41218-84-2Relevant articles and documents
Synthetic method of epinastine hydrochloride
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, (2020/12/15)
The invention relates to a synthesis method of epinastine hydrochloride. The method comprises the following steps: reacting phthalic anhydride with aniline to obtain a compound 1, reacting the compound 1 with polyphosphoric acid under certain conditions to perform cyclization to obtain a compound 2, reducing carbonyl of the compound 2 under certain conditions to obtain a compound 3, and carrying out chlorination reaction on the compound 3 to obtain a compound 4, carrying out cyano substitution reaction on the compound 4 to obtain a compound 5, reducing the compound 5 by using a carbon-nitrogenunsaturated bond to obtain a compound 6, reacting the compound 6 with cyanogen bromide, and forming hydrochloride by using hydrochloric acid to obtain a compound 7; according to the method, the epinastine hydrochloride is prepared from bulk chemical products, is extremely low in price and mild in reaction condition, avoids the use of azide compounds, and the method is suitable for large-scale industrial production. The prepared epinastine hydrochloride is high in purity and low in cost, and has higher market competitiveness.
Synthesis method of epinastine hydrochloride
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Paragraph 0027-0029; 0032-0034; 0037-0039; 0042-0044, (2018/09/08)
The invention discloses a synthesis method of epinastine hydrochloride and relates to the technical field of medicines. The synthesis method comprises the following steps of: adopting 6-cyano-6,111H-dibenzo[b,e]azacycloheptatriene as a raw material, under the existence of RaneyNi, adopting methanol solution of ammonia as a solvent, introducing hydrogen to generate reduction reaction, and then obtaining 6-(aminomethyl)-6,11-dihydro-1H-dibenzo[b,e]azacycloheptatriene; leading the 6-(aminomethyl)-6,11-dihydro-1H-dibenzo[b,e]azacycloheptatriene and cyanogen bromide to generate cyclization reaction, then using alkaline for neutralization, and obtaining 3-amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5a]azacycloheptatriene; leading the 3-amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5a]azacycloheptatriene and hydrochloric acid to form a salt, and obtaining the epinastine hydrochloride. The synthesis method disclosed by the invention has the beneficial effects that in the reduction step, the RaneyNi is adopted as a catalyst, catalytic hydrogenation reaction is carried out in the methanol solution of the ammonia, the reaction conditions are moderate, the reaction time is shorter, the yield of reduction products can reach 90% or more, the whole synthesis process is stable, the reaction steps are simple, the consumed time is short and the prepared epinastine hydrochloride is high in purityand yield.
Synthetic method of epinastine hydrochloride
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Paragraph 0093; 0096; 0120, (2017/10/27)
The invention discloses a synthetic method of epinastine hydrochloride. The synthetic method comprises the following steps: enabling a substance A to react with a substance B to obtain a substance C; enabling the substance C to be subjected to ring closing reaction with polyphosphoric acid to obtain a substance D; enabling the substance D to react with a de-protection reagent to obtain a substance E; enabling the substance E to react with cyanogen bromide to obtain epinastine and then salifying with hydrochloric acids to obtain the epinastine hydrochloride. The synthetic method disclosed by the invention is easily-available in raw materials, mild in reaction conditions, low in energy consumption, low in production cost, simple to operate, short in preparation period and suitable for large-scale industrial production; the prepared epinastine hydrochloride is high in purity and relatively high in yield in each step of reaction.
