RU98119523A - COMPOUNDS OF PIPERAZIN AND PIPERIDINE - Google Patents

COMPOUNDS OF PIPERAZIN AND PIPERIDINE

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Publication number
RU98119523A
RU98119523A RU98119523/04A RU98119523A RU98119523A RU 98119523 A RU98119523 A RU 98119523A RU 98119523/04 A RU98119523/04 A RU 98119523/04A RU 98119523 A RU98119523 A RU 98119523A RU 98119523 A RU98119523 A RU 98119523A
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RU
Russia
Prior art keywords
formula
group
compound
salts
phenyl
Prior art date
Application number
RU98119523/04A
Other languages
Russian (ru)
Other versions
RU2178414C2 (en
Inventor
Рулоф Виллем Фенстра
Корнелис Геррит Крюсе
Мартинус Теодорус Мария Тюлп
Вильма Кейперс
Стивен Кеннет Лонг
Original Assignee
Дюфар Интернэшнл Рисерч Б.В.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Дюфар Интернэшнл Рисерч Б.В. filed Critical Дюфар Интернэшнл Рисерч Б.В.
Publication of RU98119523A publication Critical patent/RU98119523A/en
Application granted granted Critical
Publication of RU2178414C2 publication Critical patent/RU2178414C2/en

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Claims (6)

1. Соединения формулы a
Figure 00000001

в которой A обозначает гетероциклическую группу с 5-7 атомами в кольце, содержащую 1-3 гетероатомами из группы O, N и S; R1 обозначает водород или фтор; R2 обозначает C1-4алкил, C1-4алкокси или оксогруппу, и p равен 0, 1 или 2; Z обозначает углерод или азот, и пунктирная линия обозначает простую связь, когда Z является азотом, и простую или двойную связь, когда Z является углеродом; R3 и R4 независимо друг от друга обозначают водород или C1-4алкил; n равен 1 или 2; R5 обозначает галоген, гидрокси, C1-4алкокси или C1-4алкил, и q равен 0, 1, 2 или 3; Y обозначает фенил, фуранил или тиенил, которые могут быть замещены 1-3 заместителями из группы гидрокси, галоген, C1-4алкокси, C1-4алкил, циано, аминокарбонил, моно- иди ди-C1-4алкиламинокарбонил; и их соли.1. The compounds of formula a
Figure 00000001

in which A denotes a heterocyclic group with 5-7 atoms in the ring, containing 1-3 heteroatoms from the group O, N and S; R 1 denotes hydrogen or fluorine; R 2 is C 1-4 alkyl, C 1-4 alkoxy or oxo, and p is 0, 1 or 2; Z is carbon or nitrogen, and the dotted line indicates a single bond when Z is nitrogen, and a single or double bond when Z is carbon; R 3 and R 4 independently of one another denote hydrogen or C 1-4 alkyl; n is 1 or 2; R 5 is halogen, hydroxy, C 1-4 alkoxy or C 1-4 alkyl, and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which may be substituted by 1 to 3 substituents from the group of hydroxy, halogen, C 1-4 alkoxy, C 1-4 alkyl, cyano, aminocarbonyl, mono di di C 1-4 alkylaminocarbonyl; and their salts. 2. Соединения по п.1, отличающиеся тем, что A вместе с фенильной группой является группой формулы b-m. 2. Compounds according to claim 1, characterized in that A together with a phenyl group is a group of the formula b-m.
Figure 00000002

Figure 00000003

Figure 00000004

Figure 00000005

Figure 00000006

Figure 00000007

в которой R1 и (R2)p имеют значения, указанные в п.1, n равен 1, R3, R4, (R5)q, Y и Z имеют значения, указанные в пункте 1, и их соли.
Figure 00000002

Figure 00000003

Figure 00000004

Figure 00000005

Figure 00000006

Figure 00000007

in which R 1 and (R 2 ) p have the meanings indicated in item 1, n is 1, R 3 , R 4 , (R 5 ) q, Y and Z have the meanings indicated in item 1 and their salts. 3. Соединения по п.2, отличающиеся тем, что A вместе с фенильной группой является группой формулы (b), или группой формулы (I), которая замещена в гетерокольце оксогруппой, Y обозначает фенил, который может быть замещен, как указано в п.1, Z обозначает азот, и их соли. 3. Compounds according to claim 2, characterized in that A together with a phenyl group is a group of formula (b), or a group of formula (I) which is substituted in the hetero ring with an oxo group, Y represents phenyl which may be substituted as indicated in .1, Z denotes nitrogen, and their salts. 4. Соединения по п.3, отличающиеся тем, что R3 и R4 обозначают водород, R5 обозначает водород, гидрокси, метокси или галоген, Y имеет значения, указанные в п.3, и их соли.4. Compounds according to claim 3, wherein R 3 and R 4 are hydrogen, R 5 is hydrogen, hydroxy, methoxy or halogen, Y is as defined in claim 3, and their salts. 5. Соединения по п.4, отличающиеся тем, что A вместе с фенильной группой формулы (I), которая замещена в гетерокольце оксогруппой, R5 обозначает водород, Y обозначает фенил, и их соли.5. Compounds according to claim 4, characterized in that A together with the phenyl group of formula (I), which is substituted in the hetero ring by an oxo group, R 5 is hydrogen, Y is phenyl, and their salts. 6. Способ получения соединений, заявленных в п.1, который заключается в том, что a) соединение формулы n
Figure 00000008

подвергают взаимодействию с соединением формулы
Figure 00000009

в которой X является отщепляемой группой; или b) соединение формулы n подвергают взаимодействию с соединением формулы
Figure 00000010

и формальдегидом; или c) соединение формулы n подвергают взаимодействию с соединением формулы
Figure 00000011

с последующим восстановлением кетогруппы; или d) соединение формулы
Figure 00000012

подвергают взаимодействию с соединением Y-Br; или e) соединение формулы
Figure 00000013

подвергают взаимодействию с соединением формулы
B(OH)2-Y
причем символы, используемые в этих формулах, имеют значения, указанные в п.1.6. The method of producing compounds claimed in claim 1, which is that a) a compound of the formula n
Figure 00000008

subjected to interaction with the compound of the formula
Figure 00000009

in which X is a leaving group; or b) a compound of formula n is reacted with a compound of formula
Figure 00000010

and formaldehyde; or c) a compound of formula n is reacted with a compound of formula
Figure 00000011

with the subsequent restoration of ketogroup; or d) a compound of the formula
Figure 00000012

subjected to interaction with the compound Y-Br; or e) a compound of the formula
Figure 00000013

subjected to interaction with the compound of the formula
B (OH) 2 -Y
moreover, the symbols used in these formulas have the meanings indicated in paragraph 1.
RU98119523/04A 1996-03-29 1997-03-20 Derivatives of piperazine and piperidine and method of their synthesis RU2178414C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP96200864.5 1996-03-29
EP96200864 1996-03-29

Publications (2)

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RU98119523A true RU98119523A (en) 2000-10-20
RU2178414C2 RU2178414C2 (en) 2002-01-20

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US (1) US6225312B1 (en)
EP (1) EP0889889B1 (en)
JP (1) JP3989554B2 (en)
CN (1) CN1100055C (en)
AT (1) ATE340173T1 (en)
AU (1) AU708053B2 (en)
BR (1) BRPI9708389B8 (en)
CA (1) CA2250347C (en)
CZ (1) CZ294413B6 (en)
DE (1) DE69736704T2 (en)
DK (1) DK0889889T3 (en)
ES (1) ES2271967T3 (en)
HU (1) HU227454B1 (en)
IL (1) IL126187A0 (en)
NO (1) NO320970B1 (en)
NZ (1) NZ331860A (en)
PL (1) PL189256B1 (en)
PT (1) PT889889E (en)
RU (1) RU2178414C2 (en)
SK (1) SK285119B6 (en)
TR (1) TR199801942T2 (en)
TW (1) TW422846B (en)
UA (1) UA52656C2 (en)
WO (1) WO1997036893A1 (en)
ZA (1) ZA972639B (en)

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