306936-77-6

Usage

InChI:InChI=1/C6H7N3/c1-5-3-6(4-7)9(2)8-5/h3H,1-2H3

Upstream product

• 4027-57-0 ethyl 5-methyl-2H-pyrazole-3-carboxylate 
• 5744-40-1 ethyl 1,3-dimethylpyrazole-5-carboxylate 
• 5744-56-9 1,3-dimethylpyrazol-5-carboxylic acid 
• 25016-09-5 1,3-dimethyl-1H-pyrazole-5-carbaldehyde 
• 136678-93-8 1,3-dimethyl-1H-pyrazole-5-carboxamide 

Downstream Products

• 79080-36-7 2-cyano-1,4-dimethylimidazole 
• 19225-94-6 5-Cyan-1,2-dimethyl-imidazol 
• 1454846-35-5 (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile 
• 1454848-24-8 ((4-bromo-5-cyano-1-methyl-1H-pyrazol-3-yl)methyl)(methyl)carbamic acid tert-butyl ester 
• 499770-63-7 1-(1,3-dimethyl-1H-pyrazol-5-yl)methanamine 

Relevant academic research and scientific papers

MACROCYCLIC COMPOUNDS

Disclosed are macrocyclic compounds of formula (I) comprising a 2-carboxy indole ring. Such compounds, and their pharmaceutically acceptable salts, are useful as Mcl-1 (myeloid cell leukemia-1) inhibitors. The compounds may be used in treating a disease o

1-methyl-3-((methylamino)methyl)-1H-pyrazole-5-nitrile synthesis method

The invention belongs to the technical field of medicine and relates to a 1-methyl-3-((methylamino)methyl)-1H-pyrazole-5-nitrile synthesis method. Diethyl oxalate and acetone are easily acquirable andused as starting materials to obtain 1-methyl-3-((methylamino)methyl)-1H-pyrazole-5-nitrile through 7-step reaction including condensation, cyclization, methylation, amidation, oxidation, brominationand amination. By adoption of the method, preparation of 1-methyl-3-((methylamino)methyl)-1H-pyrazole-5-nitrile which is a key intermediate of antitumor drug lorlatinib (PF-06463922) is realized, thetotal yield reaches 5.7% or above, and simplicity in operation, convenience in aftertreatment, short time consumption and low cost are realized while industrialization can be realized beneficially. The intermediate and 5-fluoro-3-methyl isobenzofuran-1(3H)-ketone are subjected to reaction steps including ammonolysis, substitution, coupling, chiral resolution and the like to finally synthesize lorlatinib, and a novel method is provided for synthesis of the antitumor drug lorlatinib.

N-alkyl-cyanopyrazole synthetic method

The invention discloses an N-alkyl-cyanopyrazole synthetic method which comprises the following step of by taking 1-alkyl-1H-pyrazole formaldehyde or a derivative thereof, ammonia water, sodium bromate and acetic acid as raw materials and water as a reaction solvent to obtain N-alkyl-cyanopyrazole . The synthetic method provided by the invention is simple in technology without using extremely toxic substances, convenient in synthesis, high in yield, convenient in purification of an obtained product and beneficial to large-scale industrial production.

INHIBITORS OF HEPATITIS C VIRUS PROTEASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME

The present invention provides compounds of formula (I), (II) or (IV), or pharmaceutically acceptable salts and solvates thereof, which are useful as inhibitors of the Hepatitis C virus (HCV) protease enzyme and are also useful for the treatment of HCV infections in HCV--infected mammals, including humans. The present invention also provides pharmaceutical compositions comprising compounds of formula (I), (II) or (IV), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formulas (I), (II) and (IV).

2-(1H-INDAZOL-6-YLAMINO)-BENZAMIDE COMPOUNDS AS PROTEIN KINASES INHIBITORS USEFUL FOR THE TREATMENT OF OPHTALMIC DISEASES

Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating ophthalmic diseases and cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma,rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.