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RU2466994C2 - 7-членные циклические соединения, способы их получения и их фармацевтическое применение - Google Patents

7-членные циклические соединения, способы их получения и их фармацевтическое применение Download PDF

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RU2466994C2
RU2466994C2 RU2008152044/04A RU2008152044A RU2466994C2 RU 2466994 C2 RU2466994 C2 RU 2466994C2 RU 2008152044/04 A RU2008152044/04 A RU 2008152044/04A RU 2008152044 A RU2008152044 A RU 2008152044A RU 2466994 C2 RU2466994 C2 RU 2466994C2
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formula
alkyl
compound
alkoxy
iii
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Цуёси МУТО (JP)
Цуёси МУТО
Таисаку ТАНАКА (JP)
Таисаку ТАНАКА
Хироси МАРУОКА (JP)
Хироси МАРУОКА
Сеиити ИМАДЗО (JP)
Сеиити ИМАДЗО
Ёсиаки ТОМИМОРИ (JP)
Ёсиаки ТОМИМОРИ
Кодзи САТО (JP)
Кодзи САТО
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Цутоми ЯГИ
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Дайити Санкё Компани, Лимитед
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Abstract

Описывается способ получения 7-членных гетероциклических соединений формулы (R-Ia) и (S-Ia)
Figure 00000296
Figure 00000297
где значения радикалов приведены в формуле изобретения, исходя из соединения (Vaa)
Figure 00000298
через соответствующее изоцианатное производное и взаимодействие последнего с соответствующим диазепиновым реагентом. Целевые соединения обладают ингибирующей активностью в отношении химазы. 1 з.п.ф-лы, 331 прим., 12 табл.

Description

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Claims (2)

1. Способ получения соединения формулы (R-Ia) или (S-Ia)
Figure 00000288

Figure 00000289

где R2 и R3 независимо представляют собой (1) водород, (2) галоген или (3) C1-С6алкил;
R5 и R6 независимо представляют собой (1) водород или (2) C1-С6алкил необязательно замещенный группой, выбранной из группы, состоящей из (i) карбоксила, (ii) C1-С6алкокси, (iii) C1-С6алкоксикарбонила, (iv) C6-С12арилоксикарбонила, (v) С1-С10 гетероарилоксикарбонила и (vi) амино;
R2 и R3, а также R5 и R6 независимо могут образовывать 3-8-членное кольцо;
Ar' представляет собой (С6-С14) ароматическую углеводородную группу, которая может быть замещена 1-5 группами, выбранными из группы, состоящей из (i) атомов галогена, (ii) нитро, (iii) циано, (iv) (С1-С6)-алкила, который может быть, необязательно, замещен 1-3 атомами галогена, и (v) (С1-С6)-алкокси, который может быть необязательно замещен 1-3 атомами галогена,
Ха представляет собой линейный или разветвленный (С1-С6)-алкилен,
R7a представляет собой (С1-С6)-алкил, который может быть необязательно замещен группой, выбранной из группы, состоящей (i) карбоксила, (ii) (C1-С6)-алкоксикарбонила, (iii) фенила, (iv) гидроксила, (v) (С1-С6)-алкокси и (vi) атома галогена;
R8a представляет собой атом водорода;
R26, R27 и R28 могут быть одинаковыми или разными и обозначают (i) атом водорода, (ii) атом галогена, (iii) циано, (iv) нитро, (v) (С1-С6)-алкил, (vi) (С1-С6)-алкокси, (vii) (С1-С6)-алкоксикарбонил, (viii) (C1-С6)-алкилсульфонил, (ix) карбоксил, (х) карбокси-(С1-С6)-алкил, (xi) гидроксил или (xii) амино,
или его соли, или сольвата,
включающий:
превращение соединения формулы (Vaa)
Figure 00000290

где R7a и R8a имеют значения, указанные выше, a R26a, R27a и R28a могут быть одинаковыми или разными и обозначают (i) атом водорода, (ii) атом галогена, (iii) циано, (iv) нитро, (v) (С1-С6)-алкил, (vi) (С1-С6)-алкокси, (vii) (С1-С6)-алкоксикарбонил, (viii) (С1-С6)-алкилсульфонил, (ix) карбоксил, защищенный трет-бутилом, бензилом или 4-метоксибензилом, (х) карбокси-(С1-С6)-алкил, защищенный трет-бутилом, бензилом или 4-метоксибензилом, или (xi) гидроксил, защищенный трет-бутилом, бензилом или 4-метоксибензилом, или его соли
в соединение формулы (1Ха)
Figure 00000291

где R7a, R8a, R26a, R27a и R28a имеют значения, указанные выше,
последующую реакцию сочетания полученного соединения формулы (1Ха) и соединения формулы (R-IIIa) или (S-IIIa)
Figure 00000292

Figure 00000293

где Ar', Ха, R2, R3, R5 и R6 имеют значения, указанные выше, а Ра обозначает бензил, 4-метоксибензил, 2,4-диметоксибензил или 2,4,6-триметоксибензил,
которая дает соединение формулы (R-Ib) или формулы (S-Ib):
Figure 00000294

Figure 00000295

где Ar', Ха, R2, R3, R5, R6, R7a, R8a, R26a, R27a, R28a и Ра имеют значения, указанные выше,
и удаление Pa из полученного соединения формулы (R-Ib) или формулы (S-Ib) и необязательное восстановление и/или гидролиз полученного соединения одновременно с удалением Ра, или перед удалением Ра, и/или после удаления Ра в случае, когда R26a, R27a или R28a полученного соединения имеют защитную группу, или в случае, когда R26a, R27a или R28a полученного соединения представляют собой нитро, и R26, R27 или R28 этих соединений, имеющих формулу (R-Ia) или (S-Ia), представляют собой амино.
2. Способ по п.1, где Ar' представляет собой фенил, который необязательно замещен 1-5 группами, выбранными из (i) атома галогена, (ii) нитро, (iii) циано, (iv) C1-С6алкила, который необязательно замещен 1-3 атомами галогена, и (v) C1-С6алкокси, который необязательно замещен 1-3 атомами галогена, и R2, R3, R5 и R6 все являются водородом.
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