide monohydrate / methanol / 3 h / 0 - 20 °C View Scheme |
C28H36ClN3O5
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: potassium iodide / tetrahydrofuran / Inert atmosphere 2: lithium hydroxide / methanol; water / 12 h / 0 - 5 °C View Scheme |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
With lithium hydroxide In methanol; water at 0 - 5℃; for 12h; | |
With lithium hydroxide monohydrate; water In tetrahydrofuran at 25 - 30℃; for 3h; | 48.0 g |
With lithium hydroxide monohydrate In methanol at 0 - 20℃; for 3h; |
(S)-methyl 2-((S)-2-amino-4-methylpentanamido)-3-phenylpropanoate hydrochloride
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 2: hydrogenchloride / ethyl acetate / 2 h / 25 - 30 °C 3: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 4: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme |
Boc-L-homophenylalanine
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 2: hydrogenchloride / ethyl acetate / 2 h / 25 - 30 °C 3: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 4: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 2: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme |
L-leucine
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: sodium hydroxide / water / 20 h / 25 - 30 °C 2: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 3: hydrogenchloride / isopropyl alcohol / 2 h / 25 - 30 °C 4: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 5: hydrogenchloride / ethyl acetate / 2 h / 25 - 30 °C 6: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 7: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme |
methyl (2S)-2-amino-3-phenylpropanoate hydrochloride
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 2: hydrogenchloride / isopropyl alcohol / 2 h / 25 - 30 °C 3: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 4: hydrogenchloride / ethyl acetate / 2 h / 25 - 30 °C 5: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 6: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme |
L-phenylalanine
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: thionyl chloride / 8 h / 25 - 30 °C 2: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 3: hydrogenchloride / isopropyl alcohol / 2 h / 25 - 30 °C 4: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 5: hydrogenchloride / ethyl acetate / 2 h / 25 - 30 °C 6: benzotriazol-1-ol; 4-methyl-morpholine; dicyclohexyl-carbodiimide / dichloromethane / 2 h / 0 - 30 °C / Inert atmosphere 7: lithium hydroxide monohydrate; water / tetrahydrofuran / 3 h / 25 - 30 °C View Scheme |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / acetonitrile / 0 - 30 °C / Inert atmosphere 2.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 2.2: 2 - 30 °C 3.1: ammonium formate; palladium on activated charcoal / methanol / 2 h / 25 - 30 °C View Scheme |
L-phenylalanine benzyl ester hydrochloride
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 2 - 30 °C 2.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 2.2: 2 - 30 °C 3.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 3.2: 2 - 30 °C 4.1: ammonium formate; palladium on activated charcoal / methanol / 2 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 2 - 30 °C 2.1: dichloromethane / 2 h / 0 - 30 °C 3.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / acetonitrile / 0 - 30 °C / Inert atmosphere 4.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 4.2: 2 - 30 °C 5.1: ammonium formate; palladium on activated charcoal / methanol / 2 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 6 steps 1: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 2: dichloromethane / 1 h / 20 °C 3: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 4: dichloromethane / 1 h / 20 °C 5: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 6: 5 mol% Pd/C; hydrogen / methanol / 0.5 h View Scheme |
(S)-benzyl 2-((S)-2-(tert-butoxycarbonylamino)-4-methylpentanamido)-3-phenylpropanoate
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 1.2: 2 - 30 °C 2.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 2.2: 2 - 30 °C 3.1: ammonium formate; palladium on activated charcoal / methanol / 2 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: dichloromethane / 2 h / 0 - 30 °C 2.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / acetonitrile / 0 - 30 °C / Inert atmosphere 3.1: trifluoroacetic acid / dichloromethane / 2 h / 2 - 30 °C 3.2: 2 - 30 °C 4.1: ammonium formate; palladium on activated charcoal / methanol / 2 h / 25 - 30 °C View Scheme | |
Multi-step reaction with 5 steps 1: dichloromethane / 1 h / 20 °C 2: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 3: dichloromethane / 1 h / 20 °C 4: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 5: 5 mol% Pd/C; hydrogen / methanol / 0.5 h View Scheme |
morpholin-4-ylacetic acid
Fmoc-Leu-OH
N-(fluorenyl-9-methoxycarbonyl)-L-homophenylalanine
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Stage #1: Fmoc-phenylalanine-2-chlorotrityl resin With piperidine In N,N-dimethyl-formamide solid-phase peptide synthesis; Stage #2: Fmoc-Leu-OH With O‑(6‑chlorobezotriazol‑1‑yl)‑N,N,N,N‑tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide solid-phase peptide synthesis; Stage #3: morpholin-4-ylacetic acid; N-(fluorenyl-9-methoxycarbonyl)-L-homophenylalanine Further stages; |
(S)-benzyl 2-((S)-2-amino-4-methylpentanamido)-3-phenylpropanoate TFA salt
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 2: dichloromethane / 1 h / 20 °C 3: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 4: 5 mol% Pd/C; hydrogen / methanol / 0.5 h View Scheme |
(S)-benzyl 2-((S)-2-((S)-2-(tert-butoxycarbonylamino)-4-phenylbutanamido)-4-methylpentanamido)-3-phenylpropanoate
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: dichloromethane / 1 h / 20 °C 2: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 3: 5 mol% Pd/C; hydrogen / methanol / 0.5 h View Scheme |
C2HF3O2*C32H39N3O4
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; benzotriazol-1-ol / dichloromethane / 18 h / 20 °C 2: 5 mol% Pd/C; hydrogen / methanol / 0.5 h View Scheme |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 2: dichloromethane / 3 h / 0 - 20 °C 3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 4: lithium hydroxide monohydrate / methanol / 3 h / 0 - 20 °C View Scheme |
C2HF3O2*C26H35N3O4
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 2: lithium hydroxide monohydrate / methanol / 3 h / 0 - 20 °C View Scheme |
N-tert-butoxycarbonyl-L-phenylalanine
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: thionyl chloride / 2 h / 0 - 20 °C 2: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 3: dichloromethane / 3 h / 0 - 20 °C 4: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 5: dichloromethane / 3 h / 0 - 20 °C 6: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C 7: lithium hydroxide monohydrate / methanol / 3 h / 0 - 20 °C View Scheme |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-ol; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; diethylamine In N,N-dimethyl-formamide at -5℃; for 1.5h; | 88% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With benzotriazol-1-ol In dichloromethane for 0.333333h; Stage #2: C9H17NO2*C2HF3O2 With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 12.5h; Cooling; | 87% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-ol; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; diethylamine In N,N-dimethyl-formamide at -5℃; for 1.5h; Temperature; Reagent/catalyst; | 86% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
(4S,7S,10S,13S,15R)-10-benzyl-15-hydroxy-7,13-diisobutyl-15-methyl-1-morpholino-2,5,8,11,14-pentaoxo-4-phenethyl-3,6,9,12-tetraazahexadecan-16-yl 3-(prop-2-yn-1-ylcarbamoyl)benzenesulfonate
Conditions | Yield |
---|---|
Stage #1: (2R,4S)-4-((tert-butoxycarbonyl)amino)-2-hydroxy-2,6-dimethyl-3-oxoheptyl 3-(prop-2-yn-1-yloxy)propane-1-sulfonate With hydrogenchloride In 1,4-dioxane at 20℃; for 1h; Stage #2: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With benzotriazol-1-ol; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 0℃; for 0.5h; | 80% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
(S)-2-amino-1-((R)-2-methyloxiran-2-yl)-3-phenylpropan-1-one trifluoroacetate
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With benzotriazol-1-ol In dichloromethane for 0.333333h; Stage #2: (S)-2-amino-1-((R)-2-methyloxiran-2-yl)-3-phenylpropan-1-one trifluoroacetate With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 12.5h; Cooling; | 80% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
(S)-4-methyl-N-((S)-1-(((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-4-phenylbutan-2 -yl)amino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With benzotriazol-1-ol In dichloromethane for 0.333333h; Stage #2: C13H17NO2*C2HF3O2 With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 12.5h; Cooling; | 76% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With benzotriazol-1-ol In dichloromethane for 0.333333h; Stage #2: C7H13NO2*C2HF3O2 With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 12.5h; Cooling; | 73% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
trifluoroacetic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane at 0℃; for 0.333333h; Stage #2: C16H21NO5S*ClH In dichloromethane at 0℃; for 0.166667h; Stage #3: trifluoroacetic acid With N-ethyl-N,N-diisopropylamine In water; acetonitrile at 20℃; | 60% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
trifluoroacetic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane at 0℃; for 0.333333h; Stage #2: C12H19NO3S*ClH In dichloromethane at 0℃; for 0.166667h; Stage #3: trifluoroacetic acid With N-ethyl-N,N-diisopropylamine In water; acetonitrile at 20℃; | 53% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-ol; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 18h; | 48% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane at 0℃; for 0.333333h; Stage #2: L-Leu-[CH2SO2]-DFHMC . HC1 In dichloromethane at 0℃; for 0.166667h; Stage #3: With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; | 47.3% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
trifluoroacetic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane at 0℃; for 0.333333h; Stage #2: L-Leu-[CH2SO2]-DFHMC . HC1 In dichloromethane at 0℃; for 0.166667h; Stage #3: trifluoroacetic acid With N-ethyl-N,N-diisopropylamine In water; acetonitrile at 20℃; | 47% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-ol; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 18h; | 45% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
trifluoroacetic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane at 0℃; for 0.333333h; Stage #2: C12H14F5NO3S*ClH In dichloromethane at 0℃; for 0.166667h; Stage #3: trifluoroacetic acid With N-ethyl-N,N-diisopropylamine In water; acetonitrile at 20℃; | 36% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
trifluoroacetic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane at 0℃; for 0.333333h; Stage #2: C16H20FNO5S*ClH In dichloromethane at 0℃; for 0.166667h; Stage #3: trifluoroacetic acid With N-ethyl-N,N-diisopropylamine In water; acetonitrile at 20℃; | 31% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
trifluoroacetic acid
Conditions | Yield |
---|---|
Stage #1: (S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane at 0℃; for 0.333333h; Stage #2: C12H16F3NO3S*ClH In dichloromethane at 0℃; for 0.166667h; Stage #3: trifluoroacetic acid With N-ethyl-N,N-diisopropylamine In water; acetonitrile at 20℃; | 23% |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
(2S)-2-amino-4-methyl-1-[(2R)-2-methyloxiran-2-yl]pentan-1-one
Conditions | Yield |
---|---|
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine In acetonitrile at 0 - 5℃; |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate / N,N-dimethyl-formamide / 1.5 h / 0 - 5 °C 2: tetrahydrofuran; acetonitrile / 2 h / 20 °C View Scheme |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-ol; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 0 - 5℃; for 1.5h; Reagent/catalyst; Temperature; Solvent; stereoselective reaction; | 230 g |
With 4-methyl-morpholine; benzotriazol-1-ol; HATU In N,N-dimethyl-formamide at 0 - 5℃; for 3h; Inert atmosphere; | 100.0 g |
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine In acetonitrile at 0 - 5℃; Inert atmosphere; | 0.08 g |
Multi-step reaction with 2 steps 1.1: benzotriazol-1-ol; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / acetonitrile / -10 - -5 °C 1.2: 0.5 h / 25 - 30 °C 2.1: sodium hydrogencarbonate / dichloromethane; water / 0.17 h / 2 - 6 °C View Scheme |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate / 1 h / 0 °C 2: tetrahydrofuran; acetonitrile / 2 h / 20 °C View Scheme |
(S)-2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenyipropanoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-ol; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine at 0℃; for 1h; |
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