192187-30-7

Downstream Products

• 192187-31-8 6-(4-chlorobenzoyl)-4-(3-chlorophenyl)-3,4-dihydro-2(1H)-quinolinone 
• 406161-82-8 (+/-)-4-(3-chlorophenyl)-3,4-dihydro-6-(4-nitrobenzoyl)-2(1H)-quinolinone 
• 192185-72-1 tipifarnib 
• 192185-68-5 6-[amino(4-chlorophenyl)-1-methyl-1H-imidazol-5-ylmethyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone 
• 192185-51-6 4-(3-chlorophenyl)-6-[(4-chlorophenyl)hydroxy(1-methyl-1H-imidazol-5-yl)methyl]-1-methyl-2(1H)-quinolinone 
• 192187-32-9 R₁₀₁₇₆₃ 
• 192187-33-0 R₁₀₄₂₀₉ 

Relevant academic research and scientific papers

Efficient synthesis method of tipirfarnequinolinone intermediate

The invention provides an efficient synthesis method of 6-(4-chlorobenzoyl)-4-(3-chlorophenyl)-3, 4-dihydro-2(1H)-quinolinone as a tipirfarneb intermediate, and belongs to the technical field of organic synthesis. The method provided by the invention comprises the following steps: in the presence of an Eaton reagent, (E)-3-(3-chlorphenyl)-N-phenylacrylamide is subjected to a ring closing reaction in a solvent to generate 4-(3-chlorphenyl)-3, 4-dihydro-2(1H)-quinolinone, then 4-chlorobenzoic acid and a metal-doped modified molecular sieve catalyst are added into a reaction system, and a Friedel-Crafts acylation reaction is performed to obtain 6-(4-chlorobenzoyl)-4-(3-chlorophenyl)-3, 4-dihydro-2(1H)-quinolinone, namely the tipirfarnequinolinone intermediate. The synthesis method provided by the invention has the advantages of high product yield, easy purification, simple post-treatment operation, and good application value, and the catalyst can be recycled and reused.

Synthesis Routes Towards the Farnesyl Protein Transferase Inhibitor ZARNESTRA

The discovery that post-translational farnesylation of Ras oncoprotein was an essential step in exercising its biological effect led to the design of farnesyl protein transferase inhibitors (FTIs) in order to control growth of tumors bearing Ras mutations. Pre-clinical studies on murine models have confirmed their inhibitory effect on tumor growth and enabled clinical development. R115777 (ZARNESTRA) is currently undergoing clinical evaluation and recent studies have confirmed its antitumor potential and low toxicity. We wish to describe here the chemical synthesis routes that our group have developed to access ZARNESTRA. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.