Synthetic route of Copanlisib

The synthetic route of Copanlisib/Copanlisib (Copanlisib) is complex and usually involves multiple intermediates and multiple reaction steps. The following is a brief synthesis route of copanliside/Cupanisi, which includes some main reaction steps:

1.Bromobenzophenones synthesis: The first step in the synthesis usually involves converting benzophenones into the corresponding bromobenzophenones. This can be achieved by performing a bromination reaction under alkaline conditions using a brominating agent such as bromine or phosphorus tribromide.

2.Preparation of aldehydes: Bromobenzophenone can be reduced to aldehydes through appropriate reactions. A typical reducing reagent is hydrogen and a catalyst (such as lithium aluminum hydride).

3.Arylation of aldehydes: The aldehyde in the synthesis intermediate can react with an appropriate arylamine to generate an aryl compound.

4.Synthesis of Ketones: Aryl compounds can be further oxidized to convert aldehydes into the corresponding ketones.

5.Epoxidation reaction: This is the key step in the synthesis of copanliside/cupanisi. Ketone compounds form an epoxy ring through an epoxidation reaction, usually using t-butyl peroxide or a similar oxidizing agent.

6.Ring-opening of the epoxy ring: The epoxy ring can be opened in the reaction by an appropriate acid catalyst to generate the skeleton structure of copanliside/cupanisi.

7.Copanliside/Modification of Kupanisi: Finally, some necessary chemical modifications can be made to the generated copanliside/cupanisi skeleton to obtain the desired product.

It should be pointed out that this is only a brief example of the synthetic route of Copanliside/Kupanisi. The actual synthesis may be more complex, including more intermediates and delicate chemical steps. In addition, the synthesis process requires strict control and purification to ensure the purity and quality of the product. This process is usually performed in specialized chemical laboratories and requires rigorous chemical techniques and equipment.

Copanliside/Kupanisi has just been launched in China and has not been included in medical insurance. The specific price may not be determined yet. Please consult your local pharmacy for details. There is only the American version of the original drug available abroad, and the price is as high as more than 70,000 yuan.