22782-40-7

Usage

Class

benzene and substituted derivatives

Structure

contains a benzene ring with an amino group and a formyl group attached

Uses

used in the synthesis of pharmaceuticals and agrochemicals, as a building block in the production of dyes, pigments, and fine chemicals

Potential applications

in organic synthesis and chemical research

Upstream product

• 39263-32-6 2-amino-5-bromobenzonitrile 
• 68-12-2 N,N-dimethyl-formamide 
• 218301-22-5 2-fluoro-5-formylbenzonitrile 

Downstream Products

• 1092931-91-3 C₁₂H₁₅N₃ 

Relevant academic research and scientific papers

Scalable 18F processing conditions for copper-mediated radiofluorination chemistry facilitate DoE optimization studies and afford an improved synthesis of [18F]olaparib

A convenient and scalable base-free method for processing [18F]fluoride as [18F]TBAF is reported and applied to copper-mediated radiofluorination radiosyntheses. A central feature of this method is that a single production of [18F]TBAF can be divided into small aliquots that can be used to perform multiple small-scale reactions in DoE optimization studies. The results of these studies can then be reliably translated to full batch tracer productions using automated synthesizers. The processing method was applied to the DoE optimization of [18F]olaparib, affording the tracer in high radiochemical yields via both manual (%RCY = 78 ± 6%, n = 4 (CMRF step only)) and automated (up to 80% (%RCY); 41% activity yield (%AY)) radiosynthesis procedures.

Olaparib impurity intermediate, olaparib impurity and preparation method of olaparib impurity

The invention discloses an olaparib impurity intermediate, an olaparib impurity and a preparation method thereof. The olaparib impurity intermediate has the structure shown in the formula 2 and the structure shown in the formula 3; the olaparib impurity has the structure shown in the formula I. With 3-cyano-4-fluorobenzaldehyde as an initial material, the olaparib impurity intermediate shown as a formula 2 is prepared through amination and condensation reaction; then an impurity intermediate shown as a formula 3 is prepared through cyclization reaction; finally an olaparib impurity shown as a formula I is prepared through diazotization reduction reaction. According to the invention, the purity and yield of the prepared impurity are stable, and the method can be used for controlling the quality of the olaparib intermediate and crude drugs. By quantifying the specific impurities, the quality of crude drugs is improved.

RADIOLABELLED COMPOUND

The present invention relates to radiolabelled olaparib and in particular [ 18 F]olaparib, a process for producing radiolabelled olaparib, and uses of radiolabelled olaparib in medical imaging.

NEW COMPOUNDS

The present invention encompasses compounds of general Formula (I) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation

Heteroarylethanol-pyridylalkylamines for controlling animal growth

A compound for promoting livestock production and for controlling obesity in humans and animals, of the formula STR1 in which A represents =CH-- or =N--, R0 represents hydrogen or methyl, R1 and R3 each independently represents hydrogen, hydroxyl, halogen, cyano, alkyl, halogenoalkyl, hydroxyalkyl, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio, NHSO2 -alkyl, R2 represents hydrogen, hydroxyl, alkoxy or the radical --NR5 R6, R4 represents hydrogen, C1 -C10 -alkyl which is optionally substituted by hydroxyl, halogen, alkoxy, acyloxy or the radical --NH7 R8, or represents the radical COR9 or the radical --O--Z--R10, Z represents C1 -C10 -alkylene, -alkenylene or alkynylene, R5 represents hydrogen or alkyl, R6 represents hydrogen, alkyl, halogenoalkyl or acyl, or R5 and R6 together with the adjoining N atom form a saturated or unsaturated heterocyclic 4-, 5- or 6-membered ring, R7 and R8 each independently represents hydrogen, optionally substituted alkyl, optionally substituted aryl, R9 represents hydroxyl, alkoxy or the radical --NR7 R8, R10 represents hydroxyl, alkoxy, acyloxy, optionally substituted aryloxy or aralkyloxy, with the substituent R4 and the alkylamino group in the pyridyl ring of the formula I being in the p position with respect to one another, or a physiologically tolerated salt thereof, or, if A represents nitrogen, optionally the N-oxide thereof.