37622-90-5Relevant articles and documents
NAPHTHO[2,1 -D]THIAZOLE DERIVATIVES, COMPOSITIONS THEREOF AND METHODS OF TREATING DISORDERS
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Paragraph 0134, (2021/05/29)
The present application relates to the compounds of formula (I) that inhibit CDK9, pharmaceutical compositions thereof and methods of making and using the same.
Synthesis and preparation method of 4-pyrazole ethyl formate
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Paragraph 0037; 0040-0043; 0046-0049; 0052-0054, (2021/03/13)
The invention discloses a synthesis and preparation method of 4-pyrazole ethyl formate. The method comprises the following steps: dissolving ethyl 2-dichloroacetyl-3-(dimethylamino) acrylate in an organic solvent, and reacting with methylhydrazine to obtain ethyl 1-methyl-3-dichloromethyl-4-pyrazole formate; reacting the obtained ethyl 1-methyl-3-dichloromethyl-4-pyrazole formate with a fluorination reagent to obtain 1-methyl- 3-difluoromethyl-4-pyrazole ethyl formate; mixing 1-methyl- 3-difluoromethyl-4-pyrazole ethyl formate with glacial acetic acid, dropwise adding a strong acidic solutionat the temperature of 0 DEG C, and then adding dichloromethane and water for stirring and layering to obtain an organic layer; and recrystallizing the organic layer by using a mixed solvent of petroleum ether and ethyl acetate to obtain the 4-pyrazole ethyl formate. The method has the advantages of wide raw material source, low raw material price and simple preparation process, and the obtained product is easy to purify, low in production cost and suitable for large-scale industrial production.
Silica supported palladium-phosphine as a reusable catalyst for alkoxycarbonylation and aminocarbonylation of aryl and heteroaryl iodides
Mane, Rajendra Shivaji,Sasaki, Takehiko,Bhanage, Bhalchandra Mahadeo
, p. 94776 - 94785 (2015/11/24)
Silica-supported palladium phosphine complexes were prepared for alkoxycarbonylation and aminocarbonylation of aryl iodides. These catalysts were highly efficient for the carbonylation of unprotected hydroxy-aryl, amino-aryl, iodoindole and iodopyrazole. The carbonylation of unprotected iodopyrazole is challenging and their carbonylation was achieved for the first and obtained corresponding carbonylative products are biologically active. The applicability of developed protocols tolerates wide range of functional groups with excellent yields. The catalyst was easily recovered and shows significant recyclability up to five consecutive cycles without loss in its catalytic activity and selectivity. The prepared catalysts were characterized by different techniques such as FEG-SEM, EDS, FT-IR, XPS and ICP-AES spectroscopy.