ChemicalBook CAS DataBase List 2-FLUORO-5-FORMYLBENZONITRILE

2-FLUORO-5-FORMYLBENZONITRILE synthesis

5synthesis methods

Product Name:2-FLUORO-5-FORMYLBENZONITRILE
CAS Number:218301-22-5
Molecular formula:C8H4FNO
Molecular Weight:149.12

2-Fluoro-5-formylbenzonitrile is a pharmaceutical intermediate that can be used to prepare olaparib intermediates. It can be synthesized by heating reaction of 3-bromo-4-fluoro-benzaldehyde with cuprous cyanide as raw material.

227609-85-0 Synthesis

Benzonitrile, 2-fluoro-5-(hydroxymethyl)- (9CI)

227609-85-0
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218301-22-5
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Yield:218301-22-5 84.7 g

Reaction Conditions:

with pyridinium chlorochromate in dichloromethane at 20;Reagent/catalyst;Temperature;

Steps:

3; 6 Example 6: Preparation of target product 2-fluoro-5-formylbenzonitrile

Put 500ml of dichloromethane in a 1000ml bottle, 138.9g of intermediate II crude product prepared in Example 5, cool and stir in a cold water bath.Add 200 g of pyridinium chlorochromate in batches, keep stirring the reaction at room temperature, and monitor by HPLC until the conversion of intermediate II is complete.The reaction solution was suction filtered, the filter cake was rinsed with 200ml of dichloromethane, the solvent was removed under reduced pressure, and the residue was recrystallized from toluene to obtain 84.7g of a yellow solid, namely the target product 2-fluoro-5-formylbenzonitrile, with a purity of >97% , yield 65%.

References:

CN114907234,2022,A Location in patent:Paragraph 0040-0041; 0046-0047