Title:
RIOCIGUAT INTERMEDIATE AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2016/202124
Kind Code:
A1
Abstract:
Disclosed are an intermediate, N-methyl-N-methyl formate-2-aminomalononitrile (II), for preparing Riociguat (I) and a preparation method therefor. Preparation steps comprise: 2-aminomalononitrile undergoes an n-methylation reaction to produce N-methyl-2-aminomalononitrile (IV), and N-methyl-2-aminomalononitrile (IV) undergoes an amidation reaction with methyl chloroformate or methyl bromoformate to produce N-methyl-N-methyl formate-2aminoalononitrile (II). The intermediate (II) undergoes a cyclization reaction with 1-(2- fluorobenzyl)-1H-pyrazol[3, 4-b]pyridine-3-formamidine (III) to produce Riociguat (I). The preparation method has readily available raw materials and a simple process and is economical, environmental friendly, and suitable for industrialized production.
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Inventors:
XU XUENONG (CN)
Application Number:
PCT/CN2016/081940
Publication Date:
December 22, 2016
Filing Date:
May 13, 2016
Export Citation:
Assignee:
SUZHOU MIRACPHARMA TECH CO LTD (CN)
International Classes:
C07D471/04; C07C271/22
Foreign References:
| CN104892459A | 2015-09-09 | |||
| CN104086545A | 2014-10-08 | |||
| CN104530044A | 2015-04-22 | |||
| CN1317005A | 2001-10-10 |
Other References:
JOACHIM MITTENDORF ET AL.: "Discovery of Riociguat (BAY 63-2521): A Potent, OralStimulator of Soluble Guanylate Cyclase for the Treatmentof Pulmonary Hypertension", CHEMMEDCHEM, vol. 4, 4 March 2009 (2009-03-04), pages 853 - 865, XP002622987
Attorney, Agent or Firm:
SUZHOU WISTONG INTELLECTUAL PROPERTY AGENCY (COMMON PARTNERSHIP) (CN)
苏州慧通知识产权代理事务所（普通合伙） (CN)
苏州慧通知识产权代理事务所（普通合伙） (CN)
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