1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride
- Product Name
- 1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride
- CAS No.
- 256499-19-1
- Chemical Name
- 1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride
- Synonyms
- 1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide hydrochloride;1-(2-Fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboxaMidine hydrochloride;Riociguat-10;Riociguat Impurity 3 HCl;Riociguat Impurity 2 HCl;Riociguat EP Impurity 10;Riociguanidine Intermediate;1-(2-Fluoro-benzyl)-1H-py...;1-(2-fluorobenzyl)-1H-pyrazolo;1-(2-Fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboxamidine
- CBNumber
- CB52525708
- Molecular Formula
- C14H13ClFN5
- Formula Weight
- 305.74
- MOL File
- 256499-19-1.mol
1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride Property
- Melting point:
- 247-249oC
- storage temp.
- Inert atmosphere,Room Temperature
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- Solid
- color
- White
- InChI
- InChI=1S/C14H12FN5.ClH/c15-11-6-2-1-4-9(11)8-20-14-10(5-3-7-18-14)12(19-20)13(16)17;/h1-7H,8H2,(H3,16,17);1H
- InChIKey
- DQASIYVADJWVLY-UHFFFAOYSA-N
- SMILES
- C(C1C=CC=CC=1F)N1N=C(C(N)=N)C2C=CC=NC1=2.Cl
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- F588235
- Product name
- 1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamideHydrochloride
- Packaging
- 250mg
- Price
- $50
- Updated
- 2021/12/16
- Product number
- F588235
- Product name
- 1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamideHydrochloride
- Packaging
- 5g
- Price
- $250
- Updated
- 2021/12/16
- Product number
- 068862
- Product name
- 1-(2-Fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboxamidine hydrochloride
- Purity
- >95%
- Packaging
- 5g
- Price
- $270
- Updated
- 2021/12/16
- Product number
- Y8461
- Product name
- 1-(2-Fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboxamidinehydrochloride
- Packaging
- 5g
- Price
- $311
- Updated
- 2021/12/16
- Product number
- 068862
- Product name
- 1-(2-Fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboxamidine hydrochloride
- Purity
- >95%
- Packaging
- 25g
- Price
- $710
- Updated
- 2021/12/16
1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride Chemical Properties,Usage,Production
Uses
1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride is a key intermediate in the synthesis of Riociguat, a potent, oral stimulator of soluble guanylate cyclase for the treatment of pulmonary hypertension.
Synthesis
In a 10 L four-necked flask, 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carbonitrile 919.7 g (3.646 mol, 10 eq), MeOH 7 L was added, and MeONa 295 g (5.469 mol, 1.5 eq) was added with stirring, and stirred at room temperature for 2 h. Has disappeared, completely converted to the intermediate (7), added CH 3 C0 2 H 329 g (5.469 mol, 1.5 eq), NH 4 C1 293 g (5.469 mol, 1.5 eq), heated to reflux overnight, TLC monitoring reaction completely The temperature was lowered, a large amount of solid was precipitated, filtered, and washed with DCM to give 981 g of white solid as 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide (8), which was used directly in the next step. The compound 8 981.0 g (3.646 mol, lO eq) was added to 5 L of methyl tert-butyl ether, stirred, suspended as a suspension, passed through HC1 gas for about 2.5 h, filtered, washed with DCM, and dried by filtration. 1103.7 g of white solid 1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride. Total yield in two steps: 99.0%. Purity: 99%.
1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride Suppliers
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View Lastest Price from 1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide Hydrochloride manufacturers
- Product
- 1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide hydrochloride 256499-19-1
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- 98.0%
- Supply Ability
- 10kg/month
- Release date
- 2021-12-17
- Product
- 1H-Pyrazolo[3,4-b]pyridine-3-carboximidamide, 1-[(2-fluorophenyl)methyl]-, hydrochloride (1:1) 256499-19-1
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- 98%
- Supply Ability
- 100kgs
- Release date
- 2024-12-20
- Product
- Riociguanidine Intermediate 256499-19-1
- Price
- US $30.00-28.00/Kg
- Min. Order
- 1Kg
- Purity
- 99.0% up
- Supply Ability
- 50 tons per month
- Release date
- 2022-09-16