870063-52-8Relevant articles and documents
Preparation method of 5-fluoro-3-iodo-1H-pyrazolo [3, 4-b] pyridine
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Paragraph 0020, (2021/09/08)
The invention discloses a preparation method of 5-fluoro-3-iodo-1H-pyrazolo [3, 4-b] pyridine, and belongs to the field of medicinal chemistry. The method specifically comprises the following steps: S1, carrying out reduction reaction on 2-chloro-5-fluoronicotinic acid serving as a starting point to obtain 2-chloro-3-hydroxymethyl-5-fluoropyridine; S2,carrying out oxidation reaction on the 2-chloro-3-hydroxymethyl-5-fluoropyridineto obtain 2-chloro-3-formyl-5-fluoropyridine; S3, enabling that the 2-chloro-3-formyl-5-fluoropyridine is subjected to ring closing through hydrazine hydrate, so that 5-fluoro-1H-pyrazolo [3, 4-b] pyridine is obtained; and S4, carrying out an iodination reaction on the 5-fluoro-1H-pyrazolo [3, 4-b] pyridine, so as to obtain the 5-fluoro-3-iodo-1H-pyrazolo [3, 4-b] pyridine. The four-step reaction of the preparation method does not use strongly corrosive acidic materials, so that the preparation method has the advantages of high safety operability, small damage to equipment and facilities, high safety operability in material storage, transfer and use links, avoidance of diazonium salt reaction for releasing nitrogen in the prior art, high safety controllability, mild reaction conditions, higher safety, simplicity in operation, high yield, and suitability for industrial production.
ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF BIRTHMARKS
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Paragraph 0567, (2020/06/10)
Provided herein are compounds and pharmaceutical compositions thereof for treating a birthmark in a subject in need thereof, wherein the compound is according to any one of formula (1), (II), (III), (IV), and (V). wherein X1, X2, X3, R1, R2, R2a, R13, R13a, R23, R23a, R23b, R33, R33a, R33b, R43, R43a, R51, R53, R53a, R53b, bond "a", and subscript n are described herein.
HETEROCYCLIC COMPOUNDS WITH AN ROR(GAMMA)T MODULATING ACTIVITY
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, (2018/03/06)
The present invention relates to a compound that may have an ROR(gamma)t modulating activity and can thus be useful in the treatment of cancer.