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2 517 170

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(51)

IPC

C07D231/54(2006-01-01)

(21) (22)

Application

2012115956/04, 2012-04-19

(24)

Start date

2012-04-19

(22)

Actual filing date

2012-04-19

(45)

Published

2014-05-27

(72)

Inventor

Dzhemilev Usein MemetovichTuktarov Ajrat RamilevichKhuzina Lilija Linatovna

(73)

Holder

Federal'Noe Gosudarstvennoe Bjudzhetnoe Uchrezhdenie Nauki Institut Neftekhimii I Kataliza Ran

METHOD OF PRODUCING N-ALKYL AND N-ARYLCARBOXAMIDYL-1aH,2'H-[1,2]PYRAZOLINO[3',4':1,9](C-I)-[5,6]FULLERENES Russian patent published in 2014 - IPC C07D231/54

Abstract RU 2517170 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to a method of producing functionally substituted fullerene derivatives, and specifically to a method of producing N-alkyl- and N-arylcarboxamidyl-1aH,2'H-[1,2]pyrazolino[3',4':1,9](C₆₀-I_h)-[5,6]fullerenes of formula (1). Said compounds can be used as highly active starting substances in synthesis of new-generation medicinal preparations for treating dangerous human diseases. The method involves reacting fullerene (C₆₀) (2) with alkyl- and aryldiazoamides of formula N₂CHC(O)NR (R = cyclohexyl, phenyl, adamantyl) in o-dichlorobenzene (o-DCB) in the presence of a three-component catalyst system {Pd(acac)₂ : 2PPh₃ : 4Et₃Al}, taken in molar ratio C₆₀ : diazo compound : Pd(acac)₂ : PPh₃ : Et₃Al = 1:(3-7):(0.1-0.3):(0.2-0.6):(0.4-1.2), preferably 1:5:0.2:0.4:0.8, at temperature of 80°C for 0.5-1.5 hours.

EFFECT: selective production of desired compounds with output of 44-68% , , , .

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RU 2 517 170 C2

Authors

Dzhemilev Usein Memetovich

Tuktarov Ajrat Ramilevich

Khuzina Lilija Linatovna

Dates

2014-05-27—Published

2012-04-19—Filed