Abstract

A method for synthesizing a 3',5'-dichloro-2,2,2-trifluoroacetophenone derivative. The method specifically comprises the following steps: S1, preparing a Grignard reagent from a 1-bromo-3,5-dichloro-4-substituted compound by means of a grignardization reagent; and S2, reacting the Grignard reagent and a trifluoroacetyl compound, and then subjecting same to an acid treatment, so as to obtain a 3',5'-dichloro-2,2,2-trifluoroacetophenone derivative. The technical solution used in the present application has mild reaction conditions, involves readily available raw materials and has a relatively high yield, which helps to save the production cost of enterprises and is suitable for large-scale production.

IPC Classes  ?

• C07C 45/45 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by condensation
• C07C 49/80 - Ketones containing a keto group bound to a six-membered aromatic ring containing halogen

Abstract

The present application relates to the technical field of chemical pharmacy, and in particular, to a method for preparing 3,5-dihalotrifluoroacetophenone and a derivative thereof. 3-halogen-4-nitrotrifluoroacetophenone is used as a raw material, and the 3,5-dihalotrifluoroacetophenone derivative is finally obtained by means of a reduction reaction, a halogenation reaction and an amino substitution reaction. The raw material thereof is cheap and easily available, the process is simple, the conditions are mild, and the method has the prospect of large-scale production and has good economic effects.

IPC Classes  ?

• C07C 45/61 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups
• C07C 45/63 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by introduction of halogenPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by substitution of halogen atoms by other halogen atoms
• C07C 49/80 - Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
• C07C 49/825 - Ketones containing a keto group bound to a six-membered aromatic ring containing hydroxy groups all hydroxy groups bound to the ring
• C07C 245/20 - Diazonium compounds
• C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
• C07C 225/22 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton

Abstract

The present application relates to the technical field of chemical pharmaceutics, and in particular, to a synthesis method for 3',5'-dichloro-2,2,2-trifluoroacetophenone. The method comprises: first reacting 1,3,5-trichlorobenzene or 3,5-dichloro-1-bromobenzene with magnesium to form a Grignard reagent; and then subjecting the Grignard reagent and a trifluoroacetyl reagent to a nucleophilic addition reaction to obtain 3',5'-dichloro-2,2,2-trifluoroacetophenone after acid treatment. The synthesis method has mild reaction conditions, low raw material cost, favorable economic effect, and broad prospects for industrial production.

IPC Classes  ?

• C07C 45/45 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by condensation
• C07C 49/80 - Ketones containing a keto group bound to a six-membered aromatic ring containing halogen

Abstract

A method for preparing 3',5'-dichloro-2,2,2-trifluoroacetophenone. The method comprises subjecting 3'-chloro-2,2,2-trifluoroacetophenone as a raw material to four steps, i.e. nitrification, reduction, chlorination and deamination, so as to prepare 3',5'-dichloro-2,2,2-trifluoroacetophenone. The method is low in terms of raw material cost, mild in terms of reaction conditions, simple in terms of reaction process, beneficial to reducing production cost, and the economic effect is improved.

IPC Classes  ?

• C07C 45/61 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups
• C07C 49/80 - Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
• C07C 245/20 - Diazonium compounds
• C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
• C07C 225/22 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
• C07C 201/08 - Preparation of nitro compounds by substitution of hydrogen atoms by nitro groups
• C07C 205/45 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by at least one doubly-bound oxygen atom, not being part of a —CHO group