isopropylamine
1-[2-(cyclopropyl-methoxy)-ethyl]-4-(2,3-epoxypropoxy)-benzene
betaxolol
Conditions | Yield |
---|---|
for 24h; Ambient temperature; | 90% |
for 48h; Heating; Yield given; | |
In water at 0 - 35℃; |
RS 1-{4-[2-(allyloxy)-ethyl]phenoxy}-3-isopropylamino propan-2-ol
diiodomethane
betaxolol
Conditions | Yield |
---|---|
With diethylzinc In toluene at 0℃; for 16h; | 84% |
betaxolol
Conditions | Yield |
---|---|
With hydrogenchloride In isopropyl alcohol | 74% |
4-[2-(cyclopropylmethoxy)-ethyl]-phenol
betaxolol
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: NaOH / H2O / 12 h / Ambient temperature 2: 48 h / Heating View Scheme |
1-benzyloxy-4-(2-cyclopropylmethoxyethyl)benzene
betaxolol
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 84 percent / H2 / 5percent Pd/C / tetrahydrofuran / 50 - 60 °C / 2585.7 Torr 2: NaOH / H2O / 12 h / Ambient temperature 3: 48 h / Heating View Scheme |
2-(4-benzyloxyphenyl)ethanol
betaxolol
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 1.) NaH / 1.) DMF, 2.) DMF, 60 deg, 18 h 2: 84 percent / H2 / 5percent Pd/C / tetrahydrofuran / 50 - 60 °C / 2585.7 Torr 3: NaOH / H2O / 12 h / Ambient temperature 4: 48 h / Heating View Scheme |
2-<4-(phenylmethoxy)phenyl>acetic acid ethyl ester
betaxolol
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: 86 percent / LiAlH4 / tetrahydrofuran / 3 h / Ambient temperature 2: 1.) NaH / 1.) DMF, 2.) DMF, 60 deg, 18 h 3: 84 percent / H2 / 5percent Pd/C / tetrahydrofuran / 50 - 60 °C / 2585.7 Torr 4: NaOH / H2O / 12 h / Ambient temperature 5: 48 h / Heating View Scheme |
betaxolol Hydrochloride
betaxolol
Conditions | Yield |
---|---|
With Dowex Marathon 11 chloride form In water |
betaxolol
acetic anhydride
1-(N-acetyl-N-isopropyl)amino-3-<4-(2-cyclopropylmethoxy)ethyl>phenoxyprop-2-yl acetate
Conditions | Yield |
---|---|
With pyridine for 24h; Ambient temperature; | 100% |
With pyridine; triethylamine at 20℃; |
betaxolol
acetic anhydride
B
Acetic acid (S)-2-(acetyl-isopropyl-amino)-1-[4-(2-cyclopropylmethoxy-ethyl)-phenoxymethyl]-ethyl ester
Conditions | Yield |
---|---|
With pyridine for 24h; Ambient temperature; Yield given. Yields of byproduct given; |
betaxolol
cyclopropanecarboxylic acid chloride
Conditions | Yield |
---|---|
Acylation; |
betaxolol
betaxolol Hydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride In acetone at 10 - 15℃; pH=2.0; |
betaxolol
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: pyridine; triethylamine / 20 °C 2: Rhodotorula mucilaginosa DQ832198 / 12 h / 28 °C / pH 6 / Microbiological reaction; phosphate-citric acid buffer 3: sodium hydroxide / methanol / 20 °C 4: hydrogenchloride / water / 20 °C View Scheme |
betaxolol
(-)-Betaxolol
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: pyridine; triethylamine / 20 °C 2: Rhodotorula mucilaginosa DQ832198 / 12 h / 28 °C / pH 6 / Microbiological reaction; phosphate-citric acid buffer 3: sodium hydroxide / methanol / 20 °C View Scheme |
betaxolol
Acetic acid (S)-2-(acetyl-isopropyl-amino)-1-[4-(2-cyclopropylmethoxy-ethyl)-phenoxymethyl]-ethyl ester
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: pyridine; triethylamine / 20 °C 2: Rhodotorula mucilaginosa DQ832198 / 12 h / 28 °C / pH 6 / Microbiological reaction; phosphate-citric acid buffer View Scheme |
Conditions | Yield |
---|---|
With diethylamine In acetonitrile Reagent/catalyst; Resolution of racemate; |
Molecular Formula: C18H29NO3
Molar mass: 307.43 g/mol
Density: 1.067 g/cm3
Flash Point: 224.7 °C
Index of Refraction: 1.529
Boiling Point: 448 °C at 760 mmHg
Vapour Pressure: 8.26E-09 mmHg at 25°C
Melting point: 61-63°C
Appearance: White crystalline solid
Product categories of Betaxolol (63659-18-7): Pharmaceuticals;Intermediates & Fine Chemicals;Steroids
Structure of Betaxolol (63659-18-7):
Systematic Name: 1-[4-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)propan-2-ol
SMILES: O(CCc1ccc(OCC(O)CNC(C)C)cc1)CC2CC2
InChI: InChI=1/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3
InChIKey: NWIUTZDMDHAVTP-UHFFFAOYAU
Std. InChI: InChI=1S/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3
Std. InChIKey: NWIUTZDMDHAVTP-UHFFFAOYSA-N
Betaxolol (63659-18-7) was approved Drug Administration (FDA) by and the U.S. Food for ocular use as a 0.5% solution (Betoptic) in 1985 and as a 0.25% solution (Betoptic S) in 1989.
Betaxolol (63659-18-7) is a selective beta1 receptor blocker used in the treatment of hypertension and glaucoma. And it can be used for the management of hypertension and for the management of glaucoma .
Organism | Test Type | Route | Reported Dose (Normalized Dose) | Effect | Source |
---|---|---|---|---|---|
dog | LD50 | oral | 60mg/kg (60mg/kg) | Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 18(Suppl, |
Betaxolol (63659-18-7) also can be called Betoptic , Betoptic S , Lokren ,and Kerlone .It typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta2 receptors) as timolol may.In addition to its effect on the heart, betaxolol reduces the pressure within the eye (intraocular pressure). This effect is thought to be caused by reducing the production of the liquid (which is called the aqueous humor) within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with elevated intraocular pressure due to glaucoma.It also shows greater affininty for beta1 receptors than metoprolol.
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