1702271-98-4

Usage

Uses

Used in Pharmaceutical Industry:
2-1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl-5-N-methylpyrimidine-4,5,6-triamine is used as an impurity in Riociguat (R520000) for the treatment of pulmonary hypertension. It is important to monitor and control the presence of this impurity to ensure the safety and efficacy of the medication.

Upstream product

• 77-78-1 dimethyl sulfate 
• 428854-24-4 2-(1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidine-4,5,6- triamine 
• 370879-49-5 2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-[(E)-phenyldiazen-1-yl]pyrimidine-4,6-diamine 
• 64-18-6 formic acid 
• 428854-23-3 C₂₃H₁₈FN₉ 
• 256376-68-8 please input 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-formamidine 
• 74-89-5 methylamine 

Relevant academic research and scientific papers

PROCESS FOR THE PREPARATION OF METHYL 4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL]-5-PYRIMIDINYL(METHYL)CARBAMATE AND ITS POLYMORPHS THEREOF

The present invention relates to an improved process for the preparation of methyl 4,6-diamino-2-[ 1-(2-fluorobenzyl)-1 H -pyrazolo[3,4-b )pyridin-3 -yl]-5-pyrimidinyl(methyl)carbamatecompound of formula-1 and its polymorphs thereof, represented by the fo

A method for synthesizing [...]

The invention relates to a method for synthesizing riociguat. The method includes the following steps: 1, a compound 1-(2-fluorobenzyl)-1H-[3,4-b] pyridine derivative-3-formamidine hydrochloride (1) and a compound benzeneazomalononitrile (2) are reacted i

Riociguat preparation method

The present invention discloses a new riociguat preparation method comprising the following steps: preparing intermediate N-substituted-benzyl-N-methyl-2-amino malononitrile shown in the structural formula V, preparing 5-(N-methyl) (R-substituted) benzyl amino-2-[1-(2-fluorobenzyl)-1 H-pyrazole [3, 4-b] pyridine-3-yl] pyrimidine-4, 6-diamine shown in the structural formula III, preparing 5-methyl amino-2-[1-(2-fluorobenzyl)-1 H-pyrazole [3, 4-b] pyridine-3-yl] pyrimidine-4, 6-diamine shown in the structural formula II, and preparing riociguat shown in the structural formula I. The obtained riociguat has high yield and purity, the occurrence of side effects can be effectively reduced, and production cost is saved.

Compound and application thereof in preparation of riociguat

The present invention discloses compound 5-methylamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo [3,4-b] pyridin-3-yl] pyrimidine-4,6-diamine, which can be used as an intermediate of riociguat and riociguat derivatives. The present invention also discloses a new method for the preparation of the riociguat by use of the intermediate, and the obtained riociguat has high yield and purity, the occurrence of side effects can be effectively reduced, and production cost is saved.