RU2219170C2 - Способ получения нестероидного модулятора глюкокортикоидных рецепторов и промежуточные соединения - Google Patents

Способ получения нестероидного модулятора глюкокортикоидных рецепторов и промежуточные соединения Download PDF

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RU2219170C2
RU2219170C2 RU2001131115/04A RU2001131115A RU2219170C2 RU 2219170 C2 RU2219170 C2 RU 2219170C2 RU 2001131115/04 A RU2001131115/04 A RU 2001131115/04A RU 2001131115 A RU2001131115 A RU 2001131115A RU 2219170 C2 RU2219170 C2 RU 2219170C2
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Abstract

Описывается способ получения соединения формулы (1)
Figure 00000001

из карбоновой кислоты и амина в присутствии 1,1'-карбонилдиимидазола с использованием новых промежуточных соединений, а также новые промежуточные соединения. Технический результат - получение соединения, пригодного в качестве нестероидного модулятора глюкокортикоидных рецепторов. 7 с. и 9 з.п.ф-лы.

Description

Текст описания в факсимильном виде (см. графическую часть)а

Claims (16)

1. Способ получения соединения формулы
Figure 00000059
включающий взаимодействие соединения формулы
Figure 00000060
с амином формулы
Figure 00000061
в присутствии 1,1’-карбонилдиимидазола.
2. Способ по п.1, в котором получают соединение формулы II
Figure 00000062
включающий взаимодействие соединения формулы
Figure 00000063
с водным гидроксидом натрия в полярном протонном растворителе.
3. Способ по п.2, при котором получают соединение формулы III
Figure 00000064
включающий восстановление соединения формулы
Figure 00000065
водородом в присутствии катализатора.
4. Способ по п.3, при котором получают соединение формулы IV,
Figure 00000066
включающий взаимодействие соединения формулы
Figure 00000067
с трифторметилпропином.
5. Способ по п.4, при котором получают соединение формулы V
Figure 00000068
включающий восстановление соединения формулы
Figure 00000069
водородом в присутствии катализатора и карбоната калия.
6. Способ по п.5, при котором получают соединение формулы VI
Figure 00000070
включающий взаимодействие соединения формулы
Figure 00000071
с источником цианида в присутствии катализатора.
7. Способ по п.6, при котором получают соединение формулы (VII)
Figure 00000072
включающий взаимодействие соединения формулы
Figure 00000073
с метоксидом натрия.
8. Способ по п.7, при котором получают соединение формулы VIII
Figure 00000074
включающий взаимодействие соединения формулы
Figure 00000075
с метилвинилкетоном.
9. Способ по п.8, при котором получают соединение формулы XXII
Figure 00000076
включающий взаимодействие соединения формулы
Figure 00000077
с бензилгалидом.
10. Способ по п.9, при котором получают соединение формулы ХХIII,
Figure 00000078
включающий взаимодействие соединения формулы
Figure 00000079
с амином формулы
Figure 00000080
11. Соединение формулы
Figure 00000081
12. Соединение формулы
Figure 00000082
13. Соединение формулы
Figure 00000083
14. Соединение формулы
Figure 00000084
15. Соединение формулы
Figure 00000085
16. Соединение формулы
Figure 00000086
RU2001131115/04A 2000-10-27 2001-11-19 Способ получения нестероидного модулятора глюкокортикоидных рецепторов и промежуточные соединения RU2219170C2 (ru)

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