Boron Trifluoride-Acetic Acid Complex CAS 373-61-5

Preparation of Furotriptan Succinate
CN201410799863 discloses a preparation method of furatriptan succinate, which belongs to the technical field of drug synthesis and organic compound synthesis and preparation. Furotriptan was developed by Ireland’s Elan Pharm acutieallne, and was approved by the US FDA in November 2001 in the form of its succinate (1:1) for the acute treatment of migraine with or without aura. Frova. At present, this product is not registered for sale in China. The preparation method uses 4-cyanophenylhydrazine hydrochloride as the starting material, and N-methyl-1,4-dioxaspiro[4.5]decane-8-amine hydrochloride is cyclized in hydrochloric acid, and the After splitting L-pyroglutamic acid, use boron trifluoride acetic acid complex to catalyze hydrolysis, and then use succinic acid to form a salt to obtain the finished furovatriptan succinate. The method makes up for the deficiencies of the prior art, has simple synthesis process, stable yield and high purity, and is suitable for industrial production.

Synthesis of 2,4-dichlorobenzoic acid, an antimalarial drug aldipine hydrochloride drug intermediate
2,4-Dichlorobenzoic acid is white to light yellow needle-like crystal or powder, which is used as an intermediate in the production of dyes, pesticides, fungicides, and pharmaceuticals. The pharmaceutical industry is used to manufacture the antimalarial drug Adipine hydrochloride. But existing synthetic method mostly adopts potassium permanganate and dichlorotoluene to do reactant reaction, and process is more complicated, and final yield is not very high, therefore, be necessary to propose a kind of new synthetic method, this is useful for further improving The quality and yield of the product and the reduction of by-product content are of great economic significance.

CN201710157448.8 provides a kind of synthetic method of antimalarial drug aldipine hydrochloride pharmaceutical intermediate 2,4-dichlorobenzoic acid, comprising the following steps:

(i) Add 4-5mol of N,N-dimethylacetamide solution and 3-4mol of boron trifluoride acetic acid powder into the reaction vessel, control the stirring speed at 90-110rpm, keep it for 30-40min, then add 2mol of 2,4-dichloro-6-amino-isobutylbenzene solution, raise the temperature of the solution to 40-50°C, keep it for 100-130min, continue to raise the temperature to 60-70°C, keep it for 30-40min, precipitate out, filter , the precipitate is washed with 1-chloro-2-methylpropane solution, the filtrate and washing liquid are combined, the oxalic acid solution is added to adjust the pH value to 4-5, the temperature of the solution is lowered to 10-15°C, crystals are precipitated, filtered, dehydrating agent is dehydrated, In the finished product 2,4-dichlorobenzoic acid.