Tsarkova Kseniya Valerevna (RU),Царькова Ксения Валерьевна (RU),Osipov Vasilij Nikolaevich (RU),Осипов Василий Николаевич (RU),Egorov Anton Sergeevich (RU),Егоров Антон Сергеевич (RU),Ubaskina Yuliya
申请号：
RU2019131109
公开号：
RU0002723481C1
申请日:
2019.10.03
申请国别(地区):
RU
年份:
2020
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing 4-[methyl 4-(aminomethyl)cyclohexane carboxylate]quinazoline, which is carried out by reacting equimolar amounts of 4-chloroquinazoline hydrochloride with methyl 4-(aminomethyl) cyclohexane carboxylate hydrochloride, carried out at room temperature and intensive stirring with addition of methyl 4-(aminomethyl) cyclohexane carboxylate in chloroform containing triethylamine in amount of 2–10 mol per mol of methyl 4-(aminomethyl)cyclohexane carboxylate hydrochloride dropwise to solution of 4-chloroquinazoline in chloroform. Obtained reaction mass is stirred at room temperature until formation of the end product while controlling the degree of conversion of the initial reagents to the end product by thin-layer chromatography using a mixture containing chloroform and methanol taken in the volume ratio of 10:1 as the eluent. Subsequent recovery of 4-[methyl 4-(aminomethyl)cyclohexane carboxylate]quinazoline is carried out in stages and involves filtration, washing the filtrate with water and a saturated sodium chloride solution, repeated washing with water, drying with sodium sulphate, evaporation in a vacuum, treatment with diethyl ether, repeated filtration and vacuum drying of the filtered precipitate of 4-[methyl 4-(aminomethyl)cyclohexane carboxylate]quinazoline. Output of end product is 85 %.EFFECT: obtained compound can be used as precursor for synthesis of potentially active inhibitors prolylpeptidase used in treating oncological diseases.3 cl, 1 dwg, 2 exИзобретение относится к способу получения 4-[метил 4-(аминометил)циклогексанкарбоксилат]хиназолина, который осуществляется реакцией взаимодействия эквимолярных количеств 4-хлорхиназолина с гидрохлоридом метил 4-(аминометил)циклогексанкарбоксилата, проводимой при комнатной температуре и интенсивном перемешивании при прибавлении по каплям к раствору 4-хлорхиназолина в хлороформе раствора гидрохлорида метил 4-(аминометил)циклогексанкарбоксилата в
