METHOD FOR PRODUCING OF 7-ALKYL-2,3-DIHYDRO-1H-PYRROLO[1,2-D][1,4]DYAZEPINE-4(5H)-ONE DERIVATIVES Russian patent published in 2018 - IPC C07D487/04 A61K31/551 

Abstract RU 2659390 C1

FIELD: chemistry.

SUBSTANCE: invention relates to process for production of 7-alkyl-2,3-dihydro-1H-pyrrolo[1,2-d][1,4]diazepine-4(5H)-one derivatives of formula 1, which can find application as substances possessing potential biological activity of a wide spectrum of action. Method for preparation of the 7-alkyl-2,3-dihydro-1H-pyrrolo[1,2-d][1,4]diazepin-4(5H)-one derivatives 1 is based on the simultaneous formation of two cycles of the pyrrolodiazepine framework as a result of the successive treatment of a mixture of alpha-amino acids and 2-(furan-2-yl)ethylamines with 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide and N-methylmorpholine in 1,2-dichloroethane, then a mixture of hydrochloric and acetic acids at room temperature and further cyclization by the method of Paal-Knorr by boiling in acetic acid for 30 minutes. Method allows the synthesis of 7-alkyl-2,3-dihydro-1H-pyrrolo[1,2-d][1,4]diazepin-4(5H)-one 1 derivatives with high yields.

EFFECT: new method for preparation of 7-alkyl-2,3-dihydro-1H-pyrrolo[1,2-d][1,4]diazepin-4(5H)-one 1 derivatives has been developed.

1 cl, 2 tbl, 5 ex

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RU 2 659 390 C1

Authors

Zelina Elena Yurevna

Nevolina Tatyana Anatolevna

Uchuskin Maksim Grigorevich

Sorotskaya Lyudmila Nazarovna

Trushkov Igor Viktorovich

Dates

2018-07-02Published

2017-11-03Filed