61477-40-5

Basic information

• Product Name: (R)-3-AMINO-1-BUTANOL
• Synonyms: R-3-amino-1-butanol;(3R)-3-Amino-1-butanol;1-Butanol,3-aMino-, (3R)-;(-)-(R)-3-aMinopropan-1-ol;(3R)-3-aMinobutan-1-ol;R-3-aMnio-butanol;Dolutegravir INT 2;(R)-3-AMINO-1-BUTANO
• CAS NO: 61477-40-5
• Molecular Formula: C₄H₁₁NO
• Molecular Weight: 89.14
• EINECS: 1592732-453-0
• Product Categories: Dolutegravir intermediate
• Mol File: 61477-40-5.mol

Chemical Properties

• Boiling Point: 168℃
• Flash Point: 56℃
• Appearance: /
• Density: 0.927
• Refractive Index: 1.4530 to 1.4570
• Storage Temp.: under inert gas (nitrogen or Argon) at 2–8 °C
• PKA: 15.00±0.10(Predicted)
• CAS DataBase Reference: (R)-3-AMINO-1-BUTANOL(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-3-AMINO-1-BUTANOL(61477-40-5)
• EPA Substance Registry System: (R)-3-AMINO-1-BUTANOL(61477-40-5)

Safety Data

• RIDADR: 2735
• HazardClass: 8
• PackingGroup: Ⅲ
• Hazardous Substances Data: 61477-40-5(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
(R)-3-AMINO-1-BUTANOL is used as a key intermediate for the synthesis of chiral drugs for various medical applications. Its chiral nature allows for the creation of drugs with specific therapeutic effects, targeting different receptors and pathways in the body.
Used in Drug Development:
(R)-3-AMINO-1-BUTANOL is utilized in drug development as a building block for designing and creating novel pharmaceutical compounds. Its versatility in chemical reactions enables the development of new drugs with improved efficacy, safety, and selectivity.
Used in Chiral Synthesis:
In the field of chiral synthesis, (R)-3-AMINO-1-BUTANOL is used as a starting material for the production of enantiomerically pure compounds. This is essential for creating drugs with desired pharmacological properties, as the stereochemistry of a molecule can significantly impact its biological activity.
Used in Research and Development:
(R)-3-AMINO-1-BUTANOL is also employed in research and development laboratories for studying the effects of chirality on drug action, metabolism, and toxicity. This helps in understanding the role of stereochemistry in drug design and development, leading to more effective and safer medications.

Synthesis

Release of (R)-3-amino-1-butanol From the (S)-mandelic Salt Thereof; The (S)-mandelic salt of (R)-3-amino-1-butanol obtained in Example 1.1 (372 g, 1.54 mol) was suspended in triethanolamine (1 I) at 80° C., and the slurry was admixed with sodium methoxide (277.6 g, 1.54 mol; 30% in methanol), which gave a clear solution. This was heated to 100° C. and vacuum was applied. In a stepwise manner, a pressure of 750, 500, 250, 100, 50 and finally 20 mbar was applied. Through an attached Claisen distillation head (no return stream, no column), a clear distillate distilled over at a top temperature of 50 to 60° C., which was predominantly methanol. The pressure was then lowered further to 5 mbar, and (R)-3-amino-1-butanol distilled over at a top temperature of 76° C. The product was distilled once again in a water jet pump vacuum, in the course of which (R)-3-amino-1-butanol distilled over at 93° C. and 26 mbar. This gave 125 g (91% of theory) of (R)-3-amino-1-butanol as a colorless liquid with an optical purity of 99.6% ee.The optical purity of (R)-3-amino-1-butanol was determined by means of GC. To this end, (R)-3-amino-1-butanol (200 mg) and triethylamine (300 mg) were dissolved in diethyl ether (15 ml) and admixed with trifluoroacetic anhydride (0.6 ml). After stirring for 30 minutes, saturated ammonium chloride solution (5 ml) was added and the mixture was stirred for a further 15 minutes. Subsequently, the mixture was left to stand until two phases had formed, and a sample of the upper clear phase was analyzed by GC.Column: Hydrodex-TBDAc, 25 m×0.25 mm, Macherey & NagelInlet temperature: 250° C.Detector temperature: 250° C.Injection volume : 0.5 μlMode: SplitSplit ratio: 100:1Carrier gas: HeFlow: 0.8 ml/min (constant flow)Program:Initial temperature: 135° C.Initial time: 10 minRate: 5° C./minFinal temperature: 170° C.Final time: 35 minRetention times:R enantiomer: 17.68 min (N-trifluoroacylated) 21.23 min (N,O-bis-trifluoroacylated)S enantiomer: 18.24 min (N-trifluoroacylated) 20.11 min (N,O-bis-trifluoroacylated)

Synthetic route

(R)-3-acetamidobutanol → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
In ethanol at 70 - 80℃; Alkaline conditions;	97.5%

(-)-(3R)-3-((benzyloxycarbonyl)amino)butanol (866395-21-3) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With palladium 10% on activated carbon; hydrogen In ethanol at 50 - 60℃; under 3000.3 - 4500.45 Torr;	96%

(-)-tert-butyl [(R)-3-hydroxy-1-methylpropyl]carbamate (167216-17-3) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With trifluoroacetic acid In dichloromethane at 0 - 10℃;	95.8%
With hydrogenchloride In methanol; water at 25℃; for 6h; Green chemistry;	90%
With hydrogenchloride In methanol at 25℃;	0.5 g

(3R)-3-{[(1R)-1-phenylethyl]amino}butan-1-ol → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With platinum on carbon In ethanol at 60℃; under 15001.5 Torr; for 10h; Reagent/catalyst;	95.4%

(R)-3-amino-1-butanol L-malate → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With sodium methylate In methanol at 20℃; Solvent; Reagent/catalyst;	95.3%
With sodium hydroxide In isopropyl alcohol at 10 - 20℃; for 0.666667h;	12.9 g

(R)-3-amino-1-butanol tartarate → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With potassium carbonate In acetonitrile at 40 - 45℃; Reagent/catalyst; Temperature;	95%

(R)-3-benzamido-1-butanol → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
In ethanol at 70 - 80℃; Alkaline conditions;	92.6%
With hydrogenchloride In water for 3h; Reflux;	90%

(R)-4-hydroxybutan-2-aminium (S)-2-hydroxy-2-phenylacetate (1236049-43-6) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With triethanolamine; sodium methylate In methanol at 80 - 100℃; under 3.75038 - 562.556 Torr;	91%
With sodium methylate In methanol at 20℃; for 2h;	35 g
With sodium methylate In methanol at 65℃; for 17h;

(R)-3-aminobutanol tartrate → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With potassium carbonate In methanol at 45 - 50℃; for 12h;	90%

(R)-3-aminobutanoic acid (3775-73-3) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With sodium tetrahydroborate; trifluoroacetic acid In tetrahydrofuran at 20℃; Reagent/catalyst; Temperature; Solvent; Inert atmosphere; Cooling with ice;	84.3%
With sodium tetrahydroborate; zinc(II) chloride In tetrahydrofuran at 20 - 60℃; for 3.5h; Autoclave;	54%

(R)-3-benzamido-1-butanol → (R)-3-amino-1-butanol (61477-40-5) + benzoic acid (65-85-0)

Conditions	Yield
With hydrogenchloride for 5h; Heating;	A 83% B 37.2 g

1-(tert-butyldimethylsilyloxy)-3-aminobutane (245728-81-8) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With tetrabutyl ammonium fluoride In tetrahydrofuran for 1h;	80%

(R)-3-amino-butyric acid ethyl ester hydrochloride → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
Stage #1: (R)-3-amino-butyric acid ethyl ester hydrochloride With sodium hydrogencarbonate In water at 20℃; for 0.25h; Cooling with ice; Stage #2: With potassium borohydride In ethanol at 20℃; for 12h;	77%

(R)-3-aminobutanoic acid methyl ester hydrochloride (139243-54-2) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
Stage #1: (R)-3-aminobutanoic acid methyl ester hydrochloride With sodium hydrogencarbonate In water for 0.25h; Cooling with ice; Stage #2: With potassium borohydride In methanol at 20℃; for 12h;	76%

(R)-methyl 3-aminobutanoate hydrochloride (6078-06-4, 83509-89-1, 102522-53-2, 103189-63-5) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With RuH(η1-BH4)(dppp)((R,R)-dpen); hydrogen In tetrahydrofuran at 80℃; under 37503.8 Torr; for 16h; Autoclave;	62%
With hydrogen; C40H39BN2P2Ru In tetrahydrofuran at 80℃; under 26252.6 - 37503.8 Torr; for 14h; Product distribution / selectivity;	n/a

(3R)-3-methyl-3-[((1S)-1-phenylethyl)amino]propan-1-ol (60920-20-9) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With hydrogen; palladium on activated charcoal In ethanol

3-aminobutanoic acid ethyl ester (5303-65-1) → (+)-(S)-3-aminopropan-1-ol (61477-39-2) + (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With lithium aluminium tetrahydride Yield given. Yields of byproduct given. Title compound not separated from byproducts;

methyl 3-((methoxycarbonyl)amino)-3-methylpropanoate (116173-78-5, 116173-72-9) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With lithium aluminium tetrahydride; hydrogen bromide 1.) AcOH; 2.) THF; Multistep reaction;

2-hydroxymethyl-N-(3-hydroxy-1-methyl-propyl)-benzamide (866395-51-9) → 2-benzofuran-1(3H)-one (87-41-2) + (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With acetic acid at 80℃;

(3R)-3-{benzyl[(1R)-1-phenylethyl]amino}butanol (899806-42-9) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With hydrogen; palladium hydroxide on carbon In methanol under 1551.49 Torr; for 24h;

tert-butyl (R)-3-amino-3-methyl-propionate (120686-16-0) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With potassium hydroxide; aluminium trichloride In diethyl ether; water

C8H13NO3 → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With potassium hydroxide In ethanol; water at 20 - 85℃; for 2h;

1-Hydroxy-3-butanone (590-90-9) → (R)-3-amino-1-butanol (61477-40-5)

Conditions	Yield
With SEC-BUTYLAMINE; magnesium chloride In aq. phosphate buffer; dimethyl sulfoxide at 15℃; for 24h; Reagent/catalyst; Solvent; Temperature; Enzymatic reaction;	0.45 g
With glucose dehydrogenase; ammonium hydroxide; D-glucose; NAD; ammonium chloride; lysozyme; DNase I In water at 30℃; for 24h; Reagent/catalyst; Enzymatic reaction; enantioselective reaction;	n/a

(R)-3-amino-1-butanol (61477-40-5) + methyl 1-(2,2-dihydroxyethyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylate (1206102-08-0) → (4R,12aS)-7-(benzyloxy)-4-methyl-3,4,12,12a-tetrahydro-2H-pyrido[1′,2’:4,5] pyrazino[2,1-b][1,3]oxazine-6,8-dione (1206102-09-1)

Conditions	Yield
With acetic acid In toluene at 90℃; for 3.5h;	96%
With acetic acid In toluene at 90℃; for 2.5h; Product distribution / selectivity;	83%
With acetic acid In methanol; toluene at 90℃; for 2.5h; Reagent/catalyst; Temperature;	83%
With acetic acid In toluene at 90℃; for 2h; diastereoselective reaction;	80%

di-tert-butyl dicarbonate (24424-99-5) + (R)-3-amino-1-butanol (61477-40-5) → (-)-tert-butyl [(R)-3-hydroxy-1-methylpropyl]carbamate (167216-17-3)

Conditions	Yield
With triethylamine In dichloromethane at 25℃; for 16h;	91.3%
With triethylamine In dichloromethane at 20 - 24℃; for 4h;	80%
With triethylamine In dichloromethane at 20℃; for 4h;
With triethylamine In dichloromethane at 0 - 20℃; for 1h;

(R)-3-amino-1-butanol (61477-40-5) + benzaldehyde (100-52-7) → (R)-3-(benzylamino)butan-1-ol

Conditions	Yield
Stage #1: (R)-3-amino-1-butanol; benzaldehyde In methanol at 20℃; for 1h; Stage #2: With methanol; sodium tetrahydroborate at 0 - 20℃; for 2.33333h;	90%

(R)-3-amino-1-butanol (61477-40-5) + methyl 5-(2,4-difluorobenzylcarbamoyl)-3-methoxy-4-oxo-1-(2-oxoethyl)-1,4-dihydropyridine-2-carboxylate → (4R,12aS)-N-(2,4-difluorobenzyl)-7-methyloxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido [1',2',:4,5]pyrazino[2,1-b] [1,3]oxazine-9-carboxamide (1335210-35-9) + N-(2,4-difluorobenzyl)-7-methoxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide + (R)-N-(2,4-difluorobenzyl)-2-(4-hydroxybutan-2-yl)-9-methoxy-1,8-dioxo-1,8-dihydro-2H-pyrido[1,2-a]pyrazine-7-carboxamide

Conditions	Yield
In toluene; acetonitrile at 100℃; under 5171.62 Torr; Flow reactor;	A n/a B n/a C 88%

(R)-3-amino-1-butanol (61477-40-5) + C18H17NO7 (1246617-67-3) → C21H22N2O6 (1357289-10-1)

Conditions	Yield
With acetic acid In methanol; toluene at 90℃; for 3h;	81%

methyl 3-(benzyloxy)-5-(2,4-difluorobenzylcarbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyridine-2-carboxylate (1229006-25-0) + (R)-3-amino-1-butanol (61477-40-5) → (4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1′,2’:4,5]-pyrazino[2,1-b][1,3]oxazine-9-carboxamide (1206102-11-5)

Conditions	Yield
With acetic acid In dichloromethane at 140℃; Microwave irradiation;	81%
With acetic acid In methanol; toluene at 90℃; for 2h;	65%
With acetic acid In methanol; toluene at 120℃; for 4h;	0.2 g

(R)-3-amino-1-butanol (61477-40-5) + C22H26F2N2O7 → C22H23F2N3O5

Conditions	Yield
Stage #1: C22H26F2N2O7 With methanesulfonic acid; acetic acid In acetonitrile at 25 - 70℃; for 9h; Stage #2: (R)-3-amino-1-butanol In acetonitrile at 65 - 70℃; for 5h;	81%

4-tolyl iodide (624-31-7) + (R)-3-amino-1-butanol (61477-40-5) → (R)-N-(4-hydroxybutan-2-yl)-p-toluidine

Conditions	Yield
With copper(l) iodide; potassium carbonate; L-proline In dimethyl sulfoxide at 120℃; for 12h; Inert atmosphere;	79%

(R)-3-amino-1-butanol (61477-40-5) + C20H21NO7 (1246616-87-4) → (4R,12aS)-3,4,6,8,12,12a-hexahydro-4-methyl-6,8-dioxo-7-(phenylmethoxy)-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid ethyl ester (1357289-04-3)

Conditions	Yield
With acetic acid In methanol; toluene for 3h; Reflux;	78%

(R)-3-amino-1-butanol (61477-40-5) + C20H17N5O3S → C24H26N6O3S

Conditions	Yield
Stage #1: (R)-3-amino-1-butanol; C20H17N5O3S In tetrahydrofuran for 0.166667h; Inert atmosphere; Stage #2: With N-ethyl-N,N-diisopropylamine; HATU In tetrahydrofuran for 2h; Reflux;	76%

(R)-3-amino-1-butanol (61477-40-5) + C19H20F2N2O7 → C23H29F2N3O7

Conditions	Yield
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 20℃; for 2h;	76%

(R)-3-amino-1-butanol (61477-40-5) + tetraethyl 7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3,5,6-tetracarboxylate → C26H42N2O10

Conditions	Yield
In neat (no solvent) at 20℃; Schlenk technique;	74%

(R)-3-amino-1-butanol (61477-40-5) → C4H9N3O

Conditions	Yield
Stage #1: (R)-3-amino-1-butanol With copper(II) sulfate; triethylamine In water; acetonitrile at 0℃; for 0.0833333h; Inert atmosphere; Stage #2: With imidazole-1-sulfonyl azide hydrochloride In water; acetonitrile at 0 - 20℃; for 2.16667h; Inert atmosphere;	74%

(R)-3-amino-1-butanol (61477-40-5) + C20H20F2N2O6 → C22H23F2N3O5

Conditions	Yield
With acetic acid In toluene at 80 - 90℃; for 24h;	71%
With acetic acid In methanol; toluene at 25 - 90℃; for 24h;	61%

Upstream product

• 60920-20-9 (3R)-3-methyl-3-[((1S)-1-phenylethyl)amino]propan-1-ol 
• 5303-65-1 3-aminobutanoic acid ethyl ester 
• 116173-78-5 methyl 3-((methoxycarbonyl)amino)-3-methylpropanoate 
• 245728-81-8 1-(tert-butyldimethylsilyloxy)-3-aminobutane 
• 120686-16-0 tert-butyl (R)-3-amino-3-methyl-propionate 
• 6078-06-4 (R)-methyl 3-aminobutanoate hydrochloride 
• 167216-17-3 (-)-tert-butyl [(R)-3-hydroxy-1-methylpropyl]carbamate 
• 3775-73-3 (R)-3-aminobutanoic acid 
• 866395-21-3 (-)-(3R)-3-((benzyloxycarbonyl)amino)butanol 
• 590-90-9 1-Hydroxy-3-butanone 
• 139243-54-2 (R)-3-aminobutanoic acid methyl ester hydrochloride 
• 146293-15-4 (R)-3-amino-butyric acid ethyl ester hydrochloride 
• 1236049-43-6 (R)-4-hydroxybutan-2-aminium (S)-2-hydroxy-2-phenylacetate 
• 899806-42-9 (3R)-3-{benzyl[(1R)-1-phenylethyl]amino}butanol 

Downstream Products

• 1206102-09-1 (4R,12aS)-7-(benzyloxy)-4-methyl-3,4,12,12a-tetrahydro-2H-pyrido[1′,2’:4,5] pyrazino[2,1-b][1,3]oxazine-6,8-dione 
• 1357289-04-3 (4R,12aS)-3,4,6,8,12,12a-hexahydro-4-methyl-6,8-dioxo-7-(phenylmethoxy)-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid ethyl ester 
• 1357289-10-1 C₂₁H₂₂N₂O₆ 
• 1206102-11-5 (4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1′,2’:4,5]-pyrazino[2,1-b][1,3]oxazine-9-carboxamide 
• 1357289-24-7 C₂₈H₂₉F₂N₃O₆ 
• 1537863-65-2 (R)-3-(phenylmethylsulfonamido)butyl phenylmethanesulfonate 
• 1335210-35-9 (4R,12aS)-N-(2,4-difluorobenzyl)-7-methyloxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido [1',2',:4,5]pyrazino[2,1-b] [1,3]oxazine-9-carboxamide 
• 1335210-34-8 (4R,12aS)-7-methoxy-4-methyl-6,8-dioxo-3,4,6,8, 12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid 
• 245728-73-8 (R)-2-(4-hydroxybutan-2-yl)isoindoline-1,3-dione 
• 1236049-43-6 (R)-4-hydroxybutan-2-aminium (S)-2-hydroxy-2-phenylacetate 

Relevant articles and documents

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Method for preparing (R)-3-aminobutanol

The invention provides a method for preparing (R)-3-aminobutanol, and the method comprises the following steps of: (1) providing 4-hydroxy-2-butanone and carrying out ammoniation reduction on the 4-hydroxy-2-butanone to obtain racemic 3-aminobutanol; (2) reacting (S)-mandelic acid with the racemic 3-aminobutanol to obtain resolved mandelic acid salt; and (3) alkalizing the resolved mandelic acid salt to obtain the product (R)-3-aminobutanol. According to the invention, the process of preparing the (R)-3-aminobutanol through reductive amination and salification resolution is simple and convenient to operate, low in reaction danger and pollution; the purity of the obtained (R)-3-aminobutanol reaches 99.9% (GC method).

Preparation method of 3-aminopropanol or 3-aminopropionic acid derivative

The invention provides a preparation method of an optically active 3-aminopropanol or 3-aminopropionic acid derivative, and belongs to the technical field of organic synthesis. A compound having a structure as shown in a formula II and a formula III is used as a raw material, and the optically active 3-aminopropanol or 3-aminopropionic acid derivative is obtained through four basic steps, namely dehydration condensation, hydrogenation reduction, reduction and hydrolysis. The raw materials adopted in the preparation method are easy to obtain and low in cost; as a chiral phosphine-transitional metal catalyst is used in the hydrogenation reduction reaction, the optically active 3-aminopropanol or 3-aminopropionic acid derivative is efficient, high in selectivity, low in cost and suitable forlarge-scale production. Compared with existing chemical resolution and chiral introduction, the asymmetric hydrogenation synthesis method provided by the invention only produces one chiral product, ishigh in yield, and has relatively high advantages in economy and raw material utilization rate.

Preparation method for R-3-aminobutanol

The invention relates to a preparation method for R-3-aminobutanol. The preparation method specifically comprises the following steps: (a) reacting R-3-aminobutyric acid with di-tert-butyl carbonate in the presence of a polar solvent so as to form N-Boc-(R)-3-aminobutyric acid; (b) reducing N-Boc-(R)-3-aminobutyric acid in the presence of a reducing agent and Lewis acid so as to form N-Boc-(R)-3-aminobutanol; and (c) subjecting N-Boc-(R)-3-aminobutanol to a Boc removal in the presence of an acid solvent so as to form R-3-aminobutanol. The preparation method of the invention is simple in process, low in cost, friendly to environment, easier for industrial production and worth promotion.

Method for preparing 3-amino-1-butanol with single configuration by chiral separation

The invention provides a method for preparing 3-amino-1-butanol with a single configuration by chiral separation. The method comprises the following steps: a 3-amino-1-butanol racemic mixture reacts with L- or D-malic acid to form a corresponding salt, separation purification is performed, so that a malate of optically-pure 3-amino-1-butanol is obtained, and the obtained malate reacts with a base,so that the (R)- or (S)-3-amino-1-butanol with high optical purity is obtained. According to the method provided by the invention, the operation is simple and convenient, the yield is 43.4%, the purity of an enantiomer can be up to 99.9%ee, and the industrialized production of the 3-amino-1-butanol with the single configuration is easy to realize.