Welcome to LookChem.com Sign In|Join Free

CAS

  • or

223673-61-8

Post Buying Request

223673-61-8 Suppliers

Recommended suppliersmore

  • Product
  • FOB Price
  • Min.Order
  • Supply Ability
  • Supplier
  • Contact Supplier

223673-61-8 Usage

Description

Betanis (Mirabegron) was approved in July 2011 by the Japanese Ministry of Health, Labour, and Welfare for the treatment of urgency, urinary frequency, and urinary urge urinary incontinence associated with overactive bladder (OAB). Mirabegron is synthesized by coupling 4-nitrophenethyl amine to (R)-2-hydroxy-2-phenylacetic acid. The resulting amide is reduced to an amine. The nitro group is then reduced and the resulting aniline is coupled to 2-(2-aminothiazol-4-yl) acetic acid to give mirabegron. Mirabegron has an EC50 of 22 nM (intrinsic activity=0.8) for β3-AR with no detectable activity for β1- andβ2-AR (EC50>10,000 nM). In an anesthetized rat rhythmic bladder contraction model in which bladder contractions are induced by saline, mirabegron at 3 mg/kg iv decreased the frequency of rhythmic bladder contraction without suppressing contraction amplitude. These data suggest that the activation of β3-AR increases bladder capacity without influencing the frequency of bladder contraction.

Chemical Properties

White to Off-White Solid

Originator

Astellas Pharma Inc. (Japan)

Uses

Different sources of media describe the Uses of 223673-61-8 differently. You can refer to the following data:
1. Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
2. A potent bladder relaxant compound
3. Potent bladder relaxant and reagent for diabetes remedy.;Labeled Mirabegron, intended for use as an internal standard for the quantification of Mirabegron by GC- or LC-mass spectrometry.

Definition

ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-amino-1,3-thiazol-4-ylacetic acid with the anilino group of (1R)-2-{[2-(4-aminophenyl)ethyl]amino}-1-phenylethanol. Used for the treatment of overactive ladder syndrome.

Brand name

Betanis

Clinical Use

Mirabegron is an orally active β3-adrenoceptor agonist currently in development by Astellas Pharma for the treatment of overactive bladder (OAB). The drug is a nanomolar EC50 antagonist against human β3-AR biochemical assays with good selectivity over b1- and β2-ARs. Mirabegron demonstrates a novel mechanism by targeting the β3-AR for bladder relaxation to help manage OAB symptoms such as increased urinary urgency and frequency and urgency incontinence. However, mirabegron is a cytochrome P450 2D6 inhibitor, and it raises a concern for drug–drug interaction with concomitant administration of other cytochrome P450 2D6 substrates.

Synthesis

The synthesis of mirabegron began with a condensation reaction between (R)-styrene oxide (182) and 4-nitrophenylethylamine (183) in refluxing isopropanol to yield corresponding aminoalcohol 184 in 22% yield. Aminoalcohol 184 was protected as its N-Boc derivative with t-butyl dicarbonate in THF in 96% yield, and this was followed by nitro group hydrogenative reduction with 10% Pd/C to give free amine 185 in 96% yield. Aniline 185 was coupled with 2-amino-4-thiazolyl acetic acid 186 in the presence of EDCI and HOBt to give amide 187 in 85% yield. Removal of the Boc group was affected with 4 N HCl solution in a 2:1 volume ratio in ethyl acetate to obtain mirabegron HCl in 52% yield. The HCl salt was neutralized with 1 N NaOH to deliver mirabegron (XVII).

Drug interactions

Potentially hazardous interactions with other drugs None known

Metabolism

Metabolised via multiple pathways involving dealkylation, oxidation, (direct) glucuronidation, and amide hydrolysis. Renal elimination of mirabegron is primarily through active tubular secretion along with glomerular filtration.

Check Digit Verification of cas no

The CAS Registry Mumber 223673-61-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,2,3,6,7 and 3 respectively; the second part has 2 digits, 6 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 223673-61:
(8*2)+(7*2)+(6*3)+(5*6)+(4*7)+(3*3)+(2*6)+(1*1)=128
128 % 10 = 8
So 223673-61-8 is a valid CAS Registry Number.
InChI:InChI=1/C21H24N4O2S/c22-21-25-18(14-28-21)12-20(27)24-17-8-6-15(7-9-17)10-11-23-13-19(26)16-4-2-1-3-5-16/h1-9,14,19,23,26H,10-13H2,(H2,22,25)(H,24,27)

223673-61-8SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name mirabegron

1.2 Other means of identification

Product number -
Other names 2-(2-amino-1,3-thiazol-4-yl)-N-(4-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}phenyl)acetamide

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:223673-61-8 SDS

223673-61-8Synthetic route

2-(2-amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide acetate salt

2-(2-amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide acetate salt

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With water In water at 80℃; for 24h; Reagent/catalyst; Temperature;100%
2-amino-4-thiazoleacetic acid
29676-71-9

2-amino-4-thiazoleacetic acid

YM-208876
391901-45-4

YM-208876

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Stage #1: 2-amino-4-thiazoleacetic acid; YM-208876 In water at 20℃; for 0.0833333h;
Stage #2: With hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In water at 20℃; for 1h; Reagent/catalyst; Temperature;
92.6%
With hydrogenchloride; 1,2-dichloro-ethane In water at 30℃; for 5h;88.31%
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In d7-N,N-dimethylformamide at 25℃; for 13h; Reagent/catalyst;84%
With hydrogenchloride; dmap In water at 20℃; for 6h;79%
Stage #1: 2-amino-4-thiazoleacetic acid; YM-208876 With hydrogenchloride In water at 25 - 30℃; for 0.25h;
Stage #2: With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride at 25 - 30℃;
Stage #3: With sodium hydroxide In water at 0 - 5℃; pH=9;
144 g
2-amino-4-thiazoleacetic acid
29676-71-9

2-amino-4-thiazoleacetic acid

(1R)-2-{[2-(4-aminophenyl)ethyl]amino}-1-phenylethan-1-ol hydrochloride

(1R)-2-{[2-(4-aminophenyl)ethyl]amino}-1-phenylethan-1-ol hydrochloride

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In water at 15 - 20℃; for 1h; pH=1.8 - 2;92%
With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In water at 20 - 25℃; for 4h; Concentration;82%
With hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In water for 1h;
C26H32N4O4S

C26H32N4O4S

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With hydrogenchloride In 1,4-dioxane; water at 20℃; for 10h;90.3%
2-amino-4-thiazoleacetic acid
29676-71-9

2-amino-4-thiazoleacetic acid

(R)-2-[ [2-(4-aminophenyl)ethyl]-amino]-1-phenylethanol monohydrochloride
521284-22-0

(R)-2-[ [2-(4-aminophenyl)ethyl]-amino]-1-phenylethanol monohydrochloride

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In water at 28℃; for 3h; Concentration;84.5%
Stage #1: 2-amino-4-thiazoleacetic acid; (R)-2-[ [2-(4-aminophenyl)ethyl]-amino]-1-phenylethanol monohydrochloride With hydrogenchloride In water at 25 - 30℃;
Stage #2: With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In water at 25 - 30℃; for 2h;
84%
Stage #1: 2-amino-4-thiazoleacetic acid; (R)-2-[ [2-(4-aminophenyl)ethyl]-amino]-1-phenylethanol monohydrochloride With hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In water at 15 - 20℃; for 1h;
Stage #2: With sodium hydroxide In water
(R)-2-(2-(1,3-dioxoindolin-2-yl)thiazol-4-yl)-N-(4-(2-((2-hydroxy-2-phenylethyl)amino)ethyl)phenyl)acetamide

(R)-2-(2-(1,3-dioxoindolin-2-yl)thiazol-4-yl)-N-(4-(2-((2-hydroxy-2-phenylethyl)amino)ethyl)phenyl)acetamide

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With hydrazine hydrate In ethanol for 3h; Reflux;84%
With hydrazine hydrate In ethanol for 3h; Reflux;84%
2-amino-4-thiazoleacetic acid
29676-71-9

2-amino-4-thiazoleacetic acid

(R)-N-(4-aminophenethyl)-2-hydroxy-2-phenylacetamide hydrochloride

(R)-N-(4-aminophenethyl)-2-hydroxy-2-phenylacetamide hydrochloride

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In water at 20℃; for 1h;75.7%
(2-amino-1,3-thiazol-4-yl)acetyl chloride

(2-amino-1,3-thiazol-4-yl)acetyl chloride

YM-208876
391901-45-4

YM-208876

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With potassium carbonate In acetone at 10 - 15℃;70%
C22H24N4O3S

C22H24N4O3S

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With sodium hydroxide at 55 - 60℃; for 3h;70%
(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide monotartrate

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide monotartrate

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With sodium hydroxide In 2-methyltetrahydrofuran; water pH=9;63%
(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide hydrobromide

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide hydrobromide

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With sodium hydroxide In 2-methyltetrahydrofuran; water pH=9;63%
(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide oxalate

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide oxalate

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With sodium hydroxide In 2-methyltetrahydrofuran; water pH=9;52%
2-(2-aminothiazol-4-yl)acetic acid hydrochloride

2-(2-aminothiazol-4-yl)acetic acid hydrochloride

YM-208876
391901-45-4

YM-208876

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Stage #1: 2-(2-aminothiazol-4-yl)acetic acid hydrochloride; YM-208876 With hydrogenchloride In water at 25 - 30℃; for 0.25h;
Stage #2: With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride at 25 - 30℃;
Stage #3: With sodium hydroxide In water at 0 - 5℃; pH=9;
43 g
(R)-2-(2-aminothiazole-4-yl)-4’-[2-[(2-hydroxy-2-phenyl)ethylamino]ethyl]acetanilide monohydrochloride

(R)-2-(2-aminothiazole-4-yl)-4’-[2-[(2-hydroxy-2-phenyl)ethylamino]ethyl]acetanilide monohydrochloride

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With sodium hydroxide In water at 25 - 30℃;43 mg
4-tert-butoxycarbonylaminophenylacetonitrile
1233249-35-8

4-tert-butoxycarbonylaminophenylacetonitrile

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: hydrogen; ammonia / water; methanol / 4 h / 25 - 30 °C / 2585.81 - 3102.97 Torr
2.1: dicyclohexyl-carbodiimide; benzotriazol-1-ol / 2-methyltetrahydrofuran / 2 h / 25 - 30 °C
3.1: hydrogenchloride / water; ethyl acetate / 4 h / 20 °C
4.1: sodium hydroxide / water / 10 - 15 °C / pH 9 - 10
4.2: 4 h / 5 - 65 °C / Inert atmosphere
4.3: 0.5 h / 5 - 10 °C
5.1: hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / water / 1 h / 15 - 20 °C / pH 1.8 - 2
View Scheme
4-(2-aminoethyl)-N-(tert-butoxycarbonyl)phenylamine
457631-44-6

4-(2-aminoethyl)-N-(tert-butoxycarbonyl)phenylamine

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: dicyclohexyl-carbodiimide; benzotriazol-1-ol / 2-methyltetrahydrofuran / 2 h / 25 - 30 °C
2.1: hydrogenchloride / water; ethyl acetate / 4 h / 20 °C
3.1: sodium hydroxide / water / 10 - 15 °C / pH 9 - 10
3.2: 4 h / 5 - 65 °C / Inert atmosphere
3.3: 0.5 h / 5 - 10 °C
4.1: hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / water / 1 h / 15 - 20 °C / pH 1.8 - 2
View Scheme
(R)-N-(4-N-Boc-aminophenethyl)-2-hydroxy-2-phenylacetamide

(R)-N-(4-N-Boc-aminophenethyl)-2-hydroxy-2-phenylacetamide

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: hydrogenchloride / water; ethyl acetate / 4 h / 20 °C
2.1: sodium hydroxide / water / 10 - 15 °C / pH 9 - 10
2.2: 4 h / 5 - 65 °C / Inert atmosphere
2.3: 0.5 h / 5 - 10 °C
3.1: hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / water / 1 h / 15 - 20 °C / pH 1.8 - 2
View Scheme
4-Nitrophenylacetonitrile
555-21-5

4-Nitrophenylacetonitrile

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1.1: hydrogen; palladium 10% on activated carbon / ethyl acetate / 20 - 25 °C / 2585.81 - 3102.97 Torr
2.1: ethyl acetate / 25 - 30 °C
3.1: hydrogen; ammonia / water; methanol / 4 h / 25 - 30 °C / 2585.81 - 3102.97 Torr
4.1: dicyclohexyl-carbodiimide; benzotriazol-1-ol / 2-methyltetrahydrofuran / 2 h / 25 - 30 °C
5.1: hydrogenchloride / water; ethyl acetate / 4 h / 20 °C
6.1: sodium hydroxide / water / 10 - 15 °C / pH 9 - 10
6.2: 4 h / 5 - 65 °C / Inert atmosphere
6.3: 0.5 h / 5 - 10 °C
7.1: hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / water / 1 h / 15 - 20 °C / pH 1.8 - 2
View Scheme
Multi-step reaction with 4 steps
1: hydrazine; palladium 10% on activated carbon / ethanol / 2 h / 25 °C / Inert atmosphere
2: hydrazine / 5 h / 25 - 60 °C / Inert atmosphere
3: acetonitrile / 10 h / 70 °C
4: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / d7-N,N-dimethylformamide / 13 h / 25 °C
View Scheme
Multi-step reaction with 4 steps
1.1: diisobutylaluminium hydride / toluene / 2 h / 0 - 10 °C / Inert atmosphere
2.1: triethylamine / methanol / 2 h / 20 °C / Inert atmosphere
2.2: 1 h / 0 °C / Inert atmosphere
3.1: ammonium formate; palladium on activated charcoal / methanol / 6 h / 50 °C
4.1: hydrogenchloride; dmap / water / 6 h / 20 °C
View Scheme
phenylacetonitrile
140-29-4

phenylacetonitrile

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 8 steps
1.1: nitric acid; phosphoric acid / water / 2 h / 0 - 25 °C
2.1: hydrogen; palladium 10% on activated carbon / ethyl acetate / 20 - 25 °C / 2585.81 - 3102.97 Torr
3.1: ethyl acetate / 25 - 30 °C
4.1: hydrogen; ammonia / water; methanol / 4 h / 25 - 30 °C / 2585.81 - 3102.97 Torr
5.1: dicyclohexyl-carbodiimide; benzotriazol-1-ol / 2-methyltetrahydrofuran / 2 h / 25 - 30 °C
6.1: hydrogenchloride / water; ethyl acetate / 4 h / 20 °C
7.1: sodium hydroxide / water / 10 - 15 °C / pH 9 - 10
7.2: 4 h / 5 - 65 °C / Inert atmosphere
7.3: 0.5 h / 5 - 10 °C
8.1: hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / water / 1 h / 15 - 20 °C / pH 1.8 - 2
View Scheme
p-aminophenylacetonitrile
3544-25-0

p-aminophenylacetonitrile

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: ethyl acetate / 25 - 30 °C
2.1: hydrogen; ammonia / water; methanol / 4 h / 25 - 30 °C / 2585.81 - 3102.97 Torr
3.1: dicyclohexyl-carbodiimide; benzotriazol-1-ol / 2-methyltetrahydrofuran / 2 h / 25 - 30 °C
4.1: hydrogenchloride / water; ethyl acetate / 4 h / 20 °C
5.1: sodium hydroxide / water / 10 - 15 °C / pH 9 - 10
5.2: 4 h / 5 - 65 °C / Inert atmosphere
5.3: 0.5 h / 5 - 10 °C
6.1: hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / water / 1 h / 15 - 20 °C / pH 1.8 - 2
View Scheme
Multi-step reaction with 3 steps
1: hydrazine / 5 h / 25 - 60 °C / Inert atmosphere
2: acetonitrile / 10 h / 70 °C
3: N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / d7-N,N-dimethylformamide / 13 h / 25 °C
View Scheme
[2-(formylamino)-1,3-thiazol-4-yl]acetyl chloride
782441-52-5

[2-(formylamino)-1,3-thiazol-4-yl]acetyl chloride

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: potassium carbonate / acetonitrile / 10 - 15 °C
2: sodium hydroxide / 3 h / 55 - 60 °C
View Scheme
Multi-step reaction with 3 steps
1: potassium carbonate / dichloromethane / 10 - 15 °C
2: potassium carbonate / dichloromethane / 1 h / 25 - 30 °C
3: sodium hydroxide / 3 h / 55 - 60 °C
View Scheme
[2-(formylamino)-1,3-thiazol-4-yl]acetic acid

[2-(formylamino)-1,3-thiazol-4-yl]acetic acid

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: phosphorus pentachloride / dichloromethane / -10 °C
2: potassium carbonate / acetonitrile / 10 - 15 °C
3: sodium hydroxide / 3 h / 55 - 60 °C
View Scheme
Multi-step reaction with 4 steps
1: phosphorus pentachloride / dichloromethane / -10 °C
2: potassium carbonate / dichloromethane / 10 - 15 °C
3: potassium carbonate / dichloromethane / 1 h / 25 - 30 °C
4: sodium hydroxide / 3 h / 55 - 60 °C
View Scheme
[2-(formylamino)-1,3-thiazol-4-yl]acetic acid

[2-(formylamino)-1,3-thiazol-4-yl]acetic acid

YM-208876
391901-45-4

YM-208876

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; hydrogenchloride / water / 0.5 h / 25 - 30 °C
2: sodium hydroxide / 3 h / 55 - 60 °C
View Scheme
(2-amino-1,3-thiazol-4-yl)acetyl chloride

(2-amino-1,3-thiazol-4-yl)acetyl chloride

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: potassium carbonate / dichloromethane / 10 - 15 °C
2: potassium carbonate / dichloromethane / 1 h / 25 - 30 °C
View Scheme
2-amino-4-thiazoleacetic acid
29676-71-9

2-amino-4-thiazoleacetic acid

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: oxalyl dichloride; N,N-dimethyl-formamide / dichloromethane / 0 - 5 °C
2: potassium carbonate / acetone / 10 - 15 °C
View Scheme
Multi-step reaction with 3 steps
1: oxalyl dichloride; N,N-dimethyl-formamide / dichloromethane / 0 - 5 °C
2: potassium carbonate / dichloromethane / 10 - 15 °C
3: potassium carbonate / dichloromethane / 1 h / 25 - 30 °C
View Scheme
Multi-step reaction with 2 steps
1.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / water / 3 h / 20 - 25 °C
1.2: 1 h / 20 - 25 °C
2.1: sodium hydroxide / water; 2-methyltetrahydrofuran / pH 9
View Scheme
4-nitrophenyl-[2-(formylamino)-1,3-thiazol-4-yl]acetate

4-nitrophenyl-[2-(formylamino)-1,3-thiazol-4-yl]acetate

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: potassium carbonate / dichloromethane / 1 h / 25 - 30 °C
2: sodium hydroxide / 3 h / 55 - 60 °C
View Scheme
4-nitrophenyl-(2-amino-1,3-thiazol-4-yl)acetate

4-nitrophenyl-(2-amino-1,3-thiazol-4-yl)acetate

YM-208876
391901-45-4

YM-208876

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
With potassium carbonate In dichloromethane at 25 - 30℃; for 1h;1 g
(R)-Mandelic Acid
611-71-2

(R)-Mandelic Acid

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: triethylamine; benzotriazol-1-ol; 1,2-dichloro-ethane / N,N-dimethyl-formamide / 6 h / 30 °C
2: 1,3-dimethyl-2-imidazolidinone; borane-THF / tetrahydrofuran / 4 h / 70 °C
3: ammonium formate; palladium 10% on activated carbon / methanol / 5 h / 65 °C / Reflux
4: hydrogenchloride; 1,2-dichloro-ethane / water / 5 h / 30 °C
View Scheme
(2R)-2-hydroxy-N-[2-(4-nitrophenyl)ethyl]-2-phenylethanamide
521284-19-5

(2R)-2-hydroxy-N-[2-(4-nitrophenyl)ethyl]-2-phenylethanamide

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: 1,3-dimethyl-2-imidazolidinone; borane-THF / tetrahydrofuran / 4 h / 70 °C
2: ammonium formate; palladium 10% on activated carbon / methanol / 5 h / 65 °C / Reflux
3: hydrogenchloride; 1,2-dichloro-ethane / water / 5 h / 30 °C
View Scheme
Multi-step reaction with 3 steps
1: hydrogen; palladium 10% on activated carbon / methanol / 4 h / 20 - 25 °C
2: aluminum (III) chloride; lithium aluminium tetrahydride / tetrahydrofuran / 5 h / Reflux
3: hydrogenchloride; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / water / 1 h / 20 °C
View Scheme
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

(R)-2-(2-aminothiazole-4-yl)-4’-[2-[(2-hydroxy-2-phenyl)ethylamino]ethyl]acetanilide monohydrochloride

(R)-2-(2-aminothiazole-4-yl)-4’-[2-[(2-hydroxy-2-phenyl)ethylamino]ethyl]acetanilide monohydrochloride

Conditions
ConditionsYield
With hydrogenchloride In isopropyl alcohol at 75℃; for 0.25h;99%
With hydrogenchloride In methanol; isopropyl alcohol at 20 - 25℃; for 3h;70 g
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

citric acid
77-92-9

citric acid

mirabegron citrate

mirabegron citrate

Conditions
ConditionsYield
In methanol at 20℃; for 2h;94.6%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

p-Coumaric Acid
7400-08-0

p-Coumaric Acid

mirabegron coumarate

mirabegron coumarate

Conditions
ConditionsYield
In methanol at 20℃; for 2h;94.4%
Hippuric Acid
495-69-2

Hippuric Acid

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

mirabegron hippurate

mirabegron hippurate

Conditions
ConditionsYield
In methanol at 20℃; for 2h;93.2%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

(2E)-but-2-enedioic acid
110-17-8

(2E)-but-2-enedioic acid

mirabegron fumarate

mirabegron fumarate

Conditions
ConditionsYield
In methanol at 20℃; for 2h;93%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

(2E)-but-2-enedioic acid
110-17-8

(2E)-but-2-enedioic acid

C21H24N4O2S*C4H4O4

C21H24N4O2S*C4H4O4

Conditions
ConditionsYield
In methanol at 15 - 40℃; for 7.83333h;90%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

n-tetradecanoic acid
544-63-8

n-tetradecanoic acid

mirabegron myristate

mirabegron myristate

Conditions
ConditionsYield
In methanol at 20℃; for 2h;89.2%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

oxalic acid
144-62-7

oxalic acid

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide oxalate

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide oxalate

Conditions
ConditionsYield
In 2-methyltetrahydrofuran at 20 - 25℃; for 1h;88%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

citric acid
77-92-9

citric acid

C21H24N4O2S*C6H8O7

C21H24N4O2S*C6H8O7

Conditions
ConditionsYield
In methanol at 15 - 40℃; for 7.83333h;88%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

L-Pyroglutamic acid
98-79-3

L-Pyroglutamic acid

2-(2-amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide L-pyroglutamic acid

2-(2-amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide L-pyroglutamic acid

Conditions
ConditionsYield
In methanol at 15 - 40℃; for 7.83333h;86%
In methanol; acetone at 20℃; for 1h;4.2 g
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

mirabegron phosphate

mirabegron phosphate

Conditions
ConditionsYield
With phosphoric acid In methanol at 20℃; for 2h;83.9%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

benzoic acid
65-85-0

benzoic acid

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide benzoate

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide benzoate

Conditions
ConditionsYield
In 2-methyltetrahydrofuran at 20 - 25℃; for 1h;83%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

tartaric acid
87-69-4

tartaric acid

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide monotartrate

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide monotartrate

Conditions
ConditionsYield
In 2-methyltetrahydrofuran at 20 - 25℃; for 1h;83%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

(R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenyl)ethylamino]ethyl}acetamide magnesium chloride

(R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenyl)ethylamino]ethyl}acetamide magnesium chloride

Conditions
ConditionsYield
With magnesium(II) chloride hexahydrate In butan-1-ol at 85℃; for 0.25h; Solvent;79.5%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

orotic acid
65-86-1

orotic acid

mirabegron orotate

mirabegron orotate

Conditions
ConditionsYield
In methanol at 20℃; for 2h;79.2%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

succinic acid
110-15-6

succinic acid

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide monosuccinate

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide monosuccinate

Conditions
ConditionsYield
In 2-methyltetrahydrofuran at 20 - 25℃; for 1h;79%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

toluene-4-sulfonic acid
104-15-4

toluene-4-sulfonic acid

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide p-toluenesulfonate

(R)-2-(2-aminothiazol-4-yl)-4’-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide p-toluenesulfonate

Conditions
ConditionsYield
In 2-methyltetrahydrofuran at 20 - 40℃; for 1.5h;70%
(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide
223673-61-8

(R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide

(R)-2-(4-(2-(2-aminothiazol-4-yl)ethylamino)phenethylamino)-1-phenylethanol
1376616-22-6

(R)-2-(4-(2-(2-aminothiazol-4-yl)ethylamino)phenethylamino)-1-phenylethanol

Conditions
ConditionsYield
Stage #1: (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide With borane-THF In tetrahydrofuran at 0 - 50℃; for 2h;
Stage #2: With hydrogenchloride In tetrahydrofuran; water
Stage #3: With sodium hydroxide In tetrahydrofuran; water pH=10;
9%
Stage #1: (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide With borane-THF In tetrahydrofuran at 0 - 50℃; for 2h;
Stage #2: With sodium carbonate In water
9%

223673-61-8Relevant articles and documents

Preparation method of mirabegron key intermediate

-

, (2022/01/12)

The invention provides a preparation method of a mirabegron key intermediate, namely, a compound as shown in a formula (III). The method is simple, convenient and safe to operate, free of harsh reaction conditions, high in reaction purity and yield and low in process cost which is about 40% of that of a process using a metal catalyst such as palladium carbon, is suitable for large-scale production and conforms to the green chemistry principle. A finished product of mirabegron continues to be prepared by using the intermediate compound as shown in the formula (III) prepared by the method so as to meet the existing requirements.

Preparation method of mirabegron (by machine translation)

-

, (2020/08/02)

The method is convenient to operate, controllable in reaction process, high in 2 - final product purity,4 - high in yield and suitable for industrial production, so that a more valuable synthesis route is provided for preparing mirabead, good social benefits and economic benefits can be brought, and the economic value potential is great. (by machine translation)

Preparation method of mirabegron

-

, (2019/04/30)

The invention discloses a preparation method of mirabegron, and the method comprises: S1, carrying out reduction reaction on p-nitrophenylacetonitrile to obtain p-nitrophenylacetaldehyde; S2, carryingout condensation reduction on the p-nitrophenylacetaldehyde and (R) 2-amino-1-phenethyl alcohol to obtain (R) 2-(4-nitrophenethyl) amino)-1-phenyl ethyl alcohol; S3, carrying out reduction on the (R)2-amino-1-phenethyl alcohol to obtain (R) 2-(4-nitrophenethyl) amino)-1-phenyl ethyl alcohol to obtain an intermediate (R) 2-((4-aminophenyl ethyl) amino)-1-phenyl ethyl alcohol; and S4, carrying outcondensation on the (R) 2-((4-aminophenyl ethyl) amino)-1-phenyl ethyl alcohol and aminothiazole acetic acid to obtain the mirabegron. According to the method, the starting raw materials are cheap and easy to obtain, the reaction conditions are controllable, the synthetic route steps are few, the yield is high, the cost is low, and the prepared mirabegron is high in purity.

Post a RFQ

Enter 15 to 2000 letters.Word count: 0 letters

Attach files(File Format: Jpeg, Jpg, Gif, Png, PDF, PPT, Zip, Rar,Word or Excel Maximum File Size: 3MB)

1

What can I do for you?
Get Best Price

Get Best Price for 223673-61-8